نتائج البحث - "Chau Almaden"

1

Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants with Selectivity over Wild-Type EGFR

المصدر: Journal of Medicinal Chemistry. 60:3002-3019

URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_________::b35c90cb7e71bbfee825479df1f470d5
https://doi.org/10.1021/acs.jmedchem.6b01894

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2

Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants

المؤلفون: Marlena Walls, Tod Smeal, Suvi T. M. Orr, Zhengyu Liu, Cheng Hengmiao, Shuiwang Wang, Kephart Susan Elizabeth, Jean Joo Matthews, Rose Ann Ferre, Neal W. Sach, Scott L. Weinrich, Doug Behenna, Sherry Niessen, Sangita M. Baxi, Deepak Dalvie, Sujin Cho-Schultz, Dac M. Dinh, Kevin Ryan, Jim Solowiej, Elaine E. Tseng, Simon Paul Planken, Sajiv Krishnan Nair, Brion W. Murray, Jun Li Feng, Jennifer Lafontaine, Pairish Mason Alan, Shijian Ren, Michelle Hemkens, Shuibo Xin, Mehran Jalaie, Tran Khanh Tuan, Robert Steven Kania, Sutton Scott Channing, William F. Vernier, Kevin K.-C. Liu, Amy Jackson-Fisher, Beth Lunney, Min-Jean Yin, Ketan S. Gajiwala, Asako Nagata, Haiwei Xu, Michael Zientek, Ru Zhou, Daniel Tyler Richter, Simon Bailey, Martin Paul Edwards, Martha A. Ornelas, Chau Almaden, John Charles Kath, Hong Shen, Theodore O. Johnson

المصدر: Journal of Medicinal Chemistry. 59:2005-2024

URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_________::dcd650965ee5ecc3e2b378a7f2542e1b
https://doi.org/10.1021/acs.jmedchem.5b01633

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3

Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants with Selectivity over Wild-Type EGFR

المصدر: Journal of medicinal chemistry. 60(7)

مصطلحات موضوعية: Models, Molecular, Acrylamides, Lung Neoplasms, Pyrrolidines, Halogenation, Rats, ErbB Receptors, Molecular Docking Simulation, Mice, Dogs, Carcinoma, Non-Small-Cell Lung, Cell Line, Tumor, Drug Design, Mutation, Animals, Humans, Lung, Protein Kinase Inhibitors

URL الوصول: https://explore.openaire.eu/search/publication?articleId=pmid________::424669cfffca599d5b525ea1e0d9fe2e
https://pubmed.ncbi.nlm.nih.gov/28287730

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4

Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants

المؤلفون: Hengmiao, Cheng, Sajiv K, Nair, Brion W, Murray, Chau, Almaden, Simon, Bailey, Sangita, Baxi, Doug, Behenna, Sujin, Cho-Schultz, Deepak, Dalvie, Dac M, Dinh, Martin P, Edwards, Jun Li, Feng, Rose Ann, Ferre, Ketan S, Gajiwala, Michelle D, Hemkens, Amy, Jackson-Fisher, Mehran, Jalaie, Ted O, Johnson, Robert S, Kania, Susan, Kephart, Jennifer, Lafontaine, Beth, Lunney, Kevin K-C, Liu, Zhengyu, Liu, Jean, Matthews, Asako, Nagata, Sherry, Niessen, Martha A, Ornelas, Suvi T M, Orr, Mason, Pairish, Simon, Planken, Shijian, Ren, Daniel, Richter, Kevin, Ryan, Neal, Sach, Hong, Shen, Tod, Smeal, Jim, Solowiej, Scott, Sutton, Khanh, Tran, Elaine, Tseng, William, Vernier, Marlena, Walls, Shuiwang, Wang, Scott L, Weinrich, Shuibo, Xin, Haiwei, Xu, Min-Jean, Yin, Michael, Zientek, Ru, Zhou, John C, Kath

المصدر: Journal of medicinal chemistry. 59(5)

مصطلحات موضوعية: Models, Molecular, Lung Neoplasms, Dose-Response Relationship, Drug, Molecular Structure, ErbB Receptors, Structure-Activity Relationship, Pyrimidines, Carcinoma, Non-Small-Cell Lung, Drug Discovery, Mutation, Tumor Cells, Cultured, Humans, Mutant Proteins, Pyrroles, Protein Kinase Inhibitors

URL الوصول: https://explore.openaire.eu/search/publication?articleId=pmid________::f69cf3e766e492ce164cc24ad82b59de
https://pubmed.ncbi.nlm.nih.gov/26756222

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5

Proteome-wide Map of Targets of T790M-EGFR-Directed Covalent Inhibitors

المؤلفون: Michael R. Lazear, Sherry Niessen, Shuyan Lu, Sabrina Barbas, Zachary E. Potter, Melissa M. Dix, Douglas Carl Behenna, Matthew Merrill Hayward, Kevin Ryan, Simon Paul Planken, John Charles Kath, Benjamin F. Cravatt, Oleg Brodsky, Ketan S. Gajiwala, Chau Almaden, RoseAnn Ferre

