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


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Tytuł :
Half-Life Defined as the Time Until Half of the Log Titer Is Not Informative and Should Be Replaced With Segments: Comment on Hirose et al, 2020.
Autorzy :
Gracely EJ; College of Medicine and Dornsife School of Public Health, Drexel University, Philadelphia, Pennsylvania, USA.
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Źródło :
Clinical infectious diseases : an official publication of the Infectious Diseases Society of America [Clin Infect Dis] 2021 Aug 02; Vol. 73 (3), pp. e853-e854.
Typ publikacji :
Letter; Comment
MeSH Terms :
Half-Life*
Humans
Opinia redakcyjna
Tytuł :
The Effect of Mitochondrial DNA Half-Life on Deletion Mutation Proliferation in Long Lived Cells.
Autorzy :
Holt AG; Malmesbury, Wiltshire, UK.
Davies AM; Shrewsbury, Shropshire, UK. .
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Źródło :
Acta biotheoretica [Acta Biotheor] 2021 Dec; Vol. 69 (4), pp. 671-695. Date of Electronic Publication: 2021 Jun 15.
Typ publikacji :
Journal Article
MeSH Terms :
DNA, Mitochondrial*/genetics
Ecosystem*
Cell Proliferation ; Computer Simulation ; Half-Life ; Mitochondria/genetics ; Sequence Deletion/genetics
Czasopismo naukowe
Tytuł :
Improvement of stability and in vivo antioxidant effect of human glutathione peroxidase mutant by PEGylation.
Autorzy :
Wang Y; College of Pharmaceutical Science, Jilin University, Changchun 130021, China.
Niu S; College of Pharmaceutical Science, Jilin University, Changchun 130021, China.
Li B; College of Pharmaceutical Science, Jilin University, Changchun 130021, China.
Yan Q; College of Pharmaceutical Science, Jilin University, Changchun 130021, China.
Zhao Y; College of Agriculture and Environmental Science, University of California Davis, Davis, CA 95616, United States.
Wang Z; College of Pharmaceutical Science, Jilin University, Changchun 130021, China.
Xiong C; College of Pharmaceutical Science, Jilin University, Changchun 130021, China.
Wei J; College of Pharmaceutical Science, Jilin University, Changchun 130021, China; Key Laboratory for Molecular Enzymology and Engineering of the Ministry of Education, Jilin University, Changchun 130000, China. Electronic address: .
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Źródło :
International journal of pharmaceutics [Int J Pharm] 2021 Nov 20; Vol. 609, pp. 121152. Date of Electronic Publication: 2021 Oct 07.
Typ publikacji :
Journal Article
MeSH Terms :
Antioxidants*
Polyethylene Glycols*
Animals ; Glutathione Peroxidase/genetics ; Half-Life ; Humans ; Recombinant Proteins/genetics ; Succinic Acid
Czasopismo naukowe
Tytuł :
Dinitrophenol-mediated modulation of an anti-PD-L1 VHH for Fc-dependent effector functions and prolonged serum half-life.
Autorzy :
Liu J; Key Laboratory of Carbohydrate Chemistry & Biotechnology, Ministry of Education, School of Biotechnology, Jiangnan University, Wuxi 214122, China.
Hong H; Key Laboratory of Carbohydrate Chemistry & Biotechnology, Ministry of Education, School of Biotechnology, Jiangnan University, Wuxi 214122, China.
Shi J; Key Laboratory of Carbohydrate Chemistry & Biotechnology, Ministry of Education, School of Biotechnology, Jiangnan University, Wuxi 214122, China. Electronic address: .
Xie Y; Key Laboratory of Carbohydrate Chemistry & Biotechnology, Ministry of Education, School of Biotechnology, Jiangnan University, Wuxi 214122, China.
Lu Z; Key Laboratory of Carbohydrate Chemistry & Biotechnology, Ministry of Education, School of Biotechnology, Jiangnan University, Wuxi 214122, China.
Liu Z; Key Laboratory of Carbohydrate Chemistry & Biotechnology, Ministry of Education, School of Biotechnology, Jiangnan University, Wuxi 214122, China.
Zhou Z; Key Laboratory of Carbohydrate Chemistry & Biotechnology, Ministry of Education, School of Biotechnology, Jiangnan University, Wuxi 214122, China.
Bian Z; Wuxi Cancer Institute, Affiliated Hospital of Jiangnan University, Wuxi, Jiangsu 214122, China.
Huang Z; Wuxi Cancer Institute, Affiliated Hospital of Jiangnan University, Wuxi, Jiangsu 214122, China. Electronic address: .
Wu Z; Key Laboratory of Carbohydrate Chemistry & Biotechnology, Ministry of Education, School of Biotechnology, Jiangnan University, Wuxi 214122, China. Electronic address: .
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Źródło :
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences [Eur J Pharm Sci] 2021 Oct 01; Vol. 165, pp. 105941. Date of Electronic Publication: 2021 Jul 10.
Typ publikacji :
Journal Article
MeSH Terms :
B7-H1 Antigen*
Neoplasms*/drug therapy
Dinitrophenols ; Half-Life ; Humans ; Immunotherapy
Czasopismo naukowe
Tytuł :
Formulation, characterization, optimization, and in-vivo performance of febuxostat self-nano-emulsifying system loaded sublingual films.
Autorzy :
Habib BA; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
Abd El-Samiae AS; Department of Pharmaceutics, National Organization for Drug Control and Research (NODCAR), Giza, Egypt.
