Informacja

Drogi użytkowniku, aplikacja do prawidłowego działania wymaga obsługi JavaScript. Proszę włącz obsługę JavaScript w Twojej przeglądarce.

Przeglądasz jako GOŚĆ

Wyszukujesz frazę ""Half-Life"" wg kryterium: Temat


Tytuł :
The impact of extended half-life factor concentrates on prophylaxis for severe hemophilia in the United States.
Autorzy :
Malec LM; Versiti Blood Research Institute, Milwaukee, Wisconsin.; Medical College of Wisconsin, Milwaukee, Wisconsin.
Cheng D; American Thrombosis and Hemostasis Network, Chicago, Illinois.
Witmer CM; The Children's Hospital of Philadelphia, Philadelphia, Pennsylvania.
Jaffray J; Keck School of Medicine, Children's Hospital Los Angeles, University of Southern California, Los Angeles, California.
Kouides PA; Mary M. Gooley Hemophilia Center, Rochester, New York.
Haley KM; Oregon Health & Science University, Portland, Oregon.
Sidonio RF Jr; Children's Healthcare of Atlanta, Atlanta, Georgia.
Johnson K; Versiti Blood Research Institute, Milwaukee, Wisconsin.
Recht M; American Thrombosis and Hemostasis Network, Chicago, Illinois.; Oregon Health & Science University, Portland, Oregon.
White G; Versiti Blood Research Institute, Milwaukee, Wisconsin.; Medical College of Wisconsin, Milwaukee, Wisconsin.
Croteau SE; Boston Hemophilia Center, Boston Children's Hospital, Boston, Maryland.
Ragni MV; Hemophilia Center of Western Pennsylvania, Pittsburgh, Pennsylvania.; University of Pittsburgh, Pittsburgh, Pennsylvania.
Pokaż więcej
Źródło :
American journal of hematology [Am J Hematol] 2020 Aug; Vol. 95 (8), pp. 960-965.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Half-Life*
Hemophilia A/*therapy
Adolescent ; Adult ; Aged ; Cohort Studies ; Female ; Humans ; Male ; Middle Aged ; United States ; Young Adult
Czasopismo naukowe
Tytuł :
Real-world outcomes associated with standard half-life and extended half-life factor replacement products for treatment of haemophilia A and B.
Autorzy :
Chhabra A; Pfizer Inc, New York, New York, USA.
Spurden D; Pfizer Limited, Tadworth, Surrey, UK.
Fogarty PF; Pfizer Inc, Collegeville, Pennsylvania, USA.
Tortella BJ; Pfizer Inc, Collegeville, Pennsylvania, USA.
Rubinstein E; Pfizer Inc, New York, New York, USA.
Harris S; Pfizer Limited, Tadworth, Surrey, UK.
Pleil AM; Pfizer Inc, San Diego, California, USA.
Mellor J; Adelphi Real World, Bollington, Cheshire, UK.
de Courcy J; Adelphi Real World, Bollington, Cheshire, UK.
Alvir J; Pfizer Inc, New York, New York, USA.
Pokaż więcej
Źródło :
Blood coagulation & fibrinolysis : an international journal in haemostasis and thrombosis [Blood Coagul Fibrinolysis] 2020 Apr; Vol. 31 (3), pp. 186-192.
Typ publikacji :
Journal Article
MeSH Terms :
Half-Life*
Hemophilia A/*drug therapy
Hemophilia B/*drug therapy
Female ; Humans ; Male ; Treatment Outcome
Czasopismo naukowe
Tytuł :
First report on chemometric modeling of hydrolysis half-lives of organic chemicals.
Autorzy :
Khan PM; Department of Pharmacoinformatics, National Institute of Pharmaceutical Educational and Research (NIPER), Chunilal Bhawan, 168, Manikatala Main Road, Kolkata, 700054, India.
Lombardo A; Laboratory of Environmental Chemistry and Toxicology, Department of Environmental Health, Istituto Di Ricerche Farmacologiche Mario Negri IRCCS, Via Mario Negri, 2, 20156, Milano, Italy.
Benfenati E; Laboratory of Environmental Chemistry and Toxicology, Department of Environmental Health, Istituto Di Ricerche Farmacologiche Mario Negri IRCCS, Via Mario Negri, 2, 20156, Milano, Italy.
Roy K; Drug Theoretics and Cheminformatics Laboratory, Department of Pharmaceutical Technology, Jadavpur University, 188 Raja S C Mullick Road, Kolkata, 700032, India. .
Pokaż więcej
Źródło :
Environmental science and pollution research international [Environ Sci Pollut Res Int] 2021 Jan; Vol. 28 (2), pp. 1627-1642. Date of Electronic Publication: 2020 Aug 26.
Typ publikacji :
Journal Article
MeSH Terms :
Organic Chemicals*
Quantitative Structure-Activity Relationship*
Half-Life ; Hydrolysis ; Least-Squares Analysis
Czasopismo naukowe
Tytuł :
Bifenthrin in the tropical sugarcane ecosystem: persistence and environmental risk assessment.
Autorzy :
Ramasubramanian T; Division of Crop Protection, ICAR-Sugarcane Breeding Institute, Indian Council of Agricultural Research, Coimbatore, Tamil Nadu, 641 007, India. .
Paramasivam M; Pesticide Toxicology Laboratory, Department of Agricultural Entomology, Tamil Nadu Agricultural University, Coimbatore, 641 003, India.
Pokaż więcej
Źródło :
Environmental science and pollution research international [Environ Sci Pollut Res Int] 2021 Jan; Vol. 28 (3), pp. 3524-3532. Date of Electronic Publication: 2020 Sep 12.
Typ publikacji :
Journal Article
MeSH Terms :
Insecticides*/analysis
Pesticide Residues*/analysis
Saccharum*
Soil Pollutants*/analysis
Ecosystem ; Environmental Monitoring ; Half-Life ; Pyrethrins ; Risk Assessment ; Soil
Czasopismo naukowe
Tytuł :
Prediction of half-life for adsorption kinetics in a batch reactor.
Autorzy :
Hu Q; College of Ecology and Environment, Chengdu University of Technology, Chengdu, 610059, China. .; Graduate School of Life and Environmental Sciences, University of Tsukuba, Ibaraki, 305-8572, Japan. .
Zhang Z; Graduate School of Life and Environmental Sciences, University of Tsukuba, Ibaraki, 305-8572, Japan.
Pokaż więcej
Źródło :
Environmental science and pollution research international [Environ Sci Pollut Res Int] 2020 Dec; Vol. 27 (35), pp. 43865-43869. Date of Electronic Publication: 2020 Aug 01.
Typ publikacji :
Journal Article
MeSH Terms :
Bentonite*
Water Pollutants, Chemical*
Adsorption ; Half-Life ; Hydrogen-Ion Concentration ; Kinetics ; Phosphates
Czasopismo naukowe
Tytuł :
Direct comparison of two extended half-life PEGylated recombinant FVIII products: a randomized, crossover pharmacokinetic study in patients with severe hemophilia A.
