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Tytuł :
Early antihypertensive treatment and ischemia-induced acute kidney injury.
Autorzy :
Greite R; Nephrology, Hannover Medical School, Hannover, Germany.
Derlin K; Diagnostic and Interventional Radiology, Hannover Medical School, Hannover, Germany.
Hensen B; Diagnostic and Interventional Radiology, Hannover Medical School, Hannover, Germany.
Thorenz A; Nephrology, Hannover Medical School, Hannover, Germany.
Rong S; Nephrology, Hannover Medical School, Hannover, Germany.
Chen R; Nephrology, Hannover Medical School, Hannover, Germany.
Hellms S; Diagnostic and Interventional Radiology, Hannover Medical School, Hannover, Germany.
Jang MS; Nephrology, Hannover Medical School, Hannover, Germany.
Bräsen JH; Pathology, Hannover Medical School, Hannover, Germany.
Meier M; Imaging Center, Institute of Laboratory Animal Sciences, Hannover Medical School, Hannover, Germany.
Willenberg I; Faculty of Mathematics and Natural Sciences, University of Wuppertal, Wuppertal, Germany.
Immenschuh S; Transfusion Medicine, Hannover Medical School, Hannover, Germany.
Haller H; Nephrology, Hannover Medical School, Hannover, Germany.
Luft FC; Experimental and Clinical Research Center, Max-Delbrück Center/Charité, Berlin, Germany.
Panigrahy D; Department of Pathology, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, Massachusetts.
Hwang SH; Department of Entomology and Nematology, UC Davis Comprehensive Cancer Center, University of California, Davis, California.
Hammock BD; Department of Entomology and Nematology, UC Davis Comprehensive Cancer Center, University of California, Davis, California.
Schebb NH; Faculty of Mathematics and Natural Sciences, University of Wuppertal, Wuppertal, Germany.
Gueler F; Nephrology, Hannover Medical School, Hannover, Germany.
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Źródło :
American journal of physiology. Renal physiology [Am J Physiol Renal Physiol] 2020 Oct 01; Vol. 319 (4), pp. F563-F570. Date of Electronic Publication: 2020 Aug 17.
Typ publikacji :
Comparative Study; Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't
MeSH Terms :
Acute Kidney Injury/*drug therapy
Antihypertensive Agents/*pharmacology
Blood Pressure/*drug effects
Enzyme Inhibitors/*pharmacology
Glomerulonephritis/*prevention & control
Hypertension/*drug therapy
Phenylurea Compounds/*pharmacology
Piperidines/*pharmacology
Reperfusion Injury/*drug therapy
Acute Kidney Injury/etiology ; Acute Kidney Injury/pathology ; Acute Kidney Injury/physiopathology ; Angiotensin-Converting Enzyme Inhibitors/pharmacology ; Animals ; Antihypertensive Agents/toxicity ; Disease Models, Animal ; Disease Progression ; Enalapril/pharmacology ; Enzyme Inhibitors/toxicity ; Epoxide Hydrolases/antagonists & inhibitors ; Fibrosis ; Glomerular Mesangium/drug effects ; Glomerular Mesangium/pathology ; Glomerular Mesangium/physiopathology ; Glomerulonephritis/etiology ; Glomerulonephritis/pathology ; Glomerulonephritis/physiopathology ; Hypertension/etiology ; Hypertension/physiopathology ; Male ; Mice ; Phenylurea Compounds/toxicity ; Piperidines/toxicity ; Reperfusion Injury/complications ; Reperfusion Injury/physiopathology
Czasopismo naukowe
Tytuł :
A systematic review and meta-analysis of the use of renin-angiotensin system drugs and COVID-19 clinical outcomes: What is the evidence so far?
Autorzy :
Kurdi A; Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, Glasgow, UK.; Department of Pharmacology and Toxicology, College of Pharmacy, Hawler Medical University, Kurdistan Region Government, Erbil, Iraq.
Abutheraa N; Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, Glasgow, UK.
Akil L; Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, Glasgow, UK.
Godman B; Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, Glasgow, UK.; Division of Clinical Pharmacology, Karolinska Institute, Stockholm, Sweden.; Division of Public Health Pharmacy and Management, School of Pharmacy, Sefako Makgatho Health Sciences University, Pretoria, South Africa.
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Źródło :
Pharmacology research & perspectives [Pharmacol Res Perspect] 2020 Dec; Vol. 8 (6), pp. e00666.
Typ publikacji :
Journal Article; Meta-Analysis; Systematic Review
MeSH Terms :
Angiotensin Receptor Antagonists/*pharmacology
Angiotensin-Converting Enzyme Inhibitors/*pharmacology
Betacoronavirus/*drug effects
Cardiovascular Diseases/*drug therapy
Coronavirus Infections/*mortality
Pneumonia, Viral/*mortality
Adult ; Aged ; Angiotensin Receptor Antagonists/adverse effects ; Angiotensin Receptor Antagonists/therapeutic use ; Angiotensin-Converting Enzyme Inhibitors/adverse effects ; Angiotensin-Converting Enzyme Inhibitors/therapeutic use ; COVID-19 ; Cardiovascular Diseases/complications ; Comorbidity ; Coronavirus Infections/epidemiology ; Coronavirus Infections/virology ; Female ; Hospital Mortality/trends ; Hospitalization/statistics & numerical data ; Humans ; Hypertension/complications ; Hypertension/drug therapy ; Intensive Care Units/statistics & numerical data ; Male ; Middle Aged ; Observational Studies as Topic ; Outcome Assessment, Health Care ; Pandemics ; Pneumonia, Viral/epidemiology ; Pneumonia, Viral/virology ; Risk Assessment ; SARS-CoV-2 ; Ventilators, Mechanical/adverse effects ; Ventilators, Mechanical/statistics & numerical data
Czasopismo naukowe
Tytuł :
Denovo designing, retro-combinatorial synthesis, and molecular dynamics analysis identify novel antiviral VTRM1.1 against RNA-dependent RNA polymerase of SARS CoV2 virus.
Autorzy :
Tiwari V; Department of Biochemistry, Central University of Rajasthan, Ajmer 305817, India. Electronic address: .
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Źródło :
International journal of biological macromolecules [Int J Biol Macromol] 2021 Feb 28; Vol. 171, pp. 358-365. Date of Electronic Publication: 2021 Jan 07.
Typ publikacji :
Journal Article
MeSH Terms :
Antiviral Agents*/chemical synthesis
Antiviral Agents*/chemistry
Drug Design*
Enzyme Inhibitors*/chemical synthesis
Enzyme Inhibitors*/chemistry
Coronavirus RNA-Dependent RNA Polymerase/*antagonists & inhibitors
SARS-CoV-2/*enzymology
Binding Sites ; COVID-19 ; Humans ; Molecular Dynamics Simulation ; Protein Domains
Czasopismo naukowe
Tytuł :
Tipiracil binds to uridine site and inhibits Nsp15 endoribonuclease NendoU from SARS-CoV-2.