El-Houssieny BM; Department of Pharmaceutics, National Organization for Drug Control and Research (NODCAR), Giza, Egypt.
Tag R; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
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Źródło :
Drug delivery [Drug Deliv] 2021 Dec; Vol. 28 (1), pp. 1321-1333.
Typ publikacji :
Journal Article
MeSH Terms :
Drug Carriers/*chemistry
Febuxostat/*pharmacokinetics
Gout Suppressants/*pharmacokinetics
Nanoparticles/*chemistry
Animals ; Area Under Curve ; Chemistry, Pharmaceutical ; Cross-Over Studies ; Drug Liberation ; Drug Stability ; Emulsions ; Febuxostat/administration & dosage ; Gout Suppressants/administration & dosage ; Half-Life ; Particle Size ; Rabbits ; Sheep ; Solubility ; Surface-Active Agents/chemistry
Czasopismo naukowe
Tytuł :
Pharmacokinetic interaction between peimine and paeoniflorin in rats and its potential mechanism.
Autorzy :
Chen Q; Department of Thyroid and Breast Surgery, Weifang Yidu Central Hospital, Weifang, Shandong, 262500, China.
Yin C; Department of Pediatrics, Weifang Yidu Central Hospital, Weifang, China.
Li Y; Department of Pediatrics, Weifang Yidu Central Hospital, Weifang, China.
Yang Z; Qingzhou Medical Security Bureau, Weifang, China.
Tian Z; Department of Human Anatomy, School of Basic Medical Sciences, Hubei University of Medicine, Shiyan, China.
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Źródło :
Pharmaceutical biology [Pharm Biol] 2021 Dec; Vol. 59 (1), pp. 129-133.
Typ publikacji :
Journal Article
MeSH Terms :
Cevanes/*pharmacology
Glucosides/*pharmacokinetics
Microsomes, Liver/*metabolism
Monoterpenes/*pharmacokinetics
ATP Binding Cassette Transporter, Subfamily B, Member 1/metabolism ; Animals ; Area Under Curve ; Caco-2 Cells ; Cevanes/administration & dosage ; Cytochrome P-450 CYP3A/metabolism ; Drug Interactions ; Glucosides/administration & dosage ; Half-Life ; Humans ; Male ; Monoterpenes/administration & dosage ; Rats ; Rats, Sprague-Dawley
Czasopismo naukowe
Tytuł :
Inhalation delivery dramatically improves the efficacy of topotecan for the treatment of local and distant lung cancer.
Autorzy :
Kuehl PJ; Lung Cancer Program, Lovelace Respiratory Research Institute, Albuquerque, NM, USA.
Yingling CM; Lung Cancer Program, Lovelace Respiratory Research Institute, Albuquerque, NM, USA.
Dubose D; Lonza-Bend Research Institute, Bend, OR, USA.
Burke M; Lonza-Bend Research Institute, Bend, OR, USA.
Revelli DA; Lung Cancer Program, Lovelace Respiratory Research Institute, Albuquerque, NM, USA.
Chen W; Lung Cancer Program, Lovelace Respiratory Research Institute, Albuquerque, NM, USA.
Dye WW; Lung Cancer Program, Lovelace Respiratory Research Institute, Albuquerque, NM, USA.
Belinsky SA; Lung Cancer Program, Lovelace Respiratory Research Institute, Albuquerque, NM, USA.
Tessema M; Lung Cancer Program, Lovelace Respiratory Research Institute, Albuquerque, NM, USA.
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Źródło :
Drug delivery [Drug Deliv] 2021 Dec; Vol. 28 (1), pp. 767-775.
Typ publikacji :
Journal Article
MeSH Terms :
Lung Neoplasms/*drug therapy
Topoisomerase I Inhibitors/*pharmacology
Topotecan/*pharmacology
Administration, Inhalation ; Animals ; Antineoplastic Combined Chemotherapy Protocols ; Cell Line, Tumor ; Chemistry, Pharmaceutical ; Genes, erbB-1/genetics ; Half-Life ; Humans ; Metabolic Clearance Rate ; Proto-Oncogene Proteins p21(ras)/genetics ; Rats ; Rats, Sprague-Dawley ; Topoisomerase I Inhibitors/administration & dosage ; Topoisomerase I Inhibitors/pharmacokinetics ; Topotecan/administration & dosage ; Topotecan/pharmacokinetics ; Tumor Burden ; Xenograft Model Antitumor Assays
Czasopismo naukowe
Tytuł :
Efficient Discovery of Visible Light-Activated Azoarene Photoswitches with Long Half-Lives Using Active Search.
Autorzy :
Mukadum F; Department of Chemistry and Chemical Biology, Northeastern University, Boston, Massachusetts 02115, United States.
Nguyen Q; Department of Computer Science and Engineering, Washington University in St. Louis, St. Louis, Missouri 63130, United States.
Adrion DM; Department of Chemistry and Chemical Biology, Northeastern University, Boston, Massachusetts 02115, United States.
Appleby G; Department of Computer Science, Tufts University, Medford, Massachusetts 02155, United States.
Chen R; Department of Computer Science, Tufts University, Medford, Massachusetts 02155, United States.
Dang H; Department of Chemistry and Chemical Biology, Northeastern University, Boston, Massachusetts 02115, United States.
Chang R; Department of Computer Science, Tufts University, Medford, Massachusetts 02155, United States.
