Search Results - "Almaden, Chau"
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Covalent EGFR inhibitor analysis reveals importance of reversible interactions to potency and mechanisms of drug resistance
Published in Proceedings of the National Academy of Sciences - PNAS (07-01-2014)“…Covalent inhibition is a reemerging paradigm in kinase drug design, but the roles of inhibitor binding affinity and chemical reactivity in overall potency are…”
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Proteome-wide Map of Targets of T790M-EGFR-Directed Covalent Inhibitors
Published in Cell chemical biology (16-11-2017)“…Patients with non-small cell lung cancers that have kinase-activating epidermal growth factor receptor (EGFR) mutations are highly responsive to first-…”
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Structure-Based Drug Design and Synthesis of PI3Kα-Selective Inhibitor (PF-06843195)
Published in Journal of medicinal chemistry (14-01-2021)“…The phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) signaling pathway is a frequently dysregulated pathway in human cancer, and PI3Kα is…”
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Effect of PF-04217329 a prodrug of a selective prostaglandin EP2 agonist on intraocular pressure in preclinical models of glaucoma
Published in Experimental eye research (01-09-2011)Get full text
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Ocular pharmacokinetics and hypotensive activity of PF-04475270, an EP4 prostaglandin agonist in preclinical models
Published in Experimental eye research (01-11-2009)“…Prostaglandins are widely used to lower intraocular pressure (IOP) as part of the treatment regimen for glaucoma. While FP and EP2 agonists are known to lower…”
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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
Published in Journal of medicinal chemistry (13-04-2017)“…Mutant epidermal growth factor receptor (EGFR) is a major driver of non-small-cell lung cancer (NSCLC). Marketed first generation inhibitors, such as…”
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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
Published in Journal of medicinal chemistry (10-03-2016)“…First generation EGFR TKIs (gefitinib, erlotinib) provide significant clinical benefit for NSCLC cancer patients with oncogenic EGFR mutations. Ultimately,…”
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Effect of PF-04217329 a prodrug of a selective prostaglandin EP 2 agonist on intraocular pressure in preclinical models of glaucoma
Published in Experimental eye research (01-09-2011)“…Better control of intraocular pressure (IOP) is the most effective way to preserve visual field function in glaucomatous patients. While prostaglandin FP…”
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Discovery of N -((3 R ,4 R )-4-Fluoro-1-(6-((3-methoxy-1-methyl-1 H -pyrazol-4-yl)amino)-9-methyl-9 H -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
Published in Journal of medicinal chemistry (13-04-2017)Get full text
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Abstract 5043: Effects of a novel PI3 kinase/mTOR inhibitor on proliferation and pAKT signaling in canine lymphoma
Published in Cancer research (Chicago, Ill.) (15-04-2010)“…Abstract PF-04691503 is a dual inhibitor of both PI3K and mTOR, inhibits PI3K signaling in cancer cell lines, and exhibits in vitro and in vivo…”
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Effect of PF-04217329 a prodrug of a selective prostaglandin EP(2) agonist on intraocular pressure in preclinical models of glaucoma
Published in Experimental eye research (01-09-2011)“…Better control of intraocular pressure (IOP) is the most effective way to preserve visual field function in glaucomatous patients. While prostaglandin FP…”
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