Autorzy :
Kim Y; Center for Structural Genomics of Infectious Diseases, Consortium for Advanced Science and Engineering, University of Chicago, Chicago, IL, 60667, USA.; Structural Biology Center, X-ray Science Division, Argonne National Laboratory, Argonne, IL, 60439, USA.
Wower J; Department of Animal Sciences, Auburn University, Auburn, AL, 36849, USA.
Maltseva N; Center for Structural Genomics of Infectious Diseases, Consortium for Advanced Science and Engineering, University of Chicago, Chicago, IL, 60667, USA.; Structural Biology Center, X-ray Science Division, Argonne National Laboratory, Argonne, IL, 60439, USA.
Chang C; Center for Structural Genomics of Infectious Diseases, Consortium for Advanced Science and Engineering, University of Chicago, Chicago, IL, 60667, USA.; Structural Biology Center, X-ray Science Division, Argonne National Laboratory, Argonne, IL, 60439, USA.
Jedrzejczak R; Center for Structural Genomics of Infectious Diseases, Consortium for Advanced Science and Engineering, University of Chicago, Chicago, IL, 60667, USA.; Structural Biology Center, X-ray Science Division, Argonne National Laboratory, Argonne, IL, 60439, USA.
Wilamowski M; Department of Biochemistry and Molecular Biology, University of Chicago, Chicago, IL, 60367, USA.
Kang S; Department of Microbiology, Ricketts Laboratory, University of Chicago, Chicago, IL, 60367, USA.
Nicolaescu V; Department of Microbiology, Ricketts Laboratory, University of Chicago, Chicago, IL, 60367, USA.
Randall G; Department of Microbiology, Ricketts Laboratory, University of Chicago, Chicago, IL, 60367, USA.
Michalska K; Center for Structural Genomics of Infectious Diseases, Consortium for Advanced Science and Engineering, University of Chicago, Chicago, IL, 60667, USA.; Structural Biology Center, X-ray Science Division, Argonne National Laboratory, Argonne, IL, 60439, USA.
Joachimiak A; Center for Structural Genomics of Infectious Diseases, Consortium for Advanced Science and Engineering, University of Chicago, Chicago, IL, 60667, USA. .; Structural Biology Center, X-ray Science Division, Argonne National Laboratory, Argonne, IL, 60439, USA. .; Department of Biochemistry and Molecular Biology, University of Chicago, Chicago, IL, 60367, USA. .
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Źródło :
Communications biology [Commun Biol] 2021 Feb 09; Vol. 4 (1), pp. 193. Date of Electronic Publication: 2021 Feb 09.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, Non-P.H.S.
MeSH Terms :
Antiviral Agents/*pharmacology
COVID-19/*drug therapy
COVID-19/*virology
Endoribonucleases/*antagonists & inhibitors
Enzyme Inhibitors/*pharmacology
Pyrrolidines/*pharmacology
SARS-CoV-2/*drug effects
SARS-CoV-2/*enzymology
Thymine/*pharmacology
Viral Nonstructural Proteins/*antagonists & inhibitors
A549 Cells ; Antiviral Agents/chemistry ; Antiviral Agents/pharmacokinetics ; Catalytic Domain ; Crystallography, X-Ray ; Endoribonucleases/chemistry ; Endoribonucleases/metabolism ; Enzyme Inhibitors/chemistry ; Enzyme Inhibitors/pharmacokinetics ; Humans ; Ligands ; Models, Molecular ; Protein Conformation ; Pyrrolidines/chemistry ; Pyrrolidines/pharmacokinetics ; Thymine/chemistry ; Thymine/pharmacokinetics ; Uridine/metabolism ; Viral Nonstructural Proteins/chemistry ; Viral Nonstructural Proteins/metabolism
Czasopismo naukowe
Tytuł :
Development of a thin-layer chromatography bioautographic assay for neuraminidase inhibitors hyphenated with electrostatic field induced spray ionisation-mass spectrometry for identification of active Isatis indigotica root compounds.
Autorzy :
Zang Y; Department of Natural Medicine, School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai 201203, China.
Miao Y; Key Laboratory of Standardization of Chinese Medicines of Ministry of Education, Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Shanghai 201203, China.
Wu T; Key Laboratory of Standardization of Chinese Medicines of Ministry of Education, Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Shanghai 201203, China. Electronic address: .
Cheng Z; Department of Natural Medicine, School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai 201203, China. Electronic address: .
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Źródło :
Journal of chromatography. A [J Chromatogr A] 2021 Feb 08; Vol. 1638, pp. 461597. Date of Electronic Publication: 2020 Sep 29.
Typ publikacji :
Journal Article
MeSH Terms :
Static Electricity*
Chromatography, Thin Layer/*methods
Enzyme Inhibitors/*analysis
Enzyme Inhibitors/*pharmacology
Isatis/*chemistry
Mass Spectrometry/*methods
Neuraminidase/*antagonists & inhibitors
Plant Roots/*chemistry
Analysis of Variance ; Biological Assay ; Calcium Chloride/pharmacology ; Chemical Fractionation ; Enzyme Inhibitors/chemistry ; Hydrogen-Ion Concentration ; Limit of Detection ; Plant Extracts/chemistry ; Spectrophotometry, Ultraviolet ; Substrate Specificity/drug effects ; Time Factors
Czasopismo naukowe
Tytuł :
Diverse chemical space of indoleamine-2,3-dioxygenase 1 (Ido1) inhibitors.
Autorzy :
Singh R; Department of Chemistry and Centre of Advanced Studies in Chemistry, Panjab University, Chandigarh, 160 014, India.
Salunke DB; Department of Chemistry and Centre of Advanced Studies in Chemistry, Panjab University, Chandigarh, 160 014, India; National Interdisciplinary Centre of Vaccine, Immunotherapeutics and Antimicrobials, Panjab University, Chandigarh, 160 014, India. Electronic address: .
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Źródło :
European journal of medicinal chemistry [Eur J Med Chem] 2021 Feb 05; Vol. 211, pp. 113071. Date of Electronic Publication: 2020 Dec 02.
Typ publikacji :
Journal Article; Review
MeSH Terms :
COVID-19/*drug therapy
Enzyme Inhibitors/*pharmacology
Indoleamine-Pyrrole 2,3,-Dioxygenase/*antagonists & inhibitors
Biological Products ; Enzyme Inhibitors/chemistry ; Enzyme Inhibitors/therapeutic use ; Humans ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł :
Advantages of brain penetrating inhibitors of kynurenine-3-monooxygenase for treatment of neurodegenerative diseases.