Garnett R; Department of Computer Science and Engineering, Washington University in St. Louis, St. Louis, Missouri 63130, United States.
Lopez SA; Department of Chemistry and Chemical Biology, Northeastern University, Boston, Massachusetts 02115, United States.
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Źródło :
Journal of chemical information and modeling [J Chem Inf Model] 2021 Nov 22; Vol. 61 (11), pp. 5524-5534. Date of Electronic Publication: 2021 Nov 09.
Typ publikacji :
Journal Article; Research Support, U.S. Gov't, Non-P.H.S.
MeSH Terms :
Light*
Catalysis ; Half-Life ; Isomerism
Czasopismo naukowe
Tytuł :
Development of a selective matrix metalloproteinase 13 (MMP-13) inhibitor for the treatment of Osteoarthritis.
Autorzy :
Bendele AM; BolderBioPath, Inc., 5541 Central Avenue, Suite 160, Boulder, CO, 80301, USA.
Neelagiri M; Aquilus Pharmaceuticals Inc., 400 West Cummings Park, Woburn, MA, 01801, USA.
Neelagiri V; Aquilus Pharmaceuticals Inc., 400 West Cummings Park, Woburn, MA, 01801, USA.
Sucholeiki I; Aquilus Pharmaceuticals Inc., 400 West Cummings Park, Woburn, MA, 01801, USA. Electronic address: .
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Źródło :
European journal of medicinal chemistry [Eur J Med Chem] 2021 Nov 15; Vol. 224, pp. 113666. Date of Electronic Publication: 2021 Jun 29.
Typ publikacji :
Journal Article
MeSH Terms :
Matrix Metalloproteinase 13/*chemistry
Matrix Metalloproteinase Inhibitors/*therapeutic use
Osteoarthritis/*drug therapy
Amides/chemistry ; Amides/metabolism ; Amides/therapeutic use ; Animals ; Disease Models, Animal ; Half-Life ; Humans ; Isoenzymes/antagonists & inhibitors ; Isoenzymes/metabolism ; Joints/pathology ; Matrix Metalloproteinase 13/metabolism ; Matrix Metalloproteinase Inhibitors/chemistry ; Matrix Metalloproteinase Inhibitors/pharmacokinetics ; Osteoarthritis/chemically induced ; Osteoarthritis/pathology ; Pyrimidines/chemistry ; Rats ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł :
Discovery and characterization of novel peptide inhibitors of the NRF2/MAFG/DNA ternary complex for the treatment of cancer.
Autorzy :
Simov V; Merck & Co., Inc., Chemistry, 33 Avenue Louis Pasteur, Boston, MA 02127, USA. Electronic address: .
Altman MD; Merck & Co., Inc., Chemistry, 33 Avenue Louis Pasteur, Boston, MA 02127, USA.
Bianchi E; Peptides and Small Molecules R&D, IRBM, Via Pontina, 30,600, 00071 Pomezia RM, Italy.
DelRizzo S; Peptides and Small Molecules R&D, IRBM, Via Pontina, 30,600, 00071 Pomezia RM, Italy.
DiNunzio EN; Merck & Co., Inc., Chemistry, 2000 Galloping Hill Road, K-15, Kenilworth, NJ 07033, USA.
Feng G; Merck & Co., Inc., Quantitative Biosciences, 33 Avenue Louis Pasteur, Boston, MA 02127, USA.
Goldenblatt P; Merck & Co., Inc., Quantitative Biosciences, 33 Avenue Louis Pasteur, Boston, MA 02127, USA.
Ingenito R; Peptides and Small Molecules R&D, IRBM, Via Pontina, 30,600, 00071 Pomezia RM, Italy.
Johnson SA; Merck & Co., Inc., Chemistry, 33 Avenue Louis Pasteur, Boston, MA 02127, USA.
Mansueto MS; Merck & Co., Inc., Quantitative Biosciences, 33 Avenue Louis Pasteur, Boston, MA 02127, USA.
Mayhood T; Merck & Co., Inc., Chemistry, 2000 Galloping Hill Road, K-15, Kenilworth, NJ 07033, USA.
Mortison JD; Merck & Co., Inc., Chemistry, 33 Avenue Louis Pasteur, Boston, MA 02127, USA.
Serebrov V; Merck & Co., Inc., Quantitative Biosciences, 33 Avenue Louis Pasteur, Boston, MA 02127, USA.
Sondey C; Merck & Co., Inc., Quantitative Biosciences, 33 Avenue Louis Pasteur, Boston, MA 02127, USA.
Sriraman V; Merck & Co., Inc., Quantitative Biosciences, 33 Avenue Louis Pasteur, Boston, MA 02127, USA.
Tucker TJ; Merck & Co., Inc., Chemistry, 770 Sumneytown Pike, West Point, PA 19486, USA.
Walji A; Merck & Co., Inc., Chemistry, 770 Sumneytown Pike, West Point, PA 19486, USA.
Wan H; Merck & Co., Inc., PPDM, 126 East Lincoln Avenue, Rahway, NJ 07065, USA.
Yue Y; Merck & Co., Inc., Biology, 33 Avenue Louis Pasteur, Boston, MA 02127, USA.
Stoeck A; Merck & Co., Inc., Biology, 33 Avenue Louis Pasteur, Boston, MA 02127, USA.
DiMauro EF; Merck & Co., Inc., Chemistry, 33 Avenue Louis Pasteur, Boston, MA 02127, USA.
