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Discovery of Potent and Orally Bioavailable Small Molecule Antagonists of Toll-like Receptors 7/8/9 (TLR7/8/9).
Mussari CP, Dodd DS, Sreekantha RK, Pasunoori L, Wan H, Posy SL, Critton D, Ruepp S, Subramanian M, Watson A, Davies P, Schieven GL, Salter-Cid LM, Srivastava R, Tagore DM, Dudhgaonkar S, Poss MA, Carter PH, Dyckman AJ. Mussari CP, et al. ACS Med Chem Lett. 2020 Jul 29;11(9):1751-1758. doi: 10.1021/acsmedchemlett.0c00264. eCollection 2020 Sep 10. ACS Med Chem Lett. 2020. PMID: 32944143 Free PMC article.
Identification of 2-Pyridinylindole-Based Dual Antagonists of Toll-like Receptors 7 and 8 (TLR7/8).
Sreekantha RK, Mussari CP, Dodd DS, Pasunoori L, Hegde S, Posy SL, Critton D, Ruepp S, Subramanian M, Salter-Cid LM, Tagore DM, Sarodaya S, Dudhgaonkar S, Poss MA, Schieven GL, Carter PH, Macor JE, Dyckman AJ. Sreekantha RK, et al. Among authors: mussari cp. ACS Med Chem Lett. 2022 Apr 25;13(5):812-818. doi: 10.1021/acsmedchemlett.2c00049. eCollection 2022 May 12. ACS Med Chem Lett. 2022. PMID: 35586440 Free PMC article.
Discovery and Preclinical Pharmacology of an Oral Bromodomain and Extra-Terminal (BET) Inhibitor Using Scaffold-Hopping and Structure-Guided Drug Design.
Gavai AV, Norris D, Delucca G, Tortolani D, Tokarski JS, Dodd D, O'Malley D, Zhao Y, Quesnelle C, Gill P, Vaccaro W, Huynh T, Ahuja V, Han WC, Mussari C, Harikrishnan L, Kamau M, Poss M, Sheriff S, Yan C, Marsilio F, Menard K, Wen ML, Rampulla R, Wu DR, Li J, Zhang H, Li P, Sun D, Yip H, Traeger SC, Zhang Y, Mathur A, Zhang H, Huang C, Yang Z, Ranasinghe A, Everlof G, Raghavan N, Tye CK, Wee S, Hunt JT, Vite G, Westhouse R, Lee FY. Gavai AV, et al. J Med Chem. 2021 Oct 14;64(19):14247-14265. doi: 10.1021/acs.jmedchem.1c00625. Epub 2021 Sep 20. J Med Chem. 2021. PMID: 34543572
Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535.
Duplantier AJ, Dombroski MA, Subramanyam C, Beaulieu AM, Chang SP, Gabel CA, Jordan C, Kalgutkar AS, Kraus KG, Labasi JM, Mussari C, Perregaux DG, Shepard R, Taylor TJ, Trevena KA, Whitney-Pickett C, Yoon K. Duplantier AJ, et al. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3708-11. doi: 10.1016/j.bmcl.2011.04.077. Epub 2011 Apr 24. Bioorg Med Chem Lett. 2011. PMID: 21565499