Autorzy :
Solms A; Clinical Pharmacometrics, Pharmaceuticals Research & Development, Bayer AG, 13353, Berlin, Germany. .
Shah A; Bayer, Whippany, NJ, USA.
Berntorp E; Centre for Thrombosis and Haemostasis, Lund University, Skåne University Hospital, Malmö, Sweden.
Tiede A; Department of Hematology, Hemostasis, Oncology and Stem Cell Transplantation, Hannover Medical School, Hanover, Germany.
Iorio A; McMaster-Bayer Endowed Research Chair in Clinical Epidemiology of Congenital Bleeding Disorders, Department of Medicine, McMaster University, Hamilton, Canada.; Department of Health Research Methods, Evidence and Impact, McMaster University, Hamilton, Canada.
Linardi C; Bayer, Whippany, NJ, USA.
Ahsman M; LAP&P Consultants BV, Leiden, the Netherlands.
Mancuso ME; Center for Thrombosis and Hemorrhagic Diseases, Humanitas Clinical and Research Center - IRCCS, Rozzano, Milan, Italy.
Zhivkov T; Specialized Hospital for Active Treatment, Sofia, Bulgaria.
Lissitchkov T; Specialized Hospital for Active Treatment, Sofia, Bulgaria.
Pokaż więcej
Źródło :
Annals of hematology [Ann Hematol] 2020 Nov; Vol. 99 (11), pp. 2689-2698. Date of Electronic Publication: 2020 Sep 24.
Typ publikacji :
Clinical Trial; Comparative Study; Journal Article; Randomized Controlled Trial
MeSH Terms :
Factor VIII*/administration & dosage
Factor VIII*/pharmacokinetics
Hemophilia A*/blood
Hemophilia A*/drug therapy
Adolescent ; Adult ; Aged ; Cross-Over Studies ; Half-Life ; Humans ; Male ; Middle Aged ; Polyethylene Glycols ; Recombinant Proteins/administration & dosage ; Recombinant Proteins/pharmacokinetics
Czasopismo naukowe
Tytuł :
Residue and dissipation kinetics of toosendanin in cabbage, tobacco and soil using IC-ELISA detection.
Autorzy :
Li H; College of Plant Protection, Northwest A&F University, Yangling 712100, Shaanxi, China.
He S; College of Plant Protection, Northwest A&F University, Yangling 712100, Shaanxi, China.
Liu G; College of Plant Protection, Northwest A&F University, Yangling 712100, Shaanxi, China.
Li C; College of Plant Protection, Northwest A&F University, Yangling 712100, Shaanxi, China.
Ma Z; College of Plant Protection, Northwest A&F University, Yangling 712100, Shaanxi, China; Provincial Center for Bio-Pesticide Engineering, Yangling, Shaanxi Province 712100, China. Electronic address: .
Zhang X; Provincial Center for Bio-Pesticide Engineering, Yangling, Shaanxi Province 712100, China.
Pokaż więcej
Źródło :
Food chemistry [Food Chem] 2021 Jan 15; Vol. 335, pp. 127600. Date of Electronic Publication: 2020 Jul 18.
Typ publikacji :
Journal Article
MeSH Terms :
Brassica/*metabolism
Drugs, Chinese Herbal/*metabolism
Enzyme-Linked Immunosorbent Assay/*methods
Soil/*chemistry
Soil Pollutants/*metabolism
China ; Chromatography, High Pressure Liquid/methods ; Half-Life ; Kinetics ; Pesticide Residues/analysis ; Tobacco
Czasopismo naukowe
Tytuł :
Dissipation behavior of thiophanate-methyl in strawberry under open field condition in Egypt and consumer risk assessment.
Autorzy :
Malhat F; Pesticide Residues and Environmental Pollution Department, Central Agricultural Pesticide Laboratory, Agricultural Research Center, Dokki, Giza, 12618, Egypt. .
Abdallah O; Pesticide Residues and Environmental Pollution Department, Central Agricultural Pesticide Laboratory, Agricultural Research Center, Dokki, Giza, 12618, Egypt.
Ahmed F; Pesticide Residues and Environmental Pollution Department, Central Agricultural Pesticide Laboratory, Agricultural Research Center, Dokki, Giza, 12618, Egypt.
Salam SA; Pesticide Residues and Environmental Pollution Department, Central Agricultural Pesticide Laboratory, Agricultural Research Center, Dokki, Giza, 12618, Egypt.
Anagnostopoulos C; Department of Pesticides Control and Phytopharmacy, Laboratory of Pesticides Residues, Benaki Phytopathological Institute, 8 St. Delta Street, Kifissia, 14561, Athens, Greece. .
Ahmed MT; Plant Protection Department, Faculty of Agriculture, Suez Canal University, Ismailia, 41522, Egypt.
Pokaż więcej
Źródło :
Environmental science and pollution research international [Environ Sci Pollut Res Int] 2021 Jan; Vol. 28 (1), pp. 1029-1039. Date of Electronic Publication: 2020 Aug 22.
Typ publikacji :
Journal Article
MeSH Terms :
Fragaria*
Fungicides, Industrial*/analysis
Pesticide Residues*/analysis
Chromatography, Liquid ; Egypt ; Half-Life ; Risk Assessment ; Tandem Mass Spectrometry ; Thiophanate/analysis
Czasopismo naukowe
Tytuł :
Measuring the impact of changing from standard half-life (SHL) to extended half-life (EHL) FVIII prophylaxis on health-related quality of life (HRQoL) in boys with moderate/severe haemophilia A: Lessons learned with the CHO-KLAT tool.
Autorzy :
Carcao M; Child Health Evaluative Sciences, The Hospital for Sick Children Research Institute, Toronto, ON.; Division of Hematology/Oncology, The Hospital for Sick Children, Toronto, ON, Canada.; Department of Pediatrics, University of Toronto, Toronto, ON, Canada.
Zunino L; Child Health Evaluative Sciences, The Hospital for Sick Children Research Institute, Toronto, ON.
Young NL; Child Health Evaluative Sciences, The Hospital for Sick Children Research Institute, Toronto, ON.; Department of Pediatrics, University of Toronto, Toronto, ON, Canada.; School of Rural and Northern Health, Laurentian University, Sudbury, ON, Canada.
Dover S; Child Health Evaluative Sciences, The Hospital for Sick Children Research Institute, Toronto, ON.
Bouskill V; Department of Nursing, The Hospital for Sick Children, Toronto, ON, Canada.
Hilliard P; Child Health Evaluative Sciences, The Hospital for Sick Children Research Institute, Toronto, ON.
Price VE; Division of Pediatric Hematology/Oncology, Department of Pediatrics, IWK Health Centre, Dalhousie University, Halifax, NS, Canada.
Blanchette VS; Child Health Evaluative Sciences, The Hospital for Sick Children Research Institute, Toronto, ON.; Division of Hematology/Oncology, The Hospital for Sick Children, Toronto, ON, Canada.; Department of Pediatrics, University of Toronto, Toronto, ON, Canada.
Pokaż więcej
Źródło :
Haemophilia : the official journal of the World Federation of Hemophilia [Haemophilia] 2020 Jan; Vol. 26 (1), pp. 73-78. Date of Electronic Publication: 2019 Dec 22.