Autorzy :
Zhang S; Manchester Institute of Biotechnology, Department of Chemistry, School of Natural Sciences, The University of Manchester, 131 Princess Street, Manchester, M1 7DN, UK.
Collier MEW; Department of Genetics and Genome Biology, University of Leicester, Leicester, LE1 7RH, UK.
Heyes DJ; Manchester Institute of Biotechnology, Department of Chemistry, School of Natural Sciences, The University of Manchester, 131 Princess Street, Manchester, M1 7DN, UK.
Giorgini F; Department of Genetics and Genome Biology, University of Leicester, Leicester, LE1 7RH, UK.
Scrutton NS; Manchester Institute of Biotechnology, Department of Chemistry, School of Natural Sciences, The University of Manchester, 131 Princess Street, Manchester, M1 7DN, UK. Electronic address: .
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Źródło :
Archives of biochemistry and biophysics [Arch Biochem Biophys] 2021 Jan 15; Vol. 697, pp. 108702. Date of Electronic Publication: 2020 Dec 01.
Typ publikacji :
Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't; Review
MeSH Terms :
Brain/*metabolism
Enzyme Inhibitors/*metabolism
Enzyme Inhibitors/*pharmacology
Kynurenine 3-Monooxygenase/*antagonists & inhibitors
Neurodegenerative Diseases/*drug therapy
Animals ; Brain/drug effects ; Drug Discovery ; Enzyme Inhibitors/therapeutic use ; Humans ; Neurodegenerative Diseases/enzymology ; Neurodegenerative Diseases/metabolism
Czasopismo naukowe
Tytuł :
Diflunisal Derivatives as Modulators of ACMS Decarboxylase Targeting the Tryptophan-Kynurenine Pathway.
Autorzy :
Yang Y; Department of Chemistry, University of Texas at San Antonio, San Antonio, Texas 78249, United States.
Borel T; Department of Medicinal Chemistry, The University of Kansas, Lawrence, Kansas 66045, United States.
de Azambuja F; Department of Chemistry, KU Leuven, Celestijnenlaan 200F, 3001 Leuven, Belgium.
Johnson D; Computational Chemical Biology Core and Molecular Graphics and Modeling Laboratory, The University of Kansas, Lawrence, Kansas 66045, United States.
Sorrentino JP; Department of Medicinal Chemistry, The University of Kansas, Lawrence, Kansas 66045, United States.
Udokwu C; Department of Chemistry, University of Texas at San Antonio, San Antonio, Texas 78249, United States.
Davis I; Department of Chemistry, University of Texas at San Antonio, San Antonio, Texas 78249, United States.
Liu A; Department of Chemistry, University of Texas at San Antonio, San Antonio, Texas 78249, United States.
Altman RA; Department of Medicinal Chemistry and Molecular Pharmacology and Department of Chemistry, Purdue University, 575 Stadium Mall Drive, West Lafayette, Indiana 47907, United States.
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Źródło :
Journal of medicinal chemistry [J Med Chem] 2021 Jan 14; Vol. 64 (1), pp. 797-811. Date of Electronic Publication: 2020 Dec 28.
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 :
Carboxy-Lyases/*metabolism
Diflunisal/*metabolism
Enzyme Inhibitors/*metabolism
Bacterial Proteins/antagonists & inhibitors ; Bacterial Proteins/metabolism ; Binding Sites ; Biosynthetic Pathways/drug effects ; Carboxy-Lyases/antagonists & inhibitors ; Catalytic Domain ; Crystallography, X-Ray ; Diflunisal/analogs & derivatives ; Diflunisal/pharmacology ; Enzyme Inhibitors/chemistry ; Enzyme Inhibitors/pharmacology ; Humans ; Inhibitory Concentration 50 ; Kynurenine/metabolism ; Molecular Docking Simulation ; NAD/metabolism ; Pseudomonas fluorescens/enzymology ; Structure-Activity Relationship ; Tryptophan/metabolism
Czasopismo naukowe
Tytuł :
In Search for Multi-Target Ligands as Potential Agents for Diabetes Mellitus and Its Complications-A Structure-Activity Relationship Study on Inhibitors of Aldose Reductase and Protein Tyrosine Phosphatase 1B.
Autorzy :
Ottanà R; Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Viale Palatucci, Polo Universitario Annunziata, 98168 Messina, Italy.
Paoli P; Department of Scienze Biomediche Sperimentali e Cliniche, Sezione di Scienze Biochimiche, University of Firenze, Viale Morgagni 50, 50134 Firenze, Italy.
Cappiello M; Department of Biology, Biochemistry Unit, University of Pisa, Via S. Zeno, 51, 56123 Pisa, Italy.
Nguyen TN; Molecular Design Lab, Institute of Pharmacy, Freie Universität Berlin, Königin-Luisestr. 2 + 4, 14195 Berlin, Germany.
Adornato I; Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Viale Palatucci, Polo Universitario Annunziata, 98168 Messina, Italy.
Del Corso A; Department of Biology, Biochemistry Unit, University of Pisa, Via S. Zeno, 51, 56123 Pisa, Italy.
Genovese M; Department of Scienze Biomediche Sperimentali e Cliniche, Sezione di Scienze Biochimiche, University of Firenze, Viale Morgagni 50, 50134 Firenze, Italy.
Nesi I; Department of Scienze Biomediche Sperimentali e Cliniche, Sezione di Scienze Biochimiche, University of Firenze, Viale Morgagni 50, 50134 Firenze, Italy.
Moschini R; Department of Biology, Biochemistry Unit, University of Pisa, Via S. Zeno, 51, 56123 Pisa, Italy.
Naß A; Molecular Design Lab, Institute of Pharmacy, Freie Universität Berlin, Königin-Luisestr. 2 + 4, 14195 Berlin, Germany.
Wolber G; Molecular Design Lab, Institute of Pharmacy, Freie Universität Berlin, Königin-Luisestr. 2 + 4, 14195 Berlin, Germany.
Maccari R; Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Viale Palatucci, Polo Universitario Annunziata, 98168 Messina, Italy.
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Źródło :
Molecules (Basel, Switzerland) [Molecules] 2021 Jan 10; Vol. 26 (2). Date of Electronic Publication: 2021 Jan 10.