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Źródło :
European journal of medicinal chemistry [Eur J Med Chem] 2021 Nov 15; Vol. 224, pp. 113686. Date of Electronic Publication: 2021 Jul 07.
Typ publikacji :
Journal Article
MeSH Terms :
DNA/*chemistry
MafG Transcription Factor/*antagonists & inhibitors
NF-E2-Related Factor 2/*antagonists & inhibitors
Peptides/*chemistry
Antioxidant Response Elements/drug effects ; DNA/metabolism ; Drug Design ; Drug Stability ; Electrophoretic Mobility Shift Assay ; Half-Life ; HeLa Cells ; Humans ; MafG Transcription Factor/metabolism ; NF-E2-Related Factor 2/metabolism ; Neoplasms/drug therapy ; Neoplasms/pathology ; Peptides/metabolism ; Peptides/pharmacology ; Peptides/therapeutic use ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł :
Design and synthesis of novel orally selective and type II pan-TRK inhibitors to overcome mutations by property-driven optimization.
Autorzy :
Li MC; Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, No. 35, Keyan Road, Zhunan Town, Miaoli County, 350401, Taiwan, ROC; Department of Chemistry, National Tsing Hua University, No. 101, Sec. 2, Kuang-Fu Road, Hsinchu, 300044, Taiwan, ROC; Biomedical Translation Research Center, Academia Sinica, No. 99, Ln. 130, Sec. 1, Academia Road, Taipei City, 115202, Taiwan, ROC.
Lin WH; Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, No. 35, Keyan Road, Zhunan Town, Miaoli County, 350401, Taiwan, ROC.
Wang PC; Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, No. 35, Keyan Road, Zhunan Town, Miaoli County, 350401, Taiwan, ROC.
Su YC; Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, No. 35, Keyan Road, Zhunan Town, Miaoli County, 350401, Taiwan, ROC.
Chen PY; Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, No. 35, Keyan Road, Zhunan Town, Miaoli County, 350401, Taiwan, ROC.
Fan CM; Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, No. 35, Keyan Road, Zhunan Town, Miaoli County, 350401, Taiwan, ROC.
Chen CP; Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, No. 35, Keyan Road, Zhunan Town, Miaoli County, 350401, Taiwan, ROC.
Huang CL; Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, No. 35, Keyan Road, Zhunan Town, Miaoli County, 350401, Taiwan, ROC.
Chiu CH; Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, No. 35, Keyan Road, Zhunan Town, Miaoli County, 350401, Taiwan, ROC.
Chang L; Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, No. 35, Keyan Road, Zhunan Town, Miaoli County, 350401, Taiwan, ROC.
Chen CT; Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, No. 35, Keyan Road, Zhunan Town, Miaoli County, 350401, Taiwan, ROC.
Yeh TK; Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, No. 35, Keyan Road, Zhunan Town, Miaoli County, 350401, Taiwan, ROC.
Hsieh HP; Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, No. 35, Keyan Road, Zhunan Town, Miaoli County, 350401, Taiwan, ROC; Department of Chemistry, National Tsing Hua University, No. 101, Sec. 2, Kuang-Fu Road, Hsinchu, 300044, Taiwan, ROC; Biomedical Translation Research Center, Academia Sinica, No. 99, Ln. 130, Sec. 1, Academia Road, Taipei City, 115202, Taiwan, ROC. Electronic address: .
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Źródło :
European journal of medicinal chemistry [Eur J Med Chem] 2021 Nov 15; Vol. 224, pp. 113673. Date of Electronic Publication: 2021 Jun 29.
Typ publikacji :
Journal Article
MeSH Terms :
Drug Design*
Protein Kinase Inhibitors/*chemistry
Receptor, trkA/*antagonists & inhibitors
Administration, Oral ; Animals ; Aurora Kinase A/antagonists & inhibitors ; Aurora Kinase A/metabolism ; Aurora Kinase B/antagonists & inhibitors ; Aurora Kinase B/metabolism ; Binding Sites ; Cell Line, Tumor ; Half-Life ; Humans ; Mice ; Mice, Nude ; Molecular Docking Simulation ; Neoplasms/drug therapy ; Neoplasms/pathology ; Protein Kinase Inhibitors/metabolism ; Protein Kinase Inhibitors/therapeutic use ; Rats ; Receptor, trkA/metabolism ; Structure-Activity Relationship ; Transplantation, Heterologous
Czasopismo naukowe
Tytuł :
Synthesis and evaluation of FAK inhibitors with a 5-fluoro-7H-pyrrolo[2,3-d]pyrimidine scaffold as anti-hepatocellular carcinoma agents.
Autorzy :
Tan H; Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai, 201203, China.
Liu Y; Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai, 201203, China.
Gong C; Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai, 201203, China.
Zhang J; Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai, 201203, China.
Huang J; Key Laboratory of Systems Biomedicine (Ministry of Education), Shanghai Centre for Systems Biomedicine, Shanghai Jiao Tong University, Shanghai, 200240, China. Electronic address: .
Zhang Q; Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai, 201203, China. Electronic address: .
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Źródło :
European journal of medicinal chemistry [Eur J Med Chem] 2021 Nov 05; Vol. 223, pp. 113670. Date of Electronic Publication: 2021 Jun 25.