Typ publikacji :
Journal Article
MeSH Terms :
Half-Life*
Factor VIII/*therapeutic use
Hemophilia A/*drug therapy
Quality of Life/*psychology
Adolescent ; Child ; Child, Preschool ; Factor VIII/pharmacology ; Humans ; Male ; Retrospective Studies
Czasopismo naukowe
Tytuł :
Potential Therapeutic Roles for Direct Factor Xa Inhibitors in Coronavirus Infections.
Autorzy :
Al-Horani RA; Division of Basic Pharmaceutical Sciences, College of Pharmacy, Xavier University of Louisiana, 1 Drexel Drive, New Orleans, LA, 70125-1089, USA. .
Pokaż więcej
Źródło :
American journal of cardiovascular drugs : drugs, devices, and other interventions [Am J Cardiovasc Drugs] 2020 Dec; Vol. 20 (6), pp. 525-533.
Typ publikacji :
Journal Article; Review
MeSH Terms :
COVID-19/*drug therapy
COVID-19/*physiopathology
Factor Xa Inhibitors/*pharmacology
Factor Xa Inhibitors/*therapeutic use
Blood Coagulation/drug effects ; Cytokine Release Syndrome/drug therapy ; Cytokine Release Syndrome/physiopathology ; Cytokines/biosynthesis ; Drug Interactions ; Factor Xa/metabolism ; Factor Xa Inhibitors/adverse effects ; Factor Xa Inhibitors/pharmacokinetics ; Half-Life ; Humans ; Inflammation Mediators/metabolism ; Metabolic Clearance Rate ; Multiple Organ Failure/physiopathology ; Multiple Organ Failure/prevention & control ; Pandemics ; Protein Binding/physiology ; SARS-CoV-2 ; Severity of Illness Index
Czasopismo naukowe
Tytuł :
Targeting Enteropeptidase with Reversible Covalent Inhibitors To Achieve Metabolic Benefits.
Autorzy :
Sun W; DPDS Discovery Technology and Molecular Pharmacology, Spring House, Pennsylvania (W.S., M.W., R.A.); DPDS Analytical Sciences, La Jolla, California (J.W.); Discovery Chemistry, Spring House, Pennsylvania (X.Z., M.D.C., B.Z., Y.Z., J.La.); CVM Discovery, Spring House, Pennsylvania (K.A., J.Leo., J.Len.); and Janssen Research & Development, LLC, Spring House, Pennsylvania .
Zhang X; DPDS Discovery Technology and Molecular Pharmacology, Spring House, Pennsylvania (W.S., M.W., R.A.); DPDS Analytical Sciences, La Jolla, California (J.W.); Discovery Chemistry, Spring House, Pennsylvania (X.Z., M.D.C., B.Z., Y.Z., J.La.); CVM Discovery, Spring House, Pennsylvania (K.A., J.Leo., J.Len.); and Janssen Research & Development, LLC, Spring House, Pennsylvania.
Cummings MD; DPDS Discovery Technology and Molecular Pharmacology, Spring House, Pennsylvania (W.S., M.W., R.A.); DPDS Analytical Sciences, La Jolla, California (J.W.); Discovery Chemistry, Spring House, Pennsylvania (X.Z., M.D.C., B.Z., Y.Z., J.La.); CVM Discovery, Spring House, Pennsylvania (K.A., J.Leo., J.Len.); and Janssen Research & Development, LLC, Spring House, Pennsylvania.
Albarazanji K; DPDS Discovery Technology and Molecular Pharmacology, Spring House, Pennsylvania (W.S., M.W., R.A.); DPDS Analytical Sciences, La Jolla, California (J.W.); Discovery Chemistry, Spring House, Pennsylvania (X.Z., M.D.C., B.Z., Y.Z., J.La.); CVM Discovery, Spring House, Pennsylvania (K.A., J.Leo., J.Len.); and Janssen Research & Development, LLC, Spring House, Pennsylvania.
Wu J; DPDS Discovery Technology and Molecular Pharmacology, Spring House, Pennsylvania (W.S., M.W., R.A.); DPDS Analytical Sciences, La Jolla, California (J.W.); Discovery Chemistry, Spring House, Pennsylvania (X.Z., M.D.C., B.Z., Y.Z., J.La.); CVM Discovery, Spring House, Pennsylvania (K.A., J.Leo., J.Len.); and Janssen Research & Development, LLC, Spring House, Pennsylvania.
Wang M; DPDS Discovery Technology and Molecular Pharmacology, Spring House, Pennsylvania (W.S., M.W., R.A.); DPDS Analytical Sciences, La Jolla, California (J.W.); Discovery Chemistry, Spring House, Pennsylvania (X.Z., M.D.C., B.Z., Y.Z., J.La.); CVM Discovery, Spring House, Pennsylvania (K.A., J.Leo., J.Len.); and Janssen Research & Development, LLC, Spring House, Pennsylvania.
Alexander R; DPDS Discovery Technology and Molecular Pharmacology, Spring House, Pennsylvania (W.S., M.W., R.A.); DPDS Analytical Sciences, La Jolla, California (J.W.); Discovery Chemistry, Spring House, Pennsylvania (X.Z., M.D.C., B.Z., Y.Z., J.La.); CVM Discovery, Spring House, Pennsylvania (K.A., J.Leo., J.Len.); and Janssen Research & Development, LLC, Spring House, Pennsylvania.
Zhu B; DPDS Discovery Technology and Molecular Pharmacology, Spring House, Pennsylvania (W.S., M.W., R.A.); DPDS Analytical Sciences, La Jolla, California (J.W.); Discovery Chemistry, Spring House, Pennsylvania (X.Z., M.D.C., B.Z., Y.Z., J.La.); CVM Discovery, Spring House, Pennsylvania (K.A., J.Leo., J.Len.); and Janssen Research & Development, LLC, Spring House, Pennsylvania.
Zhang Y; DPDS Discovery Technology and Molecular Pharmacology, Spring House, Pennsylvania (W.S., M.W., R.A.); DPDS Analytical Sciences, La Jolla, California (J.W.); Discovery Chemistry, Spring House, Pennsylvania (X.Z., M.D.C., B.Z., Y.Z., J.La.); CVM Discovery, Spring House, Pennsylvania (K.A., J.Leo., J.Len.); and Janssen Research & Development, LLC, Spring House, Pennsylvania.
Leonard J; DPDS Discovery Technology and Molecular Pharmacology, Spring House, Pennsylvania (W.S., M.W., R.A.); DPDS Analytical Sciences, La Jolla, California (J.W.); Discovery Chemistry, Spring House, Pennsylvania (X.Z., M.D.C., B.Z., Y.Z., J.La.); CVM Discovery, Spring House, Pennsylvania (K.A., J.Leo., J.Len.); and Janssen Research & Development, LLC, Spring House, Pennsylvania.