Typ publikacji :
Journal Article
MeSH Terms :
Enzyme Inhibitors*/chemistry
Enzyme Inhibitors*/pharmacology
Hypoglycemic Agents*/chemistry
Hypoglycemic Agents*/pharmacology
Aldehyde Reductase/*antagonists & inhibitors
Diabetes Mellitus/*drug therapy
Protein Tyrosine Phosphatase, Non-Receptor Type 1/*antagonists & inhibitors
Aldehyde Reductase/metabolism ; Animals ; Diabetes Mellitus/enzymology ; Drug Evaluation, Preclinical ; Hep G2 Cells ; Humans ; Ligands ; Mice ; Protein Tyrosine Phosphatase, Non-Receptor Type 1/metabolism ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł :
Crystal structures of human NSDHL and development of its novel inhibitor with the potential to suppress EGFR activity.
Autorzy :
Kim DG; Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul, 08826, Republic of Korea.
Cho S; Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul, 08826, Republic of Korea.
Lee KY; Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul, 08826, Republic of Korea.
Cheon SH; Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul, 08826, Republic of Korea.
Yoon HJ; Department of Chemistry, College of Natural Sciences, Seoul National University, Seoul, 08826, Republic of Korea.
Lee JY; Chemical Data-Driven Research Center, Korea Research Institute of Chemical Technology, Daejeon, 34114, Republic of Korea.
Kim D; Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul, 08826, Republic of Korea.
Shin KS; Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul, 08826, Republic of Korea.
Koh CH; Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul, 08826, Republic of Korea.
Koo JS; Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul, 08826, Republic of Korea.
Choi Y; Department of Chemistry, College of Natural Sciences, Seoul National University, Seoul, 08826, Republic of Korea.
Lee HH; Department of Chemistry, College of Natural Sciences, Seoul National University, Seoul, 08826, Republic of Korea.
Oh YK; Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul, 08826, Republic of Korea.
Jeong YS; Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul, 08826, Republic of Korea.
Chung SJ; Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul, 08826, Republic of Korea.
Baek M; Therapeutics & Biotechnology Division, Korea Research Institute of Chemical Technology, Daejeon, 34114, Republic of Korea.
Jung KY; Therapeutics & Biotechnology Division, Korea Research Institute of Chemical Technology, Daejeon, 34114, Republic of Korea.; Department of Medicinal Chemistry and Pharmacology, University of Science and Technology, Daejeon, 34113, Republic of Korea.
Lim HJ; Research Institute, National Cancer Center, Goyang-si, Gyeonggi-do, 10408, Republic of Korea.
Kim HS; Research Institute, National Cancer Center, Goyang-si, Gyeonggi-do, 10408, Republic of Korea.
Park SJ; Gachon Institute of Pharmaceutical Sciences, College of Pharmacy, Gachon University, Incheon, 13120, Republic of Korea.
Lee JY; Department of Medicine, College of Medicine, Hanyang University, Seoul, 04763, Republic of Korea.
Lee SJ; PAL-XFEL, Pohang Accelerator Laboratory, POSTECH, Pohang, Gyeongbuk, 37673, Republic of Korea. .
Lee BJ; Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul, 08826, Republic of Korea. .
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Źródło :
Cellular and molecular life sciences : CMLS [Cell Mol Life Sci] 2021 Jan; Vol. 78 (1), pp. 207-225. Date of Electronic Publication: 2020 Mar 05.
Typ publikacji :
Journal Article
MeSH Terms :
3-Hydroxysteroid Dehydrogenases/*metabolism
Enzyme Inhibitors/*metabolism
3-Hydroxysteroid Dehydrogenases/antagonists & inhibitors ; 3-Hydroxysteroid Dehydrogenases/chemistry ; 3-Hydroxysteroid Dehydrogenases/genetics ; Binding Sites ; Cell Line, Tumor ; Cell Survival/drug effects ; Cholesterol/chemistry ; Crystallography, X-Ray ; Enzyme Inhibitors/chemistry ; Enzyme Inhibitors/pharmacology ; ErbB Receptors/antagonists & inhibitors ; ErbB Receptors/metabolism ; Erlotinib Hydrochloride/chemistry ; Erlotinib Hydrochloride/metabolism ; Erlotinib Hydrochloride/pharmacology ; Humans ; Kinetics ; Molecular Docking Simulation ; Mutagenesis, Site-Directed ; NAD/chemistry ; NAD/metabolism ; Protein Structure, Tertiary ; Recombinant Proteins/biosynthesis ; Recombinant Proteins/chemistry ; Recombinant Proteins/isolation & purification ; Signal Transduction
Czasopismo naukowe
Tytuł :
Design, Synthesis, and Biological Evaluation of a Series of Oxazolone Carboxamides as a Novel Class of Acid Ceramidase Inhibitors.
Autorzy :
Caputo S; Fondazione Istituto Italiano di Tecnologia, Via Morego 30, I-16163 Genova, Italy.; Drug Discovery and Development (D3)-Validation, Via Morego 30, I-16163 Genova, Italy.
Di Martino S; Fondazione Istituto Italiano di Tecnologia, Via Morego 30, I-16163 Genova, Italy.; Drug Discovery and Development (D3)-Validation, Via Morego 30, I-16163 Genova, Italy.
Cilibrasi V; Fondazione Istituto Italiano di Tecnologia, Via Morego 30, I-16163 Genova, Italy.; Drug Discovery and Development (D3)-Validation, Via Morego 30, I-16163 Genova, Italy.
Tardia P; Fondazione Istituto Italiano di Tecnologia, Via Morego 30, I-16163 Genova, Italy.; Drug Discovery and Development (D3)-Validation, Via Morego 30, I-16163 Genova, Italy.
Mazzonna M; Fondazione Istituto Italiano di Tecnologia, Via Morego 30, I-16163 Genova, Italy.; Drug Discovery and Development (D3)-Validation, Via Morego 30, I-16163 Genova, Italy.
Russo D; Fondazione Istituto Italiano di Tecnologia, Via Morego 30, I-16163 Genova, Italy.; D3-Pharma Chemistry, Via Morego 30, I-16163 Genova, Italy.
Penna I; Fondazione Istituto Italiano di Tecnologia, Via Morego 30, I-16163 Genova, Italy.; D3-Pharma Chemistry, Via Morego 30, I-16163 Genova, Italy.
Summa M; Fondazione Istituto Italiano di Tecnologia, Via Morego 30, I-16163 Genova, Italy.; Analytical Chemistry and Translational Pharmacology, Via Morego 30, I-16163 Genova, Italy.
Bertozzi SM; Fondazione Istituto Italiano di Tecnologia, Via Morego 30, I-16163 Genova, Italy.; Analytical Chemistry and Translational Pharmacology, Via Morego 30, I-16163 Genova, Italy.
Realini N; Fondazione Istituto Italiano di Tecnologia, Via Morego 30, I-16163 Genova, Italy.; Drug Discovery and Development (D3)-Validation, Via Morego 30, I-16163 Genova, Italy.