المصدر: Cell Chemical Biology. 24:1388-1400.e7

مصطلحات موضوعية: Proteomics, 0301 basic medicine, Proteome, Transplantation, Heterologous, Clinical Biochemistry, Cell, GPI-Linked Proteins, Biochemistry, Article, Piperazines, Mice, 03 medical and health sciences, T790M, 0302 clinical medicine, Cell Line, Tumor, Drug Discovery, medicine, Animals, Humans, Osimertinib, Cysteine, Epidermal growth factor receptor, 5'-Nucleotidase, Protein Kinase Inhibitors, Molecular Biology, EGFR inhibitors, Pharmacology, Acrylamides, Aniline Compounds, biology, Rhodamines, Kinase, Cathepsins, ErbB Receptors, Mice, Inbred C57BL, Checkpoint Kinase 2, HEK293 Cells, 030104 developmental biology, medicine.anatomical_structure, Liver, 030220 oncology & carcinogenesis, Mutagenesis, Site-Directed, biology.protein, Molecular Medicine, Lysosomes

URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f03f226245f7c9e4a9c080544ab02a42
https://doi.org/10.1016/j.chembiol.2017.08.017

6

Effect of PF-04217329 a prodrug of a selective prostaglandin EP(2) agonist on intraocular pressure in preclinical models of glaucoma

المؤلفون: M.R. Niesman, David Gale, Hovhannes J. Gukasyan, Achim H.-P. Krauss, Jay H. Fortner, Jennifer Lafontaine, Husam S. Younis, Soisurin Sartnurak, Ganesh Prasanna, Carol B. Toris, Dac M. Dinh, Scott Anderson, Samantha Carreiro, Cathie Xiang, Chau Almaden, Peter A. Wells

المصدر: Experimental eye research. 93(3)

مصطلحات موضوعية: Agonist, Male, Intraocular pressure, genetic structures, Open angle glaucoma, medicine.drug_class, medicine.medical_treatment, Prostaglandin E2 receptor, Administration, Topical, Drug Evaluation, Preclinical, Glaucoma, Prostaglandin, Biological Availability, Iris, Pharmacology, Acetates, Aqueous Humor, Cornea, Cellular and Molecular Neuroscience, chemistry.chemical_compound, Tonometry, Ocular, Dogs, medicine, Cyclic AMP, Animals, Humans, Prodrugs, Antihypertensive Agents, Intraocular Pressure, Sulfonamides, Ciliary Body, Prodrug, Receptors, Prostaglandin E, EP2 Subtype, medicine.disease, eye diseases, Sensory Systems, Ophthalmology, Disease Models, Animal, Macaca fascicularis, chemistry, Calcium, sense organs, Rabbits, Ophthalmic Solutions, Glaucoma, Open-Angle, Prostaglandin E

URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::476ac4861b50ab056cfa62e7715ec521
https://pubmed.ncbi.nlm.nih.gov/21376717

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7

Ocular pharmacokinetics and hypotensive activity of PF-04475270, an EP4 prostaglandin agonist in preclinical models

المؤلفون: Scott Anderson, Cathie Xiang, Chau Almaden, Samantha Carreiro, Jay H. Fortner, Sajiv Krishnan Nair, Jennifer Lafontaine, M.R. Niesman, Hovhannes J. Gukasyan, Eric Zhang, Grace Wu, Rui Eugene Yuanjin, Ganesh Prasanna, Peter A. Wells, Achim H.-P. Krauss, Soisurin Sartnurak

المصدر: Experimental eye research. 89(5)

مصطلحات موضوعية: Agonist, Intraocular pressure, genetic structures, medicine.drug_class, Administration, Topical, Ocular hypertension, Glaucoma, Biological Availability, Hyperemia, CHO Cells, Thiophenes, Pharmacology, Eye, Transfection, Permeability, Cellular and Molecular Neuroscience, Ciliary body, Cricetulus, Dogs, Pharmacokinetics, Cornea, Cricetinae, Cyclic AMP, Medicine, Animals, Humans, Receptors, Prostaglandin E, Prodrugs, Intraocular Pressure, Dose-Response Relationship, Drug, business.industry, Hydrolysis, Prodrug, medicine.disease, eye diseases, Sensory Systems, Pyrrolidinones, Ophthalmology, medicine.anatomical_structure, Models, Animal, sense organs, Rabbits, Ophthalmic Solutions, business, Receptors, Prostaglandin E, EP4 Subtype

URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eb0c6e1d1a0225213c3cb7986f778c09
https://pubmed.ncbi.nlm.nih.gov/19445930

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8

Abstract 5043: Effects of a novel PI3 kinase/mTOR inhibitor on proliferation and pAKT signaling in canine lymphoma

المصدر: Cancer Research. 70:5043-5043

مصطلحات موضوعية: Cancer Research, Canine Lymphoma, medicine.medical_specialty, business.industry, Kinase, Follicular lymphoma, medicine.disease, Lymphoma, Endocrinology, Oncology, Apoptosis, Internal medicine, Cancer research, Medicine, business, Protein kinase B, Anaplastic large-cell lymphoma, PI3K/AKT/mTOR pathway

URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_________::7c13d86cef4a730ca8aebab3638ff526
https://doi.org/10.1158/1538-7445.am10-5043

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دورية أكاديمية

Covalent EGFR inhibitor analysis reveals importance of reversible interactions to potency and mechanisms of drug resistance.

المؤلفون: Schwartz, Phillip A., Kuzmic, Petr, Solowiej, James, Bergqvist, Simon, Bolanos, Ben, Chau Almaden, Asako Nagata, Ryan, Kevin, Junli Feng, Dalvie, Deepak, Kath, John C., Meirong Xu, Wani, Revati, William Murray, Brion

المصدر: Proceedings of the National Academy of Sciences of the United States of America; 1/7/2014, Vol. 111 Issue 1, p173-178, 6p

مصطلحات موضوعية: DRUG resistance, MATHEMATICAL models, CHEMICAL reactions, CATALYSIS, ENZYME metabolism, DIFFERENTIAL equations

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