Typ publikacji :
Journal Article
MeSH Terms :
Focal Adhesion Protein-Tyrosine Kinases/*antagonists & inhibitors
Protein Kinase Inhibitors/*chemical synthesis
Pyrimidines/*chemistry
Pyrroles/*chemistry
Animals ; Binding Sites ; Carcinoma, Hepatocellular/drug therapy ; Carcinoma, Hepatocellular/pathology ; Catalytic Domain ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Focal Adhesion Protein-Tyrosine Kinases/metabolism ; Half-Life ; Humans ; Liver Neoplasms/drug therapy ; Liver Neoplasms/pathology ; Male ; Mice ; Mice, Nude ; Molecular Docking Simulation ; Protein Kinase Inhibitors/metabolism ; Protein Kinase Inhibitors/pharmacology ; Protein Kinase Inhibitors/therapeutic use ; Pyrimidines/metabolism ; Pyrimidines/pharmacology ; Pyrimidines/therapeutic use ; Pyrroles/metabolism ; Pyrroles/pharmacology ; Pyrroles/therapeutic use ; Small Molecule Libraries/chemistry ; Small Molecule Libraries/metabolism ; Small Molecule Libraries/pharmacology ; Small Molecule Libraries/therapeutic use ; Structure-Activity Relationship ; Transplantation, Heterologous
Czasopismo naukowe
Tytuł :
Synthesis and biological evaluation of 1-(4-(piperazin-1-yl)phenyl)pyridin-2(1H)-one derivatives as potential SSRIs.
Autorzy :
Xu T; Sunshine Lake Pharma Co. Ltd., Shenzhen, 518000, PR China; HEC Pharm Group, HEC Research and Development Center, Dongguan 523871, PR China.
Xue Y; Sunshine Lake Pharma Co. Ltd., Shenzhen, 518000, PR China; HEC Pharm Group, HEC Research and Development Center, Dongguan 523871, PR China.
Lu J; Sunshine Lake Pharma Co. Ltd., Shenzhen, 518000, PR China; HEC Pharm Group, HEC Research and Development Center, Dongguan 523871, PR China.
Jin C; Sunshine Lake Pharma Co. Ltd., Shenzhen, 518000, PR China; HEC Pharm Group, HEC Research and Development Center, Dongguan 523871, PR China. Electronic address: .
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Źródło :
European journal of medicinal chemistry [Eur J Med Chem] 2021 Nov 05; Vol. 223, pp. 113644. Date of Electronic Publication: 2021 Jun 15.
Typ publikacji :
Journal Article
MeSH Terms :
Antidepressive Agents/*chemistry
Pyridones/*chemistry
Serotonin Uptake Inhibitors/*chemical synthesis
Animals ; Antidepressive Agents/metabolism ; Antidepressive Agents/pharmacology ; Drug Stability ; Half-Life ; Humans ; Hypothalamus/drug effects ; Hypothalamus/metabolism ; Maze Learning/drug effects ; Microsomes, Liver/metabolism ; Piperazine/chemistry ; Pyridones/metabolism ; Pyridones/pharmacology ; Rats ; Rats, Sprague-Dawley ; Serotonin/metabolism ; Serotonin Uptake Inhibitors/metabolism ; Serotonin Uptake Inhibitors/pharmacology ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł :
Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation.
Autorzy :
Yang C; Shanghai Key Laboratory of Molecular Catalysis and Innovative Materials, Department of Chemistry, Fudan University, Shanghai, 200433, China.
Xu C; Department of Pathology, School of Basic Medical Sciences, Fudan University, Shanghai, 200032, China.
Li Z; Shanghai Key Laboratory of Molecular Catalysis and Innovative Materials, Department of Chemistry, Fudan University, Shanghai, 200433, China.
Chen Y; Shanghai Key Laboratory of Molecular Catalysis and Innovative Materials, Department of Chemistry, Fudan University, Shanghai, 200433, China.
Wu T; Shanghai Key Laboratory of Molecular Catalysis and Innovative Materials, Department of Chemistry, Fudan University, Shanghai, 200433, China.
Hong H; Lyrae Therapeutics, L.L.C., Shanghai, 200438, China.
Lu M; Shanghai Key Laboratory of Molecular Catalysis and Innovative Materials, Department of Chemistry, Fudan University, Shanghai, 200433, China.
Jia Y; Shanghai Key Laboratory of Molecular Catalysis and Innovative Materials, Department of Chemistry, Fudan University, Shanghai, 200433, China.
Yang Y; Shanghai Key Laboratory of Molecular Catalysis and Innovative Materials, Department of Chemistry, Fudan University, Shanghai, 200433, China.
Liu X; Shanghai Key Laboratory of Molecular Catalysis and Innovative Materials, Department of Chemistry, Fudan University, Shanghai, 200433, China.
Deng M; Shanghai Key Laboratory of Molecular Catalysis and Innovative Materials, Department of Chemistry, Fudan University, Shanghai, 200433, China.
Chen Z; Shanghai Key Laboratory of Molecular Catalysis and Innovative Materials, Department of Chemistry, Fudan University, Shanghai, 200433, China.
Li Q; Department of Pathology, School of Basic Medical Sciences, Fudan University, Shanghai, 200032, China. Electronic address: .
Ling Y; Shanghai Key Laboratory of Molecular Catalysis and Innovative Materials, Department of Chemistry, Fudan University, Shanghai, 200433, China; Zhuhai-Fudan Innovation Institute, Zhuhai, Guangdong, 519000, China. Electronic address: .
Zhou Y; Shanghai Key Laboratory of Molecular Catalysis and Innovative Materials, Department of Chemistry, Fudan University, Shanghai, 200433, China. Electronic address: .
