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Structure-Based Drug Design and Synthesis of PI3Kα-Selective Inhibitor (PF-06843195).
Cheng H, Orr STM, Bailey S, Brooun A, Chen P, Deal JG, Deng YL, Edwards MP, Gallego GM, Grodsky N, Huang B, Jalaie M, Kaiser S, Kania RS, Kephart SE, Lafontaine J, Ornelas MA, Pairish M, Planken S, Shen H, Sutton S, Zehnder L, Almaden CD, Bagrodia S, Falk MD, Gukasyan HJ, Ho C, Kang X, Kosa RE, Liu L, Spilker ME, Timofeevski S, Visswanathan R, Wang Z, Meng F, Ren S, Shao L, Xu F, Kath JC. Cheng H, et al. Among authors: kosa re. J Med Chem. 2021 Jan 14;64(1):644-661. doi: 10.1021/acs.jmedchem.0c01652. Epub 2020 Dec 24. J Med Chem. 2021. PMID: 33356246
Organic Anion-Transporting Polypeptide 1B1/1B3-Mediated Hepatic Uptake Determines the Pharmacokinetics of Large Lipophilic Acids: In Vitro-In Vivo Evaluation in Cynomolgus Monkey.
Eng H, Bi YA, West MA, Ryu S, Yamaguchi E, Kosa RE, Tess DA, Griffith DA, Litchfield J, Kalgutkar AS, Varma MVS. Eng H, et al. Among authors: kosa re. J Pharmacol Exp Ther. 2021 Apr;377(1):169-180. doi: 10.1124/jpet.120.000457. Epub 2021 Jan 28. J Pharmacol Exp Ther. 2021. PMID: 33509903
Predicting Human Clearance of Organic Anion Transporting Polypeptide Substrates Using Cynomolgus Monkey: In Vitro-In Vivo Scaling of Hepatic Uptake Clearance.
De Bruyn T, Ufuk A, Cantrill C, Kosa RE, Bi YA, Niosi M, Modi S, Rodrigues AD, Tremaine LM, Varma MVS, Galetin A, Houston JB. De Bruyn T, et al. Among authors: kosa re. Drug Metab Dispos. 2018 Jul;46(7):989-1000. doi: 10.1124/dmd.118.081315. Epub 2018 May 2. Drug Metab Dispos. 2018. PMID: 29720472
Discovery of PF-5190457, a Potent, Selective, and Orally Bioavailable Ghrelin Receptor Inverse Agonist Clinical Candidate.
Bhattacharya SK, Andrews K, Beveridge R, Cameron KO, Chen C, Dunn M, Fernando D, Gao H, Hepworth D, Jackson VM, Khot V, Kong J, Kosa RE, Lapham K, Loria PM, Londregan AT, McClure KF, Orr ST, Patel J, Rose C, Saenz J, Stock IA, Storer G, VanVolkenburg M, Vrieze D, Wang G, Xiao J, Zhang Y. Bhattacharya SK, et al. Among authors: kosa re. ACS Med Chem Lett. 2014 Feb 24;5(5):474-9. doi: 10.1021/ml400473x. eCollection 2014 May 8. ACS Med Chem Lett. 2014. PMID: 24900864 Free PMC article.
Leveraging of Rifampicin-Dosed Cynomolgus Monkeys to Identify Bile Acid 3-O-Sulfate Conjugates as Potential Novel Biomarkers for Organic Anion-Transporting Polypeptides.
Thakare R, Gao H, Kosa RE, Bi YA, Varma MVS, Cerny MA, Sharma R, Kuhn M, Huang B, Liu Y, Yu A, Walker GS, Niosi M, Tremaine L, Alnouti Y, Rodrigues AD. Thakare R, et al. Among authors: kosa re. Drug Metab Dispos. 2017 Jul;45(7):721-733. doi: 10.1124/dmd.117.075275. Epub 2017 Apr 10. Drug Metab Dispos. 2017. PMID: 28396527
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