Margaroli N; Fondazione Istituto Italiano di Tecnologia, Via Morego 30, I-16163 Genova, Italy.; Drug Discovery and Development (D3)-Validation, Via Morego 30, I-16163 Genova, Italy.
Migliore M; Fondazione Istituto Italiano di Tecnologia, Via Morego 30, I-16163 Genova, Italy.; Drug Discovery and Development (D3)-Validation, Via Morego 30, I-16163 Genova, Italy.
Ottonello G; Fondazione Istituto Italiano di Tecnologia, Via Morego 30, I-16163 Genova, Italy.; Analytical Chemistry and Translational Pharmacology, Via Morego 30, I-16163 Genova, Italy.
Liu M; Lysosomal Therapeutics Inc., 19 Blackstone Street, Cambridge, Massachusetts 02139, United States.
Lansbury P; Lysosomal Therapeutics Inc., 19 Blackstone Street, Cambridge, Massachusetts 02139, United States.
Armirotti A; Fondazione Istituto Italiano di Tecnologia, Via Morego 30, I-16163 Genova, Italy.; Analytical Chemistry and Translational Pharmacology, Via Morego 30, I-16163 Genova, Italy.
Bertorelli R; Fondazione Istituto Italiano di Tecnologia, Via Morego 30, I-16163 Genova, Italy.; Analytical Chemistry and Translational Pharmacology, Via Morego 30, I-16163 Genova, Italy.
Ray SS; Lysosomal Therapeutics Inc., 19 Blackstone Street, Cambridge, Massachusetts 02139, United States.
Skerlj R; Lysosomal Therapeutics Inc., 19 Blackstone Street, Cambridge, Massachusetts 02139, United States.
Scarpelli R; Fondazione Istituto Italiano di Tecnologia, Via Morego 30, I-16163 Genova, Italy.; Drug Discovery and Development (D3)-Validation, Via Morego 30, I-16163 Genova, Italy.
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Źródło :
Journal of medicinal chemistry [J Med Chem] 2020 Dec 24; Vol. 63 (24), pp. 15821-15851. Date of Electronic Publication: 2020 Dec 08.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Drug Design*
Acid Ceramidase/*antagonists & inhibitors
Enzyme Inhibitors/*chemical synthesis
Oxazolone/*chemistry
Acid Ceramidase/metabolism ; Administration, Oral ; Animals ; Binding Sites ; Cell Line, Tumor ; Enzyme Inhibitors/metabolism ; Enzyme Inhibitors/pharmacokinetics ; Half-Life ; Humans ; Inhibitory Concentration 50 ; Kinetics ; Male ; Mice ; Mice, Inbred C57BL ; Microsomes/metabolism ; Molecular Docking Simulation ; Oxazolone/metabolism ; Oxazolone/pharmacokinetics ; Solubility ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł :
Discovery of OATD-01 , a First-in-Class Chitinase Inhibitor as Potential New Therapeutics for Idiopathic Pulmonary Fibrosis.
Autorzy :
Koralewski R; OncoArendi Therapeutics SA, Żwirki i Wigury 101, 02-089 Warsaw, Poland.
Dymek B; OncoArendi Therapeutics SA, Żwirki i Wigury 101, 02-089 Warsaw, Poland.
Mazur M; OncoArendi Therapeutics SA, Żwirki i Wigury 101, 02-089 Warsaw, Poland.
Sklepkiewicz P; OncoArendi Therapeutics SA, Żwirki i Wigury 101, 02-089 Warsaw, Poland.
Olejniczak S; OncoArendi Therapeutics SA, Żwirki i Wigury 101, 02-089 Warsaw, Poland.
Czestkowski W; OncoArendi Therapeutics SA, Żwirki i Wigury 101, 02-089 Warsaw, Poland.
Matyszewski K; OncoArendi Therapeutics SA, Żwirki i Wigury 101, 02-089 Warsaw, Poland.
Andryianau G; OncoArendi Therapeutics SA, Żwirki i Wigury 101, 02-089 Warsaw, Poland.
Niedziejko P; OncoArendi Therapeutics SA, Żwirki i Wigury 101, 02-089 Warsaw, Poland.
Kowalski M; OncoArendi Therapeutics SA, Żwirki i Wigury 101, 02-089 Warsaw, Poland.
Gruza M; OncoArendi Therapeutics SA, Żwirki i Wigury 101, 02-089 Warsaw, Poland.
Borek B; OncoArendi Therapeutics SA, Żwirki i Wigury 101, 02-089 Warsaw, Poland.
Jedrzejczak K; OncoArendi Therapeutics SA, Żwirki i Wigury 101, 02-089 Warsaw, Poland.
Bartoszewicz A; OncoArendi Therapeutics SA, Żwirki i Wigury 101, 02-089 Warsaw, Poland.
Pluta E; OncoArendi Therapeutics SA, Żwirki i Wigury 101, 02-089 Warsaw, Poland.
Rymaszewska A; OncoArendi Therapeutics SA, Żwirki i Wigury 101, 02-089 Warsaw, Poland.
Kania M; OncoArendi Therapeutics SA, Żwirki i Wigury 101, 02-089 Warsaw, Poland.
Rejczak T; OncoArendi Therapeutics SA, Żwirki i Wigury 101, 02-089 Warsaw, Poland.
Piasecka S; OncoArendi Therapeutics SA, Żwirki i Wigury 101, 02-089 Warsaw, Poland.
Mlacki M; OncoArendi Therapeutics SA, Żwirki i Wigury 101, 02-089 Warsaw, Poland.
Mazurkiewicz M; OncoArendi Therapeutics SA, Żwirki i Wigury 101, 02-089 Warsaw, Poland.
Piotrowicz M; OncoArendi Therapeutics SA, Żwirki i Wigury 101, 02-089 Warsaw, Poland.
Salamon M; OncoArendi Therapeutics SA, Żwirki i Wigury 101, 02-089 Warsaw, Poland.
Zagozdzon A; OncoArendi Therapeutics SA, Żwirki i Wigury 101, 02-089 Warsaw, Poland.
Napiorkowska-Gromadzka A; Structural Biology Center, International Institute of Molecular and Cell Biology, Trojdena 4, 02-109 Warsaw, Poland.
Bartlomiejczak A; Structural Biology Center, International Institute of Molecular and Cell Biology, Trojdena 4, 02-109 Warsaw, Poland.
Mozga W; OncoArendi Therapeutics SA, Żwirki i Wigury 101, 02-089 Warsaw, Poland.
Dobrzański P; OncoArendi Therapeutics SA, Żwirki i Wigury 101, 02-089 Warsaw, Poland.
Dzwonek K; OncoArendi Therapeutics SA, Żwirki i Wigury 101, 02-089 Warsaw, Poland.