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Źródło :
European journal of medicinal chemistry [Eur J Med Chem] 2021 Nov 05; Vol. 223, pp. 113661. Date of Electronic Publication: 2021 Jun 21.
Typ publikacji :
Journal Article
MeSH Terms :
Drug Design*
Class I Phosphatidylinositol 3-Kinases/*antagonists & inhibitors
Indoles/*chemistry
Phosphoinositide-3 Kinase Inhibitors/*chemical synthesis
Animals ; Binding Sites ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Class I Phosphatidylinositol 3-Kinases/metabolism ; G1 Phase Cell Cycle Checkpoints/drug effects ; Half-Life ; Humans ; Indoles/metabolism ; Indoles/pharmacology ; Indoles/therapeutic use ; Leukemia, Myeloid, Acute/drug therapy ; Leukemia, Myeloid, Acute/pathology ; Mice ; Mice, Nude ; Molecular Docking Simulation ; Phosphoinositide-3 Kinase Inhibitors/metabolism ; Phosphoinositide-3 Kinase Inhibitors/pharmacology ; Phosphoinositide-3 Kinase Inhibitors/therapeutic use ; Proto-Oncogene Proteins c-akt/genetics ; Proto-Oncogene Proteins c-akt/metabolism ; Rats ; Rats, Sprague-Dawley ; Structure-Activity Relationship ; Transplantation, Heterologous
Czasopismo naukowe
Tytuł :
Discovery of novel nitrogenous heterocyclic-containing quinoxaline-1,4-di-N-oxides as potent activator of autophagy in M.tb-infected macrophages.
Autorzy :
Zhang H; National Reference Laboratory of Veterinary Drug Residues and MOA Key Laboratory for Detection of Veterinary Drug Residues, Wuhan, Hubei, 430070, China; MOA Laboratory for Risk Assessment of Quality and Safety of Livestock and Poultry Products, Huazhong Agricultural University, Wuhan, Hubei, 430070, China.
Lu Q; National Reference Laboratory of Veterinary Drug Residues and MOA Key Laboratory for Detection of Veterinary Drug Residues, Wuhan, Hubei, 430070, China.
Zhang J; National Reference Laboratory of Veterinary Drug Residues and MOA Key Laboratory for Detection of Veterinary Drug Residues, Wuhan, Hubei, 430070, China; MOA Laboratory for Risk Assessment of Quality and Safety of Livestock and Poultry Products, Huazhong Agricultural University, Wuhan, Hubei, 430070, China.
Qu W; National Reference Laboratory of Veterinary Drug Residues and MOA Key Laboratory for Detection of Veterinary Drug Residues, Wuhan, Hubei, 430070, China.
Xie S; MOA Laboratory for Risk Assessment of Quality and Safety of Livestock and Poultry Products, Huazhong Agricultural University, Wuhan, Hubei, 430070, China.
Huang L; National Reference Laboratory of Veterinary Drug Residues and MOA Key Laboratory for Detection of Veterinary Drug Residues, Wuhan, Hubei, 430070, China; MOA Laboratory for Risk Assessment of Quality and Safety of Livestock and Poultry Products, Huazhong Agricultural University, Wuhan, Hubei, 430070, China.
Yuan Z; National Reference Laboratory of Veterinary Drug Residues and MOA Key Laboratory for Detection of Veterinary Drug Residues, Wuhan, Hubei, 430070, China; MOA Laboratory for Risk Assessment of Quality and Safety of Livestock and Poultry Products, Huazhong Agricultural University, Wuhan, Hubei, 430070, China.
Pan Y; National Reference Laboratory of Veterinary Drug Residues and MOA Key Laboratory for Detection of Veterinary Drug Residues, Wuhan, Hubei, 430070, China; MOA Laboratory for Risk Assessment of Quality and Safety of Livestock and Poultry Products, Huazhong Agricultural University, Wuhan, Hubei, 430070, China. Electronic address: .
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Źródło :
European journal of medicinal chemistry [Eur J Med Chem] 2021 Nov 05; Vol. 223, pp. 113657. Date of Electronic Publication: 2021 Jun 17.
Typ publikacji :
Journal Article
MeSH Terms :
Antitubercular Agents/*pharmacology
Autophagy/*drug effects
Macrophages/*microbiology
Mycobacterium tuberculosis/*drug effects
Quinoxalines/*chemistry
Animals ; Antitubercular Agents/chemistry ; Antitubercular Agents/pharmacokinetics ; Cell Survival/drug effects ; Chlorocebus aethiops ; Drug Evaluation, Preclinical ; Half-Life ; Microbial Sensitivity Tests ; Mitochondria/drug effects ; Mitochondria/metabolism ; Mycobacterium tuberculosis/physiology ; Oxides/chemistry ; Quinoxalines/pharmacokinetics ; Quinoxalines/pharmacology ; Rats ; Reactive Oxygen Species/metabolism ; Structure-Activity Relationship ; Vero Cells
Czasopismo naukowe
Tytuł :
Structure-guided design and development of novel N-phenylpyrimidin-2-amine derivatives as potential c-Met inhibitors.
Autorzy :
Huang D; School of Chemical and Pharmaceutical Engineering, Hebei University of Science and Technology, Shijiazhuang, 050018, China.
Yang J; School of Pharmacy, Hebei University of Chinese Medicine, Shijiazhuang, 050018, China.
