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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: ruggeri rb. 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
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: ruggeri rb. 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
Discovery of 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases.
Ruggeri RB, Buckbinder L, Bagley SW, Carpino PA, Conn EL, Dowling MS, Fernando DP, Jiao W, Kung DW, Orr ST, Qi Y, Rocke BN, Smith A, Warmus JS, Zhang Y, Bowles D, Widlicka DW, Eng H, Ryder T, Sharma R, Wolford A, Okerberg C, Walters K, Maurer TS, Zhang Y, Bonin PD, Spath SN, Xing G, Hepworth D, Ahn K, Kalgutkar AS. Ruggeri RB, et al. J Med Chem. 2015 Nov 12;58(21):8513-28. doi: 10.1021/acs.jmedchem.5b00963. Epub 2015 Oct 28. J Med Chem. 2015. PMID: 26509551
Truncated Glucagon-like Peptide-1 and Exendin-4 α-Conotoxin pl14a Peptide Chimeras Maintain Potency and α-Helicity and Reveal Interactions Vital for cAMP Signaling in Vitro.
Swedberg JE, Schroeder CI, Mitchell JM, Fairlie DP, Edmonds DJ, Griffith DA, Ruggeri RB, Derksen DR, Loria PM, Price DA, Liras S, Craik DJ. Swedberg JE, et al. Among authors: ruggeri rb. J Biol Chem. 2016 Jul 22;291(30):15778-87. doi: 10.1074/jbc.M116.724542. Epub 2016 May 10. J Biol Chem. 2016. PMID: 27226591 Free PMC article.
A Small-Molecule Anti-secretagogue of PCSK9 Targets the 80S Ribosome to Inhibit PCSK9 Protein Translation.
Petersen DN, Hawkins J, Ruangsiriluk W, Stevens KA, Maguire BA, O'Connell TN, Rocke BN, Boehm M, Ruggeri RB, Rolph T, Hepworth D, Loria PM, Carpino PA. Petersen DN, et al. Among authors: ruggeri rb. Cell Chem Biol. 2016 Nov 17;23(11):1362-1371. doi: 10.1016/j.chembiol.2016.08.016. Epub 2016 Oct 13. Cell Chem Biol. 2016. PMID: 27746128 Free 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: ruggeri rb. 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
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: ruggeri rb. 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.
32 results