Lanter J; DPDS Discovery Technology and Molecular Pharmacology, Spring House, Pennsylvania (W.S., M.W., R.A.); DPDS Analytical Sciences, La Jolla, California (J.W.); Discovery Chemistry, Spring House, Pennsylvania (X.Z., M.D.C., B.Z., Y.Z., J.La.); CVM Discovery, Spring House, Pennsylvania (K.A., J.Leo., J.Len.); and Janssen Research & Development, LLC, Spring House, Pennsylvania.
Lenhard J; DPDS Discovery Technology and Molecular Pharmacology, Spring House, Pennsylvania (W.S., M.W., R.A.); DPDS Analytical Sciences, La Jolla, California (J.W.); Discovery Chemistry, Spring House, Pennsylvania (X.Z., M.D.C., B.Z., Y.Z., J.La.); CVM Discovery, Spring House, Pennsylvania (K.A., J.Leo., J.Len.); and Janssen Research & Development, LLC, Spring House, Pennsylvania.
Pokaż więcej
Źródło :
The Journal of pharmacology and experimental therapeutics [J Pharmacol Exp Ther] 2020 Dec; Vol. 375 (3), pp. 510-521. Date of Electronic Publication: 2020 Oct 08.
Typ publikacji :
Journal Article
MeSH Terms :
Enteropeptidase/*antagonists & inhibitors
Enzyme Inhibitors/*pharmacology
Metabolism/*drug effects
Animals ; Blood Glucose/metabolism ; Body Weight/drug effects ; CHO Cells ; Cricetulus ; Diabetes Mellitus/metabolism ; Eating/drug effects ; Enteropeptidase/chemistry ; Enzyme Inhibitors/chemistry ; Half-Life ; Humans ; Kinetics ; Models, Molecular ; Obesity/metabolism ; Protein Conformation ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł :
Effects of Fuzheng Huayu recipe on entecavir pharmacokinetics in normal and dimethylnitrosamine-induced hepatic fibrosis rats.
Autorzy :
Yang T; Institute of Liver Diseases, Shuguang Hospital Affiliated to Shanghai University of Traditional Chinese Medicine, Shanghai, China.; Department of Cardiology, Institute of Cardiovascular Disease of Integrated Traditional Chinese Medicine and Western Medicine, Shuguang Hospital affiliated to Shanghai University of Traditional Chinese Medicine, Shanghai, China.; Shanghai Key Laboratory of Traditional Chinese Clinical Medicine, Shanghai, China.
Zheng TH; Institute of Liver Diseases, Shuguang Hospital Affiliated to Shanghai University of Traditional Chinese Medicine, Shanghai, China.
Zhao Q; Institute of Liver Diseases, Shuguang Hospital Affiliated to Shanghai University of Traditional Chinese Medicine, Shanghai, China.
Liu W; Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai, China.; The MOE Key Laboratory for Standardization of Chinese Medicines and The SATCM Key Laboratory for New Resources and Quality Evaluation of Chinese Medicines, Shanghai, China.
Li SP; Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai, China.; The MOE Key Laboratory for Standardization of Chinese Medicines and The SATCM Key Laboratory for New Resources and Quality Evaluation of Chinese Medicines, Shanghai, China.
Tao YY; Institute of Liver Diseases, Shuguang Hospital Affiliated to Shanghai University of Traditional Chinese Medicine, Shanghai, China.; Department of Cardiology, Institute of Cardiovascular Disease of Integrated Traditional Chinese Medicine and Western Medicine, Shuguang Hospital affiliated to Shanghai University of Traditional Chinese Medicine, Shanghai, China.
Wang CH; Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai, China.; The MOE Key Laboratory for Standardization of Chinese Medicines and The SATCM Key Laboratory for New Resources and Quality Evaluation of Chinese Medicines, Shanghai, China.
Liu CH; Institute of Liver Diseases, Shuguang Hospital Affiliated to Shanghai University of Traditional Chinese Medicine, Shanghai, China.; Shanghai Key Laboratory of Traditional Chinese Clinical Medicine, Shanghai, China.
Pokaż więcej
Źródło :
Pharmaceutical biology [Pharm Biol] 2020 Dec; Vol. 58 (1), pp. 1-7.
Typ publikacji :
Journal Article; Validation Study
MeSH Terms :
Antiviral Agents/*pharmacokinetics
Drugs, Chinese Herbal/*administration & dosage
Guanine/*analogs & derivatives
Liver Cirrhosis/*physiopathology
Animals ; Antiviral Agents/administration & dosage ; Area Under Curve ; Chromatography, High Pressure Liquid/methods ; Dimethylnitrosamine ; Drug Administration Schedule ; Drugs, Chinese Herbal/pharmacology ; Guanine/administration & dosage ; Guanine/pharmacology ; Half-Life ; Herb-Drug Interactions ; Male ; Rats ; Rats, Wistar ; Tandem Mass Spectrometry/methods
Czasopismo naukowe
Tytuł :
Physiologically-Based Pharmacokinetic Modeling to Predict the Clinical Efficacy of the Coadministration of Lopinavir and Ritonavir against SARS-CoV-2.
Autorzy :
Thakur A; Innovations in Food and Chemical Safety, Agency for Science, Technology, and Research, Singapore City, Singapore.; Skin Research Institute of Singapore, Agency for Science, Technology, and Research, Singapore City, Singapore.
Tan SPF; Innovations in Food and Chemical Safety, Agency for Science, Technology, and Research, Singapore City, Singapore.; Skin Research Institute of Singapore, Agency for Science, Technology, and Research, Singapore City, Singapore.
Chan JCY; Innovations in Food and Chemical Safety, Agency for Science, Technology, and Research, Singapore City, Singapore.; Skin Research Institute of Singapore, Agency for Science, Technology, and Research, Singapore City, Singapore.; Singapore Institute of Food and Biotechnology Innovation, Agency for Science, Technology, and Research, Singapore City, Singapore.
Pokaż więcej
Źródło :
Clinical pharmacology and therapeutics [Clin Pharmacol Ther] 2020 Dec; Vol. 108 (6), pp. 1176-1184. Date of Electronic Publication: 2020 Oct 06.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Antiviral Agents/*pharmacokinetics
COVID-19/*drug therapy
Lopinavir/*pharmacokinetics
Ritonavir/*pharmacokinetics
Area Under Curve ; Asian Continental Ancestry Group ; Dose-Response Relationship, Drug ; European Continental Ancestry Group ; HIV Infections/drug therapy ; Half-Life ; Humans ; Lopinavir/pharmacology ; Lung/metabolism ; Metabolic Clearance Rate ; Models, Biological ; Ritonavir/pharmacology ; SARS-CoV-2
SCR Protocol :
COVID-19 drug treatment
Czasopismo naukowe
Tytuł :
Structure of the Complex of an Iminopyridinedione Protein Tyrosine Phosphatase 4A3 Phosphatase Inhibitor with Human Serum Albumin.
Autorzy :
Czub MP; Departments of Molecular Physiology and Biological Physics (M.P.C., A.M.B., J.H.B., W.M.) and Pharmacology (K.E.M., E.R.S., J.S.L.) and Center for Structural Genomics of Infectious Diseases (CSGID) (M.P.C., W.M.), University of Virginia, Charlottesville, Virginia; Department of Chemistry, University of Pittsburgh, Pittsburgh, Pennsylvania (E.J.R., N.R.T., T.S.M., P.W.); and KeViRx, Inc., Charlottesville, Virginia (I.K.B., E.R.S., J.S.L.).