Zhang Q; Novel Technology Center of Pharmaceutical Chemistry, Shanghai Institute of Pharmaceutical Industry, Shanghai, 201203, China; Shanghai Engineering Research Center of Pharmaceutical Process, Shanghai, 201203, China.
Wang G; Novel Technology Center of Pharmaceutical Chemistry, Shanghai Institute of Pharmaceutical Industry, Shanghai, 201203, China; Shanghai Engineering Research Center of Pharmaceutical Process, Shanghai, 201203, China.
Zhang Z; Novel Technology Center of Pharmaceutical Chemistry, Shanghai Institute of Pharmaceutical Industry, Shanghai, 201203, China; Shanghai Engineering Research Center of Pharmaceutical Process, Shanghai, 201203, China.
Zhang Y; School of Chemical and Pharmaceutical Engineering, Hebei University of Science and Technology, Shijiazhuang, 050018, China. Electronic address: .
Li J; Novel Technology Center of Pharmaceutical Chemistry, Shanghai Institute of Pharmaceutical Industry, Shanghai, 201203, China; Shanghai Engineering Research Center of Pharmaceutical Process, Shanghai, 201203, China. Electronic address: .
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Źródło :
European journal of medicinal chemistry [Eur J Med Chem] 2021 Nov 05; Vol. 223, pp. 113648. Date of Electronic Publication: 2021 Jun 17.
Typ publikacji :
Journal Article
MeSH Terms :
Drug Design*
Amines/*chemistry
Protein Kinase Inhibitors/*chemistry
Proto-Oncogene Proteins c-met/*antagonists & inhibitors
Amines/metabolism ; Amines/pharmacology ; Animals ; Binding Sites ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Drug Screening Assays, Antitumor ; Female ; Half-Life ; Humans ; Male ; Mice ; Molecular Docking Simulation ; Protein Kinase Inhibitors/metabolism ; Protein Kinase Inhibitors/pharmacology ; Proto-Oncogene Proteins c-met/metabolism ; Rats ; Rats, Sprague-Dawley ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł :
Si113-prodrugs selectively activated by plasmin against hepatocellular and ovarian carcinoma.
Autorzy :
Rango E; Dipartimento di Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena, Via Aldo Moro 2, 53100, Siena, Italy.
D'Antona L; Dipartimento di Scienze della Salute, Università'Magna Graecia' di Catanzaro, Viale Europa, 88100, Catanzaro, Italy.
Iovenitti G; Dipartimento di Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena, Via Aldo Moro 2, 53100, Siena, Italy.
Brai A; Dipartimento di Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena, Via Aldo Moro 2, 53100, Siena, Italy.
Mancini A; Dipartimento di Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena, Via Aldo Moro 2, 53100, Siena, Italy.
Zamperini C; Lead Discovery Siena S.r.l., Via Vittorio Alfieri 31, 53019, Castelnuovo Berardenga, Siena, Italy.
Trivisani CI; Dipartimento di Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena, Via Aldo Moro 2, 53100, Siena, Italy.
Marianelli S; Dipartimento di Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena, Via Aldo Moro 2, 53100, Siena, Italy.
Fallacara AL; Dipartimento di Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena, Via Aldo Moro 2, 53100, Siena, Italy.
Molinari A; Dipartimento di Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena, Via Aldo Moro 2, 53100, Siena, Italy.
Cianciusi A; Dipartimento di Farmacia, Università degli Studi di Genova, Viale Benedetto XV 3, Genoa, 16132, Italy.
Schenone S; Dipartimento di Farmacia, Università degli Studi di Genova, Viale Benedetto XV 3, Genoa, 16132, Italy.
Perrotti N; Dipartimento di Scienze della Salute, Università'Magna Graecia' di Catanzaro, Viale Europa, 88100, Catanzaro, Italy. Electronic address: .
Dreassi E; Dipartimento di Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena, Via Aldo Moro 2, 53100, Siena, Italy. Electronic address: .
Botta M; Dipartimento di Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena, Via Aldo Moro 2, 53100, Siena, Italy; Lead Discovery Siena S.r.l., Via Vittorio Alfieri 31, 53019, Castelnuovo Berardenga, Siena, Italy; Sbarro Institute for Cancer Research and Molecular Medicine, Center for Biotechnology, College of Science and Technology Temple University, BioLife Science Building, Suite 333, 1900 North 12th Street, Philadelphia, PA, 19122, United States.
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Źródło :
European journal of medicinal chemistry [Eur J Med Chem] 2021 Nov 05; Vol. 223, pp. 113653. Date of Electronic Publication: 2021 Jun 17.
Typ publikacji :
Journal Article
MeSH Terms :
Antineoplastic Agents/*therapeutic use
Carcinoma, Hepatocellular/*drug therapy
Fibrinolysin/*metabolism
Liver Neoplasms/*drug therapy
Ovarian Neoplasms/*drug therapy
Prodrugs/*metabolism
Pyrazoles/*therapeutic use
Pyrimidines/*therapeutic use
Animals ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/metabolism ; Antineoplastic Agents/pharmacology ; Carcinoma, Hepatocellular/pathology ; Cell Line, Tumor ; Cell Survival/drug effects ; Drug Resistance, Neoplasm/drug effects ; Drug Stability ; Female ; Half-Life ; Humans ; Immediate-Early Proteins/antagonists & inhibitors ; Immediate-Early Proteins/metabolism ; Liver Neoplasms/pathology ; Mice ; Mice, Nude ; Ovarian Neoplasms/pathology ; Paclitaxel/pharmacology ; Paclitaxel/therapeutic use ; Prodrugs/chemistry ; Prodrugs/pharmacology ; Prodrugs/therapeutic use ; Protein-Serine-Threonine Kinases/antagonists & inhibitors ; Protein-Serine-Threonine Kinases/metabolism ; Pyrazoles/chemistry ; Pyrazoles/metabolism ; Pyrazoles/pharmacology ; Pyrimidines/chemistry ; Pyrimidines/metabolism ; Pyrimidines/pharmacology ; Transplantation, Heterologous
Czasopismo naukowe
Tytuł :
Discovery of novel BCR-ABL PROTACs based on the cereblon E3 ligase design, synthesis, and biological evaluation.