Golab J; OncoArendi Therapeutics SA, Żwirki i Wigury 101, 02-089 Warsaw, Poland.; Department of Immunology, Medical University of Warsaw, Nielubowicza 5, 02-097 Warsaw, Poland.
Nowotny M; Structural Biology Center, International Institute of Molecular and Cell Biology, Trojdena 4, 02-109 Warsaw, Poland.
Olczak J; OncoArendi Therapeutics SA, Żwirki i Wigury 101, 02-089 Warsaw, Poland.
Golebiowski A; OncoArendi Therapeutics SA, Żwirki i Wigury 101, 02-089 Warsaw, Poland.
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Źródło :
Journal of medicinal chemistry [J Med Chem] 2020 Dec 24; Vol. 63 (24), pp. 15527-15540. Date of Electronic Publication: 2020 Oct 20.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Chitinases/*antagonists & inhibitors
Enzyme Inhibitors/*therapeutic use
Idiopathic Pulmonary Fibrosis/*drug therapy
Piperidines/*chemistry
Administration, Oral ; Animals ; Binding Sites ; Bleomycin/toxicity ; Catalytic Domain ; Chitinases/metabolism ; Clinical Trials, Phase I as Topic ; Disease Models, Animal ; Dogs ; Enzyme Inhibitors/chemistry ; Enzyme Inhibitors/pharmacokinetics ; Female ; Half-Life ; Humans ; Idiopathic Pulmonary Fibrosis/chemically induced ; Idiopathic Pulmonary Fibrosis/pathology ; Lung/metabolism ; Mice ; Molecular Docking Simulation ; Piperidines/pharmacokinetics ; Piperidines/therapeutic use ; Rats ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł :
Switching a Xanthine Oxidase Inhibitor to a Dual-Target Antagonist of P2Y 1 and P2Y 12 as an Oral Antiplatelet Agent with a Wider Therapeutic Window in Rats than Ticagrelor.
Autorzy :
Lei Y; Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, 103 Culture Road, Shenhe District, Shenyang 110016, China.
Zhang B; Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, 103 Culture Road, Shenhe District, Shenyang 110016, China.
Liu D; Shenyang Hinewy Pharmaceutical Technology Co., Ltd., 41 Liutang Road, Shenhe District, Shenyang 110016, China.
Zhao J; Department of Pharmacology, Shenyang Pharmaceutical University, 103 Culture Road, Shenhe District, Shenyang 110016, China.
Dai X; Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, 103 Culture Road, Shenhe District, Shenyang 110016, China.
Gao J; Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, 103 Culture Road, Shenhe District, Shenyang 110016, China.
Mao Q; Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, 103 Culture Road, Shenhe District, Shenyang 110016, China.
Feng Y; Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, 103 Culture Road, Shenhe District, Shenyang 110016, China.
Zhao J; Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, 103 Culture Road, Shenhe District, Shenyang 110016, China.
Lin F; Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, 103 Culture Road, Shenhe District, Shenyang 110016, China.
Duan Y; Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, 103 Culture Road, Shenhe District, Shenyang 110016, China.
Zhang Y; Department of Pharmacology, Shenyang Pharmaceutical University, 103 Culture Road, Shenhe District, Shenyang 110016, China.
Bao Z; Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, 103 Culture Road, Shenhe District, Shenyang 110016, China.
Yang Y; Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, 103 Culture Road, Shenhe District, Shenyang 110016, China.
Mou Y; Department of Pharmacology, Shenyang Pharmaceutical University, 103 Culture Road, Shenhe District, Shenyang 110016, China.
Wang S; Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, 103 Culture Road, Shenhe District, Shenyang 110016, China.
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Źródło :
Journal of medicinal chemistry [J Med Chem] 2020 Dec 24; Vol. 63 (24), pp. 15752-15772. Date of Electronic Publication: 2020 Dec 12.
Typ publikacji :
Journal Article
MeSH Terms :
Enzyme Inhibitors/*chemistry
Platelet Aggregation Inhibitors/*chemistry
Purinergic P2Y Receptor Antagonists/*chemistry
Receptors, Purinergic P2Y1/*chemistry
Receptors, Purinergic P2Y12/*chemistry
Xanthine Oxidase/*antagonists & inhibitors
Animals ; Binding Sites ; Cytochrome P-450 Enzyme System/chemistry ; Cytochrome P-450 Enzyme System/metabolism ; Drug Stability ; Enzyme Inhibitors/metabolism ; Enzyme Inhibitors/pharmacology ; Half-Life ; Humans ; Imidazoles/chemistry ; Imidazoles/metabolism ; Imidazoles/pharmacology ; Mice ; Microsomes, Liver/metabolism ; Molecular Docking Simulation ; Platelet Aggregation/drug effects ; Platelet Aggregation Inhibitors/metabolism ; Platelet Aggregation Inhibitors/pharmacology ; Purinergic P2Y Receptor Antagonists/metabolism ; Rats ; Receptors, Purinergic P2Y1/metabolism ; Receptors, Purinergic P2Y12/metabolism ; Structure-Activity Relationship ; Ticagrelor/pharmacology ; Xanthine Oxidase/metabolism
Czasopismo naukowe
Tytuł :
From Pyrazolones to Azaindoles: Evolution of Active-Site SHP2 Inhibitors Based on Scaffold Hopping and Bioisosteric Replacement.
Autorzy :
Mostinski Y; Leibniz-Forschungsinstitut für Molekulare Pharmakologie (FMP), Campus Berlin-Buch, Robert-Rössle-Str. 10, 13125 Berlin, Germany.
Heynen GJJE; Max Delbrück Center for Molecular Medicine in the Helmholtz Association (MDC), Campus Berlin-Buch, Robert-Rössle-Str. 10, 13125 Berlin, Germany.
López-Alberca MP; Leibniz-Forschungsinstitut für Molekulare Pharmakologie (FMP), Campus Berlin-Buch, Robert-Rössle-Str. 10, 13125 Berlin, Germany.
Paul J; Leibniz-Forschungsinstitut für Molekulare Pharmakologie (FMP), Campus Berlin-Buch, Robert-Rössle-Str. 10, 13125 Berlin, Germany.
Miksche S; Leibniz-Forschungsinstitut für Molekulare Pharmakologie (FMP), Campus Berlin-Buch, Robert-Rössle-Str. 10, 13125 Berlin, Germany.
Radetzki S; Leibniz-Forschungsinstitut für Molekulare Pharmakologie (FMP), Campus Berlin-Buch, Robert-Rössle-Str. 10, 13125 Berlin, Germany.
Schaller D; Charité-Universitätsmedizin Berlin, Charitéplatz 1, 10117 Berlin, Germany.