Boulton AM; Departments of Molecular Physiology and Biological Physics (M.P.C., A.M.B., J.H.B., W.M.) and Pharmacology (K.E.M., E.R.S., J.S.L.) and Center for Structural Genomics of Infectious Diseases (CSGID) (M.P.C., W.M.), University of Virginia, Charlottesville, Virginia; Department of Chemistry, University of Pittsburgh, Pittsburgh, Pennsylvania (E.J.R., N.R.T., T.S.M., P.W.); and KeViRx, Inc., Charlottesville, Virginia (I.K.B., E.R.S., J.S.L.).
Rastelli EJ; Departments of Molecular Physiology and Biological Physics (M.P.C., A.M.B., J.H.B., W.M.) and Pharmacology (K.E.M., E.R.S., J.S.L.) and Center for Structural Genomics of Infectious Diseases (CSGID) (M.P.C., W.M.), University of Virginia, Charlottesville, Virginia; Department of Chemistry, University of Pittsburgh, Pittsburgh, Pennsylvania (E.J.R., N.R.T., T.S.M., P.W.); and KeViRx, Inc., Charlottesville, Virginia (I.K.B., E.R.S., J.S.L.).
Tasker NR; Departments of Molecular Physiology and Biological Physics (M.P.C., A.M.B., J.H.B., W.M.) and Pharmacology (K.E.M., E.R.S., J.S.L.) and Center for Structural Genomics of Infectious Diseases (CSGID) (M.P.C., W.M.), University of Virginia, Charlottesville, Virginia; Department of Chemistry, University of Pittsburgh, Pittsburgh, Pennsylvania (E.J.R., N.R.T., T.S.M., P.W.); and KeViRx, Inc., Charlottesville, Virginia (I.K.B., E.R.S., J.S.L.).
Maskrey TS; Departments of Molecular Physiology and Biological Physics (M.P.C., A.M.B., J.H.B., W.M.) and Pharmacology (K.E.M., E.R.S., J.S.L.) and Center for Structural Genomics of Infectious Diseases (CSGID) (M.P.C., W.M.), University of Virginia, Charlottesville, Virginia; Department of Chemistry, University of Pittsburgh, Pittsburgh, Pennsylvania (E.J.R., N.R.T., T.S.M., P.W.); and KeViRx, Inc., Charlottesville, Virginia (I.K.B., E.R.S., J.S.L.).
Blanco IK; Departments of Molecular Physiology and Biological Physics (M.P.C., A.M.B., J.H.B., W.M.) and Pharmacology (K.E.M., E.R.S., J.S.L.) and Center for Structural Genomics of Infectious Diseases (CSGID) (M.P.C., W.M.), University of Virginia, Charlottesville, Virginia; Department of Chemistry, University of Pittsburgh, Pittsburgh, Pennsylvania (E.J.R., N.R.T., T.S.M., P.W.); and KeViRx, Inc., Charlottesville, Virginia (I.K.B., E.R.S., J.S.L.).
McQueeney KE; Departments of Molecular Physiology and Biological Physics (M.P.C., A.M.B., J.H.B., W.M.) and Pharmacology (K.E.M., E.R.S., J.S.L.) and Center for Structural Genomics of Infectious Diseases (CSGID) (M.P.C., W.M.), University of Virginia, Charlottesville, Virginia; Department of Chemistry, University of Pittsburgh, Pittsburgh, Pennsylvania (E.J.R., N.R.T., T.S.M., P.W.); and KeViRx, Inc., Charlottesville, Virginia (I.K.B., E.R.S., J.S.L.).
Bushweller JH; Departments of Molecular Physiology and Biological Physics (M.P.C., A.M.B., J.H.B., W.M.) and Pharmacology (K.E.M., E.R.S., J.S.L.) and Center for Structural Genomics of Infectious Diseases (CSGID) (M.P.C., W.M.), University of Virginia, Charlottesville, Virginia; Department of Chemistry, University of Pittsburgh, Pittsburgh, Pennsylvania (E.J.R., N.R.T., T.S.M., P.W.); and KeViRx, Inc., Charlottesville, Virginia (I.K.B., E.R.S., J.S.L.).
Minor W; Departments of Molecular Physiology and Biological Physics (M.P.C., A.M.B., J.H.B., W.M.) and Pharmacology (K.E.M., E.R.S., J.S.L.) and Center for Structural Genomics of Infectious Diseases (CSGID) (M.P.C., W.M.), University of Virginia, Charlottesville, Virginia; Department of Chemistry, University of Pittsburgh, Pittsburgh, Pennsylvania (E.J.R., N.R.T., T.S.M., P.W.); and KeViRx, Inc., Charlottesville, Virginia (I.K.B., E.R.S., J.S.L.).
Wipf P; Departments of Molecular Physiology and Biological Physics (M.P.C., A.M.B., J.H.B., W.M.) and Pharmacology (K.E.M., E.R.S., J.S.L.) and Center for Structural Genomics of Infectious Diseases (CSGID) (M.P.C., W.M.), University of Virginia, Charlottesville, Virginia; Department of Chemistry, University of Pittsburgh, Pittsburgh, Pennsylvania (E.J.R., N.R.T., T.S.M., P.W.); and KeViRx, Inc., Charlottesville, Virginia (I.K.B., E.R.S., J.S.L.).
Sharlow ER; Departments of Molecular Physiology and Biological Physics (M.P.C., A.M.B., J.H.B., W.M.) and Pharmacology (K.E.M., E.R.S., J.S.L.) and Center for Structural Genomics of Infectious Diseases (CSGID) (M.P.C., W.M.), University of Virginia, Charlottesville, Virginia; Department of Chemistry, University of Pittsburgh, Pittsburgh, Pennsylvania (E.J.R., N.R.T., T.S.M., P.W.); and KeViRx, Inc., Charlottesville, Virginia (I.K.B., E.R.S., J.S.L.).
Lazo JS; Departments of Molecular Physiology and Biological Physics (M.P.C., A.M.B., J.H.B., W.M.) and Pharmacology (K.E.M., E.R.S., J.S.L.) and Center for Structural Genomics of Infectious Diseases (CSGID) (M.P.C., W.M.), University of Virginia, Charlottesville, Virginia; Department of Chemistry, University of Pittsburgh, Pittsburgh, Pennsylvania (E.J.R., N.R.T., T.S.M., P.W.); and KeViRx, Inc., Charlottesville, Virginia (I.K.B., E.R.S., J.S.L.) .
Pokaż więcej
Źródło :
Molecular pharmacology [Mol Pharmacol] 2020 Dec; Vol. 98 (6), pp. 648-657. Date of Electronic Publication: 2020 Sep 25.
Typ publikacji :
Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, Non-P.H.S.