Autorzy :
Liu H; School of Physical Science and Technology, ShanghaiTech University, Shanghai, 201210, China; Shanghai Institute for Advanced Immunochemical Studies, China; University of Chinese Academy of Sciences, Beijing, 100049, China.
Ding X; Shanghai Institute for Advanced Immunochemical Studies, China; School of Life Science and Technology, China; University of Chinese Academy of Sciences, Beijing, 100049, China.
Liu L; Hunan Provincial Key Laboratory of Tumor Microenvironment Responsive Drug Research, School of Pharmaceutical Science, University of South China, Hengyang City, 421001, China.
Mi Q; Shanghai Institute for Advanced Immunochemical Studies, China; School of Life Science and Technology, China.
Zhao Q; Shanghai Institute for Advanced Immunochemical Studies, China.
Shao Y; Department of Histology and Embryology, Anhui Medical University, Hefei, 230032, China.
Ren C; Shanghai Institute for Advanced Immunochemical Studies, China; School of Life Science and Technology, China.
Chen J; Shanghai Institute for Advanced Immunochemical Studies, China.
Kong Y; Shanghai Institute for Advanced Immunochemical Studies, China.
Qiu X; CAS Key Laboratory of Synthetic Chemistry of Natural Substances, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 345 Lingling Road, Shanghai, 200032, China.
Elvassore N; Shanghai Institute for Advanced Immunochemical Studies, China.
Yang X; Shanghai Institute for Advanced Immunochemical Studies, China. Electronic address: .
Yin Q; Shanghai Institute for Advanced Immunochemical Studies, China. Electronic address: .
Jiang B; Shanghai Institute for Advanced Immunochemical Studies, China; CAS Key Laboratory of Synthetic Chemistry of Natural Substances, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 345 Lingling Road, Shanghai, 200032, China. Electronic address: .
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Źródło :
European journal of medicinal chemistry [Eur J Med Chem] 2021 Nov 05; Vol. 223, pp. 113645. Date of Electronic Publication: 2021 Jun 25.
Typ publikacji :
Journal Article
MeSH Terms :
Drug Design*
Fusion Proteins, bcr-abl/*antagonists & inhibitors
Protein Kinase Inhibitors/*chemistry
Ubiquitin-Protein Ligases/*chemistry
Animals ; Cell Proliferation/drug effects ; Dasatinib/pharmacology ; Fusion Proteins, bcr-abl/metabolism ; Half-Life ; Humans ; K562 Cells ; Lenalidomide/chemistry ; Lenalidomide/metabolism ; Ligands ; Mice ; Neoplasms/drug therapy ; Protein Kinase Inhibitors/metabolism ; Protein Kinase Inhibitors/pharmacology ; Protein Kinase Inhibitors/therapeutic use ; Proteolysis ; Structure-Activity Relationship ; Thalidomide/analogs & derivatives ; Thalidomide/chemistry ; Thalidomide/metabolism ; Transplantation, Heterologous ; Ubiquitin-Protein Ligases/metabolism
Czasopismo naukowe
Tytuł :
Prophylaxis in children with haemophilia in an evolving treatment landscape.
Autorzy :
Mancuso ME; Centre for Thrombosis and Haemorrhagic Diseases, IRCCS Humanitas Research Hospital, Rozzano, Milan, Italy.
Male C; Thrombosis & Haemostasis Unit, Department of Paediatrics, Medical University of Vienna, Vienna, Austria.
Kenet G; The National Haemophilia Centre, The Amalia Biron Thrombosis Research Institute, Sheba Medical Centre, Tel Hashomer, Tel Aviv University, Tel Aviv, Israel.
Kavakli K; Department of Haematology, Ege University Faculty of Medicine, Children's Hospital, Bornova, Izmir, Turkey.
Königs C; Department of Paediatrics and Adolescent Medicine, Clinical and Molecular Haemostasis, University Hospital Frankfurt, Goethe University, Frankfurt, Germany.
Blatný J; Department of Paediatric Haematology and Biochemistry, University Hospital Brno and Masaryk University, Brno, Czech Republic.
Fijnvandraat K; Department of Paediatric Haematology, Emma Children's Hospital, Amsterdam UMC, University of Amsterdam, Amsterdam, Netherlands.
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Źródło :
Haemophilia : the official journal of the World Federation of Hemophilia [Haemophilia] 2021 Nov; Vol. 27 (6), pp. 889-896. Date of Electronic Publication: 2021 Sep 21.
Typ publikacji :
Journal Article; Review
MeSH Terms :
Hemophilia A*/drug therapy
Blood Coagulation Factors/therapeutic use ; Child ; Child, Preschool ; Factor VIII/therapeutic use ; Half-Life ; Hemorrhage ; Hormone Replacement Therapy ; Humans
Czasopismo naukowe

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