Shanina E; Max-Planck-Institut für Kolloid- und Grenzflächenforschung, Am Mühlenberg, 1, 14476 Potsdam, Germany.
Seyffarth C; Leibniz-Forschungsinstitut für Molekulare Pharmakologie (FMP), Campus Berlin-Buch, Robert-Rössle-Str. 10, 13125 Berlin, Germany.
Kolomeets Y; Leibniz-Forschungsinstitut für Molekulare Pharmakologie (FMP), Campus Berlin-Buch, Robert-Rössle-Str. 10, 13125 Berlin, Germany.
Ziebart N; Leibniz-Forschungsinstitut für Molekulare Pharmakologie (FMP), Campus Berlin-Buch, Robert-Rössle-Str. 10, 13125 Berlin, Germany.
de Schryver J; Leibniz-Forschungsinstitut für Molekulare Pharmakologie (FMP), Campus Berlin-Buch, Robert-Rössle-Str. 10, 13125 Berlin, Germany.
Oestreich S; Leibniz-Forschungsinstitut für Molekulare Pharmakologie (FMP), Campus Berlin-Buch, Robert-Rössle-Str. 10, 13125 Berlin, Germany.
Neuenschwander M; Leibniz-Forschungsinstitut für Molekulare Pharmakologie (FMP), Campus Berlin-Buch, Robert-Rössle-Str. 10, 13125 Berlin, Germany.
Roske Y; Max Delbrück Center for Molecular Medicine in the Helmholtz Association (MDC), Campus Berlin-Buch, Robert-Rössle-Str. 10, 13125 Berlin, Germany.
Heinemann U; Max Delbrück Center for Molecular Medicine in the Helmholtz Association (MDC), Campus Berlin-Buch, Robert-Rössle-Str. 10, 13125 Berlin, Germany.
Rademacher C; Max-Planck-Institut für Kolloid- und Grenzflächenforschung, Am Mühlenberg, 1, 14476 Potsdam, Germany.
Volkamer A; Charité-Universitätsmedizin Berlin, Charitéplatz 1, 10117 Berlin, Germany.
von Kries JP; Leibniz-Forschungsinstitut für Molekulare Pharmakologie (FMP), Campus Berlin-Buch, Robert-Rössle-Str. 10, 13125 Berlin, Germany.
Birchmeier W; Max Delbrück Center for Molecular Medicine in the Helmholtz Association (MDC), Campus Berlin-Buch, Robert-Rössle-Str. 10, 13125 Berlin, Germany.
Nazaré M; Leibniz-Forschungsinstitut für Molekulare Pharmakologie (FMP), Campus Berlin-Buch, Robert-Rössle-Str. 10, 13125 Berlin, Germany.
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Źródło :
Journal of medicinal chemistry [J Med Chem] 2020 Dec 10; Vol. 63 (23), pp. 14780-14804. Date of Electronic Publication: 2020 Nov 19.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Enzyme Inhibitors/*pharmacology
Indoles/*pharmacology
Protein Tyrosine Phosphatase, Non-Receptor Type 11/*antagonists & inhibitors
Pyrazolones/*pharmacology
Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/metabolism ; Antineoplastic Agents/pharmacology ; Catalytic Domain ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Drug Screening Assays, Antitumor ; Enzyme Inhibitors/chemical synthesis ; Enzyme Inhibitors/metabolism ; Humans ; Indoles/chemical synthesis ; Indoles/metabolism ; MAP Kinase Signaling System/drug effects ; Molecular Docking Simulation ; Molecular Dynamics Simulation ; Molecular Structure ; Protein Binding ; Protein Tyrosine Phosphatase, Non-Receptor Type 11/chemistry ; Protein Tyrosine Phosphatase, Non-Receptor Type 11/metabolism ; Pyrazolones/chemical synthesis ; Pyrazolones/metabolism ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł :
Design, synthesis, and biological evaluation of novel substituted thiourea derivatives as potential anticancer agents for NSCLC by blocking K-Ras protein-effectors interactions.
Autorzy :
Zhang Y; Tianjin Key Laboratory of Radiation Medicine and Molecular Nuclear Medicine, Institute of Radiation Medicine, Chinese Academy of Medical Sciences and Peking Union Medical College, Tianjin, China.
Meng X; Tianjin Key Laboratory of Radiation Medicine and Molecular Nuclear Medicine, Institute of Radiation Medicine, Chinese Academy of Medical Sciences and Peking Union Medical College, Tianjin, China.
Tang H; Tianjin Key Laboratory of Radiation Medicine and Molecular Nuclear Medicine, Institute of Radiation Medicine, Chinese Academy of Medical Sciences and Peking Union Medical College, Tianjin, China.
Cheng M; Tianjin Key Laboratory of Radiation Medicine and Molecular Nuclear Medicine, Institute of Radiation Medicine, Chinese Academy of Medical Sciences and Peking Union Medical College, Tianjin, China.
Yang F; Tianjin Key Laboratory of Radiation Medicine and Molecular Nuclear Medicine, Institute of Radiation Medicine, Chinese Academy of Medical Sciences and Peking Union Medical College, Tianjin, China.
Xu W; Tianjin Key Laboratory of Radiation Medicine and Molecular Nuclear Medicine, Institute of Radiation Medicine, Chinese Academy of Medical Sciences and Peking Union Medical College, Tianjin, China.
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Źródło :
Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2020 Dec; Vol. 35 (1), pp. 344-353.
Typ publikacji :
Journal Article
MeSH Terms :
Drug Design*
Antineoplastic Agents/*pharmacology
Carcinoma, Non-Small-Cell Lung/*drug therapy
Enzyme Inhibitors/*pharmacology
Lung Neoplasms/*drug therapy
Proto-Oncogene Proteins p21(ras)/*antagonists & inhibitors
Thiourea/*pharmacology
A549 Cells ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Carcinoma, Non-Small-Cell Lung/metabolism ; Carcinoma, Non-Small-Cell Lung/pathology ; Cell Proliferation/drug effects ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; Enzyme Inhibitors/chemical synthesis ; Enzyme Inhibitors/chemistry ; Humans ; Lung Neoplasms/metabolism ; Lung Neoplasms/pathology ; Molecular Structure ; Proto-Oncogene Proteins p21(ras)/metabolism ; Structure-Activity Relationship ; Thiourea/chemical synthesis ; Thiourea/chemistry
Czasopismo naukowe
Tytuł :
Combining carbonic anhydrase and thioredoxin reductase inhibitory motifs within a single molecule dramatically increases its cytotoxicity.
Autorzy :
Krasavin M; Saint Petersburg State University, Saint Petersburg, Russian Federation.
Sharonova T; Saint Petersburg State University, Saint Petersburg, Russian Federation.