MeSH Terms :
Imines/*pharmacology
Neoplasm Proteins/*antagonists & inhibitors
Protein Tyrosine Phosphatases/*antagonists & inhibitors
Pyridines/*pharmacology
Serum Albumin, Human/*metabolism
Binding Sites ; Calorimetry ; Cell Line, Tumor ; Cell Survival/drug effects ; Crystallography, X-Ray ; Enzyme Assays ; Half-Life ; Humans ; Imines/chemistry ; Imines/therapeutic use ; Neoplasm Proteins/metabolism ; Neoplasms/drug therapy ; Neoplasms/pathology ; Protein Tyrosine Phosphatases/metabolism ; Pyridines/chemistry ; Pyridines/therapeutic use ; Serum Albumin, Human/ultrastructure
Czasopismo naukowe
Tytuł :
Effect of Genetic Polymorphisms on the Pharmacokinetics of Deferasirox in Healthy Chinese Subjects and an Artificial Neural Networks Model for Pharmacokinetic Prediction.
Autorzy :
Chen J; Center of Clinical Pharmacology, School of Medicine, The Second Affiliated Hospital of Zhejiang University, 88 Jiefang Road, Hangzhou, 310009, Zhejiang, China.
Xu Y; Center of Clinical Pharmacology, School of Medicine, The Second Affiliated Hospital of Zhejiang University, 88 Jiefang Road, Hangzhou, 310009, Zhejiang, China.
Lou H; Center of Clinical Pharmacology, School of Medicine, The Second Affiliated Hospital of Zhejiang University, 88 Jiefang Road, Hangzhou, 310009, Zhejiang, China.
Jiang B; Center of Clinical Pharmacology, School of Medicine, The Second Affiliated Hospital of Zhejiang University, 88 Jiefang Road, Hangzhou, 310009, Zhejiang, China.
Shao R; Center of Clinical Pharmacology, School of Medicine, The Second Affiliated Hospital of Zhejiang University, 88 Jiefang Road, Hangzhou, 310009, Zhejiang, China.
Yang D; Center of Clinical Pharmacology, School of Medicine, The Second Affiliated Hospital of Zhejiang University, 88 Jiefang Road, Hangzhou, 310009, Zhejiang, China.
Hu Y; Center of Clinical Pharmacology, School of Medicine, The Second Affiliated Hospital of Zhejiang University, 88 Jiefang Road, Hangzhou, 310009, Zhejiang, China.
Ruan Z; Center of Clinical Pharmacology, School of Medicine, The Second Affiliated Hospital of Zhejiang University, 88 Jiefang Road, Hangzhou, 310009, Zhejiang, China. .
Pokaż więcej
Źródło :
European journal of drug metabolism and pharmacokinetics [Eur J Drug Metab Pharmacokinet] 2020 Dec; Vol. 45 (6), pp. 761-770.
Typ publikacji :
Journal Article; Randomized Controlled Trial
MeSH Terms :
Neural Networks, Computer*
Deferasirox/*pharmacokinetics
Iron Chelating Agents/*pharmacokinetics
Adolescent ; Adult ; Area Under Curve ; Asian Continental Ancestry Group ; Cross-Over Studies ; Cytochrome P-450 CYP1A1/genetics ; Drug Compounding ; Female ; Glucuronosyltransferase/genetics ; Half-Life ; Healthy Volunteers ; Humans ; Male ; Middle Aged ; Multidrug Resistance-Associated Proteins/genetics ; Polymorphism, Genetic/genetics ; Polymorphism, Single Nucleotide ; Predictive Value of Tests ; Young Adult
Czasopismo naukowe
Tytuł :
Novel, Potent, and Druglike Tetrahydroquinazoline Inhibitor That Is Highly Selective for Human Topoisomerase II α over β.
Autorzy :
Ortega JA; Laboratory of Molecular Modeling and Drug Discovery, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genoa, Italy.
Arencibia JM; Laboratory of Molecular Modeling and Drug Discovery, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genoa, Italy.
Minniti E; Laboratory of Molecular Modeling and Drug Discovery, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genoa, Italy.; Department of Pharmacy and Biotechnology, Alma Mater Studiorum-University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy.
Byl JAW; Department of Biochemistry, Vanderbilt University School of Medicine, Nashville, Tennessee 37232-0146, United States.
Franco-Ulloa S; Laboratory of Molecular Modeling and Drug Discovery, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genoa, Italy.
Borgogno M; Laboratory of Molecular Modeling and Drug Discovery, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genoa, Italy.
Genna V; Laboratory of Molecular Modeling and Drug Discovery, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genoa, Italy.
Summa M; Analytical Chemistry & Translational Pharmacology, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genoa, Italy.
Bertozzi SM; Analytical Chemistry & Translational Pharmacology, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genoa, Italy.
Bertorelli R; Analytical Chemistry & Translational Pharmacology, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genoa, Italy.
Armirotti A; Analytical Chemistry & Translational Pharmacology, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genoa, Italy.
Minarini A; Department of Pharmacy and Biotechnology, Alma Mater Studiorum-University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy.
Sissi C; Department of Pharmaceutical and Pharmacological Sciences, University of Padova, Via Marzolo 5, 35131 Padova, Italy.
Osheroff N; Department of Biochemistry, Vanderbilt University School of Medicine, Nashville, Tennessee 37232-0146, United States.; Department of Medicine (Hematology/Oncology), Vanderbilt University School of Medicine, Nashville, Tennessee 37232-6307, United States.; VA Tennessee Valley Healthcare System, Nashville, Tennessee 37212, United States.
De Vivo M; Laboratory of Molecular Modeling and Drug Discovery, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genoa, Italy.
Pokaż więcej
Źródło :
Journal of medicinal chemistry [J Med Chem] 2020 Nov 12; Vol. 63 (21), pp. 12873-12886. Date of Electronic Publication: 2020 Oct 20.
Typ publikacji :
Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't
MeSH Terms :
DNA Topoisomerases, Type II/*chemistry
Quinidine/*analogs & derivatives
Topoisomerase II Inhibitors/*chemistry
Animals ; Cell Line, Tumor ; Cell Survival/drug effects ; DNA/chemistry ; DNA/metabolism ; DNA Cleavage ; DNA Topoisomerases, Type II/metabolism ; Drug Screening Assays, Antitumor ; Half-Life ; Humans ; Isoenzymes/antagonists & inhibitors ; Isoenzymes/metabolism ; Mice ; Quinidine/chemistry ; Quinidine/metabolism ; Quinidine/pharmacology ; Topoisomerase II Inhibitors/metabolism ; Topoisomerase II Inhibitors/pharmacology
Czasopismo naukowe
Tytuł :
A Peptidyl Inhibitor that Blocks Calcineurin-NFAT Interaction and Prevents Acute Lung Injury.
Autorzy :
Dougherty PG; Department of Chemistry and Biochemistry, The Ohio State University, 484 West 12th Ave., Columbus, Ohio 43210, United States.; Entrada Therapeutics, 50 Northern Avenue, Boston, Massachusetts 02210, United States.
Karpurapu M; Department of Medicine, Division of Pulmonary, Critical Care and Sleep Medicine, Ohio State University Wexner Medical Center, Davis Heart and Lung Research Institute, Columbus, Ohio 43210, United States.
