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Page 1
Discovery of High-Affinity Small-Molecule Binders of the Epigenetic Reader YEATS4.
Londregan AT, Aitmakhanova K, Bennett J, Byrnes LJ, Canterbury DP, Cheng X, Christott T, Clemens J, Coffey SB, Dias JM, Dowling MS, Farnie G, Fedorov O, Fennell KF, Gamble V, Gileadi C, Giroud C, Harris MR, Hollingshead BD, Huber K, Korczynska M, Lapham K, Loria PM, Narayanan A, Owen DR, Raux B, Sahasrabudhe PV, Ruggeri RB, Sáez LD, Stock IA, Thuma BA, Tsai A, Varghese AE. Londregan AT, et al. Among authors: loria pm. J Med Chem. 2023 Jan 12;66(1):460-472. doi: 10.1021/acs.jmedchem.2c01421. Epub 2022 Dec 23. J Med Chem. 2023. PMID: 36562986
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: loria pm. 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.
A Small-Molecule Oral Agonist of the Human Glucagon-like Peptide-1 Receptor.
Griffith DA, Edmonds DJ, Fortin JP, Kalgutkar AS, Kuzmiski JB, Loria PM, Saxena AR, Bagley SW, Buckeridge C, Curto JM, Derksen DR, Dias JM, Griffor MC, Han S, Jackson VM, Landis MS, Lettiere D, Limberakis C, Liu Y, Mathiowetz AM, Patel JC, Piotrowski DW, Price DA, Ruggeri RB, Tess DA. Griffith DA, et al. Among authors: loria pm. J Med Chem. 2022 Jun 23;65(12):8208-8226. doi: 10.1021/acs.jmedchem.1c01856. Epub 2022 Jun 1. J Med Chem. 2022. PMID: 35647711 Free PMC article.
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
Evaluation and synthesis of polar aryl- and heteroaryl spiroazetidine-piperidine acetamides as ghrelin inverse agonists.
Orr ST, Beveridge R, Bhattacharya SK, Cameron KO, Coffey S, Fernando D, Hepworth D, Jackson MV, Khot V, Kosa R, Lapham K, Loria PM, McClure KF, Patel J, Rose C, Saenz J, Stock IA, Storer G, von Volkenburg M, Vrieze D, Wang G, Xiao J, Zhang Y. Orr ST, et al. Among authors: loria pm. ACS Med Chem Lett. 2014 Dec 14;6(2):156-61. doi: 10.1021/ml500414n. eCollection 2015 Feb 12. ACS Med Chem Lett. 2014. PMID: 25699143 Free PMC article.
Discovery of an in Vivo Tool to Establish Proof-of-Concept for MAP4K4-Based Antidiabetic Treatment.
Ammirati M, Bagley SW, Bhattacharya SK, Buckbinder L, Carlo AA, Conrad R, Cortes C, Dow RL, Dowling MS, El-Kattan A, Ford K, Guimarães CR, Hepworth D, Jiao W, LaPerle J, Liu S, Londregan A, Loria PM, Mathiowetz AM, Munchhof M, Orr ST, Petersen DN, Price DA, Skoura A, Smith AC, Wang J. Ammirati M, et al. Among authors: loria pm. ACS Med Chem Lett. 2015 Oct 6;6(11):1128-33. doi: 10.1021/acsmedchemlett.5b00215. eCollection 2015 Nov 12. ACS Med Chem Lett. 2015. PMID: 26617966 Free PMC article.
Optimization of amide-based EP3 receptor antagonists.
Lee EC, Futatsugi K, Arcari JT, Bahnck K, Coffey SB, Derksen DR, Kalgutkar AS, Loria PM, Sharma R. Lee EC, et al. Among authors: loria pm. Bioorg Med Chem Lett. 2016 Jun 1;26(11):2670-5. doi: 10.1016/j.bmcl.2016.04.009. Epub 2016 Apr 9. Bioorg Med Chem Lett. 2016. PMID: 27107947
Cyclic alpha-conotoxin peptidomimetic chimeras as potent GLP-1R agonists.
Swedberg JE, Schroeder CI, Mitchell JM, Durek T, Fairlie DP, Edmonds DJ, Griffith DA, Ruggeri RB, Derksen DR, Loria PM, Liras S, Price DA, Craik DJ. Swedberg JE, et al. Among authors: loria pm. Eur J Med Chem. 2015 Oct 20;103:175-84. doi: 10.1016/j.ejmech.2015.08.046. Epub 2015 Aug 29. Eur J Med Chem. 2015. PMID: 26352676
40 results