Sharoyko V; Saint Petersburg State University, Saint Petersburg, Russian Federation.
Zhukovsky D; Saint Petersburg State University, Saint Petersburg, Russian Federation.
Kalinin S; Saint Petersburg State University, Saint Petersburg, Russian Federation.
Žalubovskis R; Latvian Institute of Organic Synthesis, Riga, Latvia.; Faculty of Materials Science and Applied Chemistry, Institute of Technology of Organic Chemistry, Riga Technical University, Riga, Latvia.
Tennikova T; Saint Petersburg State University, Saint Petersburg, Russian Federation.
Supuran CT; Neurofarba Department, Universita degli Studi di Firenze, Florence, Italy.
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Źródło :
Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2020 Dec; Vol. 35 (1), pp. 665-671.
Typ publikacji :
Journal Article
MeSH Terms :
Antineoplastic Agents/*pharmacology
Carbonic Anhydrases/*metabolism
Enzyme Inhibitors/*pharmacology
Sulfonamides/*pharmacology
Thioredoxin-Disulfide Reductase/*antagonists & inhibitors
Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Cell Survival/drug effects ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; Enzyme Inhibitors/chemical synthesis ; Enzyme Inhibitors/chemistry ; Humans ; Molecular Structure ; Structure-Activity Relationship ; Sulfonamides/chemical synthesis ; Sulfonamides/chemistry ; Thioredoxin-Disulfide Reductase/metabolism
Czasopismo naukowe
Tytuł :
Strong inhibitory activities and action modes of lipopeptides on lipase.
Autorzy :
Chen MC; Agricultural Bioresources Research Institute, Fujian Academy of Agricultural Sciences, Fuzhou, China.
Liu TT; College of Biological Science and Engineering, Xiamen University, Xiamen, China.
Wang JP; Agricultural Bioresources Research Institute, Fujian Academy of Agricultural Sciences, Fuzhou, China.
Chen YP; Agricultural Bioresources Research Institute, Fujian Academy of Agricultural Sciences, Fuzhou, China.
Chen QX; College of Biological Science and Engineering, Xiamen University, Xiamen, China.
Zhu YJ; Agricultural Bioresources Research Institute, Fujian Academy of Agricultural Sciences, Fuzhou, China.
Liu B; Agricultural Bioresources Research Institute, Fujian Academy of Agricultural Sciences, Fuzhou, China.
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Źródło :
Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2020 Dec; Vol. 35 (1), pp. 897-905.
Typ publikacji :
Journal Article
MeSH Terms :
Enzyme Inhibitors/*pharmacology
Lipase/*antagonists & inhibitors
Lipopeptides/*pharmacology
Bacillus/chemistry ; Dose-Response Relationship, Drug ; Enzyme Inhibitors/chemistry ; Enzyme Inhibitors/isolation & purification ; Lipase/metabolism ; Lipopeptides/chemistry ; Lipopeptides/isolation & purification ; Molecular Docking Simulation ; Molecular Structure ; Mucor/enzymology ; Structure-Activity Relationship
SCR Organism :
Bacillus velezensis
Czasopismo naukowe
Tytuł :
Sulfocoumarins as dual inhibitors of human carbonic anhydrase isoforms IX/XII and of human thioredoxin reductase.
Autorzy :
Krasavin M; Department of Chemistry, Saint Petersburg State University, Saint Petersburg, Russian Federation.
Žalubovskis R; Latvian Institute of Organic Synthesis, Riga, Latvia.; Faculty of Materials Science and Applied Chemistry, Institute of Technology of Organic Chemistry, Riga Technical University, Riga, Latvia.
Grandāne A; Latvian Institute of Organic Synthesis, Riga, Latvia.
Domračeva I; Latvian Institute of Organic Synthesis, Riga, Latvia.
Zhmurov P; Department of Chemistry, Saint Petersburg State University, Saint Petersburg, Russian Federation.
Supuran CT; Neurofarba Department, Universita degli Studi di Firenze, Florence, Italy.
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Źródło :
Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2020 Dec; Vol. 35 (1), pp. 506-510.
Typ publikacji :
Journal Article
MeSH Terms :
Antineoplastic Agents/*pharmacology
Carbonic Anhydrase IX/*antagonists & inhibitors
Carbonic Anhydrases/*metabolism
Coumarins/*pharmacology
Enzyme Inhibitors/*pharmacology
Thioredoxin-Disulfide Reductase/*antagonists & inhibitors
Antigens, Neoplasm/metabolism ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Carbonic Anhydrase IX/metabolism ; Cell Proliferation/drug effects ; Cell Survival/drug effects ; Coumarins/chemical synthesis ; Coumarins/chemistry ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; Enzyme Inhibitors/chemical synthesis ; Enzyme Inhibitors/chemistry ; Humans ; Isoenzymes/antagonists & inhibitors ; Isoenzymes/metabolism ; MCF-7 Cells ; Molecular Structure ; Structure-Activity Relationship ; Thioredoxin-Disulfide Reductase/metabolism ; Tumor Cells, Cultured
Czasopismo naukowe
Tytuł :
Inhibition of SARS-CoV 3CL protease by flavonoids.
Autorzy :
Jo S; College of Pharmacy and Graduates School of Pharmaceutical Sciences, Ewha W. University, Seoul, Republic of Korea.
Kim S; College of Pharmacy and Graduates School of Pharmaceutical Sciences, Ewha W. University, Seoul, Republic of Korea.
Shin DH; College of Pharmacy and Graduates School of Pharmaceutical Sciences, Ewha W. University, Seoul, Republic of Korea.
Kim MS; College of Pharmacy and Graduates School of Pharmaceutical Sciences, Ewha W. University, Seoul, Republic of Korea.
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Źródło :
Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2020 Dec; Vol. 35 (1), pp. 145-151.
Typ publikacji :
Journal Article
MeSH Terms :
Antiviral Agents/*pharmacology
Enzyme Inhibitors/*pharmacology
Flavonoids/*pharmacology
SARS Virus/*drug effects
Viral Proteins/*antagonists & inhibitors
Antiviral Agents/chemical synthesis ; Antiviral Agents/chemistry ; Coronavirus 3C Proteases ; Cysteine Endopeptidases/isolation & purification ; Cysteine Endopeptidases/metabolism ; Dose-Response Relationship, Drug ; Enzyme Inhibitors/chemical synthesis ; Enzyme Inhibitors/chemistry ; Flavonoids/chemical synthesis ; Flavonoids/chemistry ; Humans ; Molecular Structure ; SARS Virus/enzymology ; Structure-Activity Relationship ; Viral Proteins/isolation & purification ; Viral Proteins/metabolism
Czasopismo naukowe

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