Koley A; Department of Chemistry and Biochemistry, The Ohio State University, 484 West 12th Ave., Columbus, Ohio 43210, United States.
Lukowski JK; Department of Chemistry and Biochemistry, University of Notre Dame, Notre Dame, Indiana 46556, United States.
Qian Z; Department of Chemistry and Biochemistry, The Ohio State University, 484 West 12th Ave., Columbus, Ohio 43210, United States.; Entrada Therapeutics, 50 Northern Avenue, Boston, Massachusetts 02210, United States.
Srinivas Nirujogi T; Department of Medicine, Division of Pulmonary, Critical Care and Sleep Medicine, Ohio State University Wexner Medical Center, Davis Heart and Lung Research Institute, Columbus, Ohio 43210, United States.; East Liverpool City Hospital, 425 W 5th Street, East Liverpool, Ohio 43920, United States.
Rusu L; Department of Medicine, Division of Pulmonary, Critical Care and Sleep Medicine, Ohio State University Wexner Medical Center, Davis Heart and Lung Research Institute, Columbus, Ohio 43210, United States.
Chung S; Department of Medicine, Division of Pulmonary, Critical Care and Sleep Medicine, Ohio State University Wexner Medical Center, Davis Heart and Lung Research Institute, Columbus, Ohio 43210, United States.
Hummon AB; Department of Chemistry and Biochemistry, The Ohio State University, 484 West 12th Ave., Columbus, Ohio 43210, United States.; Comprehensive Cancer Center, The Ohio State University, Columbus Ohio, 43210, United States.
Li HW; Columbia Center for Translational Immunology, Columbia University, 650 W. 168th Street, New York, New York 10032, United States.
Christman JW; Department of Medicine, Division of Pulmonary, Critical Care and Sleep Medicine, Ohio State University Wexner Medical Center, Davis Heart and Lung Research Institute, Columbus, Ohio 43210, United States.
Pei D; Department of Chemistry and Biochemistry, The Ohio State University, 484 West 12th Ave., Columbus, Ohio 43210, United States.
Pokaż więcej
Źródło :
Journal of medicinal chemistry [J Med Chem] 2020 Nov 12; Vol. 63 (21), pp. 12853-12872. Date of Electronic Publication: 2020 Oct 19.
Typ publikacji :
Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't
MeSH Terms :
Calcineurin/*metabolism
NFATC Transcription Factors/*metabolism
Acute Lung Injury/pathology ; Acute Lung Injury/prevention & control ; Amino Acid Sequence ; Animals ; Binding Sites ; Calcineurin/chemistry ; Calcineurin Inhibitors/chemistry ; Calcineurin Inhibitors/metabolism ; Calcineurin Inhibitors/pharmacology ; Calcineurin Inhibitors/therapeutic use ; Half-Life ; Humans ; Lipopolysaccharides/toxicity ; Lung/diagnostic imaging ; Lung/metabolism ; Mice ; Mice, Inbred BALB C ; Mice, Inbred C57BL ; Molecular Dynamics Simulation ; NFATC Transcription Factors/chemistry ; Peptides/chemistry ; Peptides/pharmacokinetics ; Peptides/pharmacology ; Peptides/therapeutic use ; Protein Interaction Domains and Motifs/drug effects ; Signal Transduction/drug effects ; Tissue Distribution
Czasopismo naukowe
Tytuł :
Therapeutic Targeting of MMP-12 for the Treatment of Chronic Obstructive Pulmonary Disease.
Autorzy :
Baggio C; Division of Biomedical Sciences, School of Medicine, University of California Riverside, 900 University Avenue, Riverside, California 92521, United States.
Velazquez JV; Division of Biomedical Sciences, School of Medicine, University of California Riverside, 900 University Avenue, Riverside, California 92521, United States.
Fragai M; Magnetic Resonance Center (CERM), University of Florence and Consorzio Interuniversitario Risonanze Magnetiche di Metallo Proteine (CIRMMP), Via L. Sacconi 6, 50019 Sesto Fiorentino, Italy.
Nordgren TM; Division of Biomedical Sciences, School of Medicine, University of California Riverside, 900 University Avenue, Riverside, California 92521, United States.
Pellecchia M; Division of Biomedical Sciences, School of Medicine, University of California Riverside, 900 University Avenue, Riverside, California 92521, United States.
Pokaż więcej
Źródło :
Journal of medicinal chemistry [J Med Chem] 2020 Nov 12; Vol. 63 (21), pp. 12911-12920. Date of Electronic Publication: 2020 Oct 27.
Typ publikacji :
Journal Article; Research Support, N.I.H., Extramural
MeSH Terms :
Matrix Metalloproteinase 12/*metabolism
Matrix Metalloproteinase Inhibitors/*chemistry
Animals ; Binding Sites ; Crystallography, X-Ray ; Disease Models, Animal ; Emphysema/drug therapy ; Emphysema/etiology ; Half-Life ; Humans ; Isoenzymes/antagonists & inhibitors ; Isoenzymes/metabolism ; Matrix Metalloproteinase 12/chemistry ; Matrix Metalloproteinase Inhibitors/pharmacokinetics ; Matrix Metalloproteinase Inhibitors/therapeutic use ; Mice ; Mice, Inbred BALB C ; Mice, Inbred C57BL ; Molecular Dynamics Simulation ; Nuclear Magnetic Resonance, Biomolecular ; Pancreatic Elastase/metabolism ; Peptides/genetics ; Peptides/metabolism ; Peptides/therapeutic use ; Pulmonary Disease, Chronic Obstructive/drug therapy ; Pulmonary Disease, Chronic Obstructive/pathology ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł :
Discovery of an Orally Available Diazabicyclooctane Inhibitor (ETX0282) of Class A, C, and D Serine β-Lactamases.
Autorzy :
Durand-Réville TF; Entasis Therapeutics, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States.
Comita-Prevoir J; Entasis Therapeutics, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States.
Zhang J; Entasis Therapeutics, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States.
Wu X; Entasis Therapeutics, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States.
May-Dracka TL; Infection Discovery, AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States.
Romero JAC; Entasis Therapeutics, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States.
Wu F; Entasis Therapeutics, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States.
Chen A; Entasis Therapeutics, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States.
Shapiro AB; Entasis Therapeutics, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States.
Carter NM; Entasis Therapeutics, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States.
McLeod SM; Entasis Therapeutics, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States.
Giacobbe RA; Infection Discovery, AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States.
Verheijen JC; Infection Discovery, AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States.
Lahiri SD; Infection Discovery, AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States.
Sacco MD; Department of Molecular Medicine, Morsani College of Medicine, University of South Florida, 12901 Bruce B. Downs Boulevard, Tampa, Florida 33612, United States.
Chen Y; Department of Molecular Medicine, Morsani College of Medicine, University of South Florida, 12901 Bruce B. Downs Boulevard, Tampa, Florida 33612, United States.
O'Donnell JP; Entasis Therapeutics, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States.
Miller AA; Entasis Therapeutics, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States.
Mueller JP; Entasis Therapeutics, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States.
Tommasi RA; Entasis Therapeutics, 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States.
