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Hit Triage and Validation in Phenotypic Screening: Considerations and Strategies.
Vincent F, Loria PM, Weston AD, Steppan CM, Doyonnas R, Wang YM, Rockwell KL, Peakman MC. Vincent F, et al. Among authors: loria pm. Cell Chem Biol. 2020 Nov 19;27(11):1332-1346. doi: 10.1016/j.chembiol.2020.08.009. Epub 2020 Sep 3. Cell Chem Biol. 2020. PMID: 32888500 Free article. Review.
Developing predictive assays: the phenotypic screening "rule of 3".
Vincent F, Loria P, Pregel M, Stanton R, Kitching L, Nocka K, Doyonnas R, Steppan C, Gilbert A, Schroeter T, Peakman MC. Vincent F, et al. Sci Transl Med. 2015 Jun 24;7(293):293ps15. doi: 10.1126/scitranslmed.aab1201. Sci Transl Med. 2015. PMID: 26109101 Review.
Discovery of Ervogastat (PF-06865571): A Potent and Selective Inhibitor of Diacylglycerol Acyltransferase 2 for the Treatment of Non-alcoholic Steatohepatitis.
Futatsugi K, Cabral S, Kung DW, Huard K, Lee E, Boehm M, Bauman J, Clark RW, Coffey SB, Crowley C, Dechert-Schmitt AM, Dowling MS, Dullea R, Gosset JR, Kalgutkar AS, Kou K, Li Q, Lian Y, Loria PM, Londregan AT, Niosi M, Orozco C, Pettersen JC, Pfefferkorn JA, Polivkova J, Ross TT, Sharma R, Stock IA, Tesz G, Wisniewska H, Goodwin B, Price DA. Futatsugi K, et al. Among authors: loria pm. J Med Chem. 2022 Nov 24;65(22):15000-15013. doi: 10.1021/acs.jmedchem.2c01200. Epub 2022 Nov 2. J Med Chem. 2022. PMID: 36322383
Chemical Probe Identification Platform for Orphan GPCRs Using Focused Compound Screening: GPR39 as a Case Example.
Boehm M, Hepworth D, Loria PM, Norquay LD, Filipski KJ, Chin JE, Cameron KO, Brenner M, Bonnette P, Cabral S, Conn E, Ebner DC, Gautreau D, Hadcock J, Lee EC, Mathiowetz AM, Morin M, Rogers L, Smith A, VanVolkenburg M, Carpino PA. Boehm M, et al. Among authors: loria pm. ACS Med Chem Lett. 2013 Sep 16;4(11):1079-84. doi: 10.1021/ml400275z. eCollection 2013 Nov 14. ACS Med Chem Lett. 2013. PMID: 24900608 Free PMC article.
Helixconstraints and amino acid substitution in GLP-1 increase cAMP and insulin secretion but not beta-arrestin 2 signaling.
Plisson F, Hill TA, Mitchell JM, Hoang HN, de Araujo AD, Xu W, Cotterell A, Edmonds DJ, Stanton RV, Derksen DR, Loria PM, Griffith DA, Price DA, Liras S, Fairlie DP. Plisson F, et al. Among authors: loria pm. Eur J Med Chem. 2017 Feb 15;127:703-714. doi: 10.1016/j.ejmech.2016.10.044. Epub 2016 Oct 21. Eur J Med Chem. 2017. PMID: 27823886
Selective stalling of human translation through small-molecule engagement of the ribosome nascent chain.
Lintner NG, McClure KF, Petersen D, Londregan AT, Piotrowski DW, Wei L, Xiao J, Bolt M, Loria PM, Maguire B, Geoghegan KF, Huang A, Rolph T, Liras S, Doudna JA, Dullea RG, Cate JH. Lintner NG, et al. Among authors: loria pm. PLoS Biol. 2017 Mar 21;15(3):e2001882. doi: 10.1371/journal.pbio.2001882. eCollection 2017 Mar. PLoS Biol. 2017. PMID: 28323820 Free PMC article.
Liver-Targeted Small-Molecule Inhibitors of Proprotein Convertase Subtilisin/Kexin Type 9 Synthesis.
McClure KF, Piotrowski DW, Petersen D, Wei L, Xiao J, Londregan AT, Kamlet AS, Dechert-Schmitt AM, Raymer B, Ruggeri RB, Canterbury D, Limberakis C, Liras S, DaSilva-Jardine P, Dullea RG, Loria PM, Reidich B, Salatto CT, Eng H, Kimoto E, Atkinson K, King-Ahmad A, Scott D, Beaumont K, Chabot JR, Bolt MW, Maresca K, Dahl K, Arakawa R, Takano A, Halldin C. McClure KF, et al. Among authors: loria pm. Angew Chem Int Ed Engl. 2017 Dec 18;56(51):16218-16222. doi: 10.1002/anie.201708744. Epub 2017 Nov 24. Angew Chem Int Ed Engl. 2017. PMID: 29073340
Identification of Morpholino-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-ones as Nonsteroidal Mineralocorticoid Antagonists.
Piotrowski DW, Futatsugi K, Casimiro-Garcia A, Wei L, Sammons MF, Herr M, Jiao W, Lavergne SY, Coffey SB, Wright SW, Song K, Loria PM, Banker ME, Petersen DN, Bauman J. Piotrowski DW, et al. Among authors: loria pm. J Med Chem. 2018 Feb 8;61(3):1086-1097. doi: 10.1021/acs.jmedchem.7b01515. Epub 2018 Jan 23. J Med Chem. 2018. PMID: 29300474
41 results