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Structure-activity relationship study of central pyridine-derived TYK2 JH2 inhibitors: Optimization of the PK profile through C4' and C6 variations.
Xiao Z, Yang MG, Liu C, Sherwood T, Gilmore JL, Lin J, Li P, Wu DR, Tokarski J, Li S, Cheng L, Xie C, Fan J, Dierks E, Strnad J, Cvijic ME, Khan J, Ruzanov M, Galella M, Khandelwal P, Dyckman AJ, Mathur A, Lombardo LJ, Macor JE, Carter PH, Aranibar N, Burke JR, Weinstein DS. Xiao Z, et al. Among authors: ruzanov m. Bioorg Med Chem Lett. 2023 Jul 15;91:129373. doi: 10.1016/j.bmcl.2023.129373. Epub 2023 Jun 12. Bioorg Med Chem Lett. 2023. PMID: 37315697
Discovery of BMS-986339, a Pharmacologically Differentiated Farnesoid X Receptor Agonist for the Treatment of Nonalcoholic Steatohepatitis.
Nara SJ, Jogi S, Cheruku S, Kandhasamy S, Jaipuri F, Kathi PK, Reddy S, Sarodaya S, Cook EM, Wang T, Sitkoff D, Rossi KA, Ruzanov M, Kiefer SE, Khan JA, Gao M, Reddy S, Sivaprasad Lvj S, Sane R, Mosure K, Zhuo X, Cao GG, Ziegler M, Azzara A, Krupinski J, Soars MG, Ellsworth BA, Wacker DA. Nara SJ, et al. Among authors: ruzanov m. J Med Chem. 2022 Jul 14;65(13):8948-8960. doi: 10.1021/acs.jmedchem.2c00165. Epub 2022 Jun 15. J Med Chem. 2022. PMID: 35704802
Discovery of Non-Nucleotide Small-Molecule STING Agonists via Chemotype Hybridization.
Cherney EC, Zhang L, Lo J, Huynh T, Wei D, Ahuja V, Quesnelle C, Schieven GL, Futran A, Locke GA, Lin Z, Monereau L, Chaudhry C, Blum J, Li S, Fereshteh M, Li-Wang B, Gangwar S, Pan C, Chong C, Zhu X, Posy SL, Sack JS, Zhang P, Ruzanov M, Harner M, Akhtar F, Schroeder GM, Vite G, Fink B. Cherney EC, et al. Among authors: ruzanov m. J Med Chem. 2022 Feb 24;65(4):3518-3538. doi: 10.1021/acs.jmedchem.1c01986. Epub 2022 Feb 2. J Med Chem. 2022. PMID: 35108011
Signal transfer in human protein tyrosine phosphatase PTP1B from allosteric inhibitor P00058.
Chirgadze YN, Battaile KP, Likhachev IV, Balabaev NK, Gordon RD, Romanov V, Lin A, Karisch R, Lam R, Ruzanov M, Brazhnikov EV, Pai EF, Neel BG, Chirgadze NY. Chirgadze YN, et al. Among authors: ruzanov m. J Biomol Struct Dyn. 2022;40(24):13823-13832. doi: 10.1080/07391102.2021.1994879. Epub 2021 Oct 27. J Biomol Struct Dyn. 2022. PMID: 34705594
Azatricyclic Inverse Agonists of RORγt That Demonstrate Efficacy in Models of Rheumatoid Arthritis and Psoriasis.
Liu Q, Xiao HY, Batt DG, Xiao Z, Zhu Y, Yang MG, Li N, Yip S, Li P, Sun D, Wu DR, Ruzanov M, Sack JS, Weigelt CA, Wang J, Li S, Shuster DJ, Xie JH, Song Y, Sherry T, Obermeier MT, Fura A, Stefanski K, Cornelius G, Chacko S, Khandelwal P, Dudhgaonkar S, Rudra A, Nagar J, Murali V, Govindarajan A, Denton R, Zhao Q, Meanwell NA, Borzilleri R, Dhar TGM. Liu Q, et al. Among authors: ruzanov m. ACS Med Chem Lett. 2021 Apr 30;12(5):827-835. doi: 10.1021/acsmedchemlett.1c00112. eCollection 2021 May 13. ACS Med Chem Lett. 2021. PMID: 34055233 Free PMC article.
Tricyclic-Carbocyclic RORγt Inverse Agonists-Discovery of BMS-986313.
Yang MG, Beaudoin-Bertrand M, Xiao Z, Marcoux D, Weigelt CA, Yip S, Wu DR, Ruzanov M, Sack JS, Wang J, Yarde M, Li S, Shuster DJ, Xie JH, Sherry T, Obermeier MT, Fura A, Stefanski K, Cornelius G, Khandelwal P, Karmakar A, Basha M, Babu V, Gupta AK, Mathur A, Salter-Cid L, Denton R, Zhao Q, Dhar TGM. Yang MG, et al. Among authors: ruzanov m. J Med Chem. 2021 Mar 11;64(5):2714-2724. doi: 10.1021/acs.jmedchem.0c01992. Epub 2021 Feb 16. J Med Chem. 2021. PMID: 33591748
Using yeast surface display to engineer a soluble and crystallizable construct of hematopoietic progenitor kinase 1 (HPK1).
Lau WL, Pearce B, Malakian H, Rodrigo I, Xie D, Gao M, Marsilio F, Chang C, Ruzanov M, Muckelbauer JK, Newitt JA, Lipovšek D, Sheriff S. Lau WL, et al. Among authors: ruzanov m. Acta Crystallogr F Struct Biol Commun. 2021 Jan 1;77(Pt 1):22-28. doi: 10.1107/S2053230X20016015. Epub 2020 Dec 22. Acta Crystallogr F Struct Biol Commun. 2021. PMID: 33439152 Free PMC article.
Substituted diaryl ether compounds as retinoic acid-related orphan Receptor-γt (RORγt) agonists.
Ruan Z, Park PK, Wei D, Purandare A, Wan H, O'Malley D, Stachura S, Perez H, Cavallaro CL, Weigelt CA, Sack JS, Ruzanov M, Khan J, Gururajan M, Wong JJ, Huang Y, Yarde M, Li Z, Chen C, Sun H, Borowski V, Xie JH, Anthony M, Agler M, Fink BE, Harikrishnan LS. Ruan Z, et al. Among authors: ruzanov m. Bioorg Med Chem Lett. 2021 Mar 1;35:127778. doi: 10.1016/j.bmcl.2021.127778. Epub 2021 Jan 8. Bioorg Med Chem Lett. 2021. PMID: 33422603
25 results