Pokaż więcej
Źródło :
Journal of medicinal chemistry [J Med Chem] 2020 Nov 12; Vol. 63 (21), pp. 12511-12525. Date of Electronic Publication: 2020 Jul 24.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Anti-Bacterial Agents/*chemistry
Azabicyclo Compounds/*chemistry
beta-Lactamase Inhibitors/*chemistry
beta-Lactamases/*chemistry
Administration, Oral ; Animals ; Anti-Bacterial Agents/pharmacokinetics ; Anti-Bacterial Agents/pharmacology ; Anti-Bacterial Agents/therapeutic use ; Azabicyclo Compounds/metabolism ; Azabicyclo Compounds/pharmacology ; Azabicyclo Compounds/therapeutic use ; Drug Design ; Drug Evaluation, Preclinical ; Gram-Negative Bacteria/drug effects ; Gram-Positive Bacteria/drug effects ; Half-Life ; Humans ; Mice ; Microbial Sensitivity Tests ; Penicillin-Binding Proteins/chemistry ; Penicillin-Binding Proteins/metabolism ; Prodrugs/chemistry ; Prodrugs/metabolism ; Protein Binding ; Rats ; Skin Diseases/drug therapy ; Skin Diseases/pathology ; Skin Diseases/veterinary ; Structure-Activity Relationship ; beta-Lactamase Inhibitors/metabolism ; beta-Lactamase Inhibitors/pharmacology ; beta-Lactamase Inhibitors/therapeutic use ; beta-Lactamases/metabolism
Czasopismo naukowe
Tytuł :
Discovery of IPN60090, a Clinical Stage Selective Glutaminase-1 (GLS-1) Inhibitor with Excellent Pharmacokinetic and Physicochemical Properties.
Autorzy :
Soth MJ; Institute for Applied Cancer Science (IACS), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Le K; Institute for Applied Cancer Science (IACS), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Di Francesco ME; Institute for Applied Cancer Science (IACS), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Hamilton MM; Institute for Applied Cancer Science (IACS), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Liu G; Institute for Applied Cancer Science (IACS), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Burke JP; Institute for Applied Cancer Science (IACS), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Carroll CL; Institute for Applied Cancer Science (IACS), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Kovacs JJ; Translational Research to Advance Therapeutics and Innovation in Oncology (TRACTION), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Bardenhagen JP; Institute for Applied Cancer Science (IACS), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Bristow CA; Translational Research to Advance Therapeutics and Innovation in Oncology (TRACTION), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Cardozo M; Institute for Applied Cancer Science (IACS), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Czako B; Institute for Applied Cancer Science (IACS), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
de Stanchina E; Antitumor Assessment Core Facility-Molecular Pharmacology Program, Memorial Sloan Kettering Cancer Center, New York, New York 10065, United States.
Feng N; Translational Research to Advance Therapeutics and Innovation in Oncology (TRACTION), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Garvey JR; Translational Research to Advance Therapeutics and Innovation in Oncology (TRACTION), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Gay JP; Translational Research to Advance Therapeutics and Innovation in Oncology (TRACTION), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Do MKG; Institute for Applied Cancer Science (IACS), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Greer J; Translational Research to Advance Therapeutics and Innovation in Oncology (TRACTION), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Han M; Institute for Applied Cancer Science (IACS), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Harris A; Translational Research to Advance Therapeutics and Innovation in Oncology (TRACTION), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Herrera Z; Institute for Applied Cancer Science (IACS), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Huang S; Institute for Applied Cancer Science (IACS), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Giuliani V; Translational Research to Advance Therapeutics and Innovation in Oncology (TRACTION), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Jiang Y; Institute for Applied Cancer Science (IACS), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Johnson SB; Translational Research to Advance Therapeutics and Innovation in Oncology (TRACTION), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Johnson TA; Institute for Applied Cancer Science (IACS), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Kang Z; Institute for Applied Cancer Science (IACS), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Leonard PG; Institute for Applied Cancer Science (IACS), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Liu Z; Institute for Applied Cancer Science (IACS), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
McAfoos T; Institute for Applied Cancer Science (IACS), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Miller M; Translational Research to Advance Therapeutics and Innovation in Oncology (TRACTION), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Morlacchi P; Institute for Applied Cancer Science (IACS), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Mullinax RA; Translational Research to Advance Therapeutics and Innovation in Oncology (TRACTION), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Palmer WS; Institute for Applied Cancer Science (IACS), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Pang J; Institute for Applied Cancer Science (IACS), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Rogers N; Institute for Applied Cancer Science (IACS), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Rudin CM; Drunkenmiller Center for Lung Cancer Research, Memorial Sloan Kettering Cancer Center, New York New York 10065, United States.
Shepard HE; Institute for Applied Cancer Science (IACS), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Spencer ND; Translational Research to Advance Therapeutics and Innovation in Oncology (TRACTION), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Theroff J; Institute for Applied Cancer Science (IACS), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Wu Q; Institute for Applied Cancer Science (IACS), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Xu A; Institute for Applied Cancer Science (IACS), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Yau JA; Institute for Applied Cancer Science (IACS), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Draetta G; Institute for Applied Cancer Science (IACS), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.; Translational Research to Advance Therapeutics and Innovation in Oncology (TRACTION), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Toniatti C; Translational Research to Advance Therapeutics and Innovation in Oncology (TRACTION), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Heffernan TP; Translational Research to Advance Therapeutics and Innovation in Oncology (TRACTION), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Jones P; Institute for Applied Cancer Science (IACS), The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
Pokaż więcej
Źródło :
Journal of medicinal chemistry [J Med Chem] 2020 Nov 12; Vol. 63 (21), pp. 12957-12977. Date of Electronic Publication: 2020 Oct 29.
Typ publikacji :
Journal Article
MeSH Terms :
Enzyme Inhibitors/*chemistry
Glutaminase/*antagonists & inhibitors
Triazoles/*pharmacokinetics
Administration, Oral ; Animals ; Cell Line, Tumor ; Dogs ; Drug Evaluation, Preclinical ; Enzyme Inhibitors/metabolism ; Enzyme Inhibitors/pharmacokinetics ; Glutaminase/genetics ; Glutaminase/metabolism ; Half-Life ; Hepatocytes/cytology ; Hepatocytes/drug effects ; Hepatocytes/metabolism ; Humans ; Inhibitory Concentration 50 ; Male ; Mice ; Microsomes/metabolism ; Protein Binding ; Rats ; Rats, Sprague-Dawley ; Recombinant Proteins/biosynthesis ; Recombinant Proteins/chemistry ; Recombinant Proteins/isolation & purification ; Structure-Activity Relationship ; Triazoles/chemistry ; Triazoles/metabolism
Czasopismo naukowe

Ta witryna wykorzystuje pliki cookies do przechowywania informacji na Twoim komputerze. Pliki cookies stosujemy w celu świadczenia usług na najwyższym poziomie, w tym w sposób dostosowany do indywidualnych potrzeb. Korzystanie z witryny bez zmiany ustawień dotyczących cookies oznacza, że będą one zamieszczane w Twoim komputerze. W każdym momencie możesz dokonać zmiany ustawień dotyczących cookies