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Page 1
Identification of highly selective SIK1/2 inhibitors that modulate innate immune activation and suppress intestinal inflammation.
Babbe H, Sundberg TB, Tichenor M, Seierstad M, Bacani G, Berstler J, Chai W, Chang L, Chung M, Coe K, Collins B, Finley M, Guletsky A, Lemke CT, Mak PA, Mathur A, Mercado-Marin EV, Metkar S, Raymond DD, Rives ML, Rizzolio M, Shaffer PL, Smith R, Smith J, Steele R, Steffens H, Suarez J, Tian G, Majewski N, Volak LP, Wei J, Desai PT, Ong LL, Koudriakova T, Goldberg SD, Hirst G, Kaushik VK, Ort T, Seth N, Graham DB, Plevy S, Venable JD, Xavier RJ, Towne JE. Babbe H, et al. Among authors: koudriakova t. Proc Natl Acad Sci U S A. 2024 Jan 2;121(1):e2307086120. doi: 10.1073/pnas.2307086120. Epub 2023 Dec 26. Proc Natl Acad Sci U S A. 2024. PMID: 38147543 Free PMC article.
Discovery of a Gut-Restricted JAK Inhibitor for the Treatment of Inflammatory Bowel Disease.
Leonard KA, Madge LA, Krawczuk PJ, Wang A, Kreutter KD, Bacani GM, Chai W, Smith RC, Tichenor MS, Harris MC, Malaviya R, Seierstad M, Johnson ME, Venable JD, Kim S, Hirst GC, Mathur AS, Rao TS, Edwards JP, Rizzolio MC, Koudriakova T. Leonard KA, et al. Among authors: koudriakova t. J Med Chem. 2020 Mar 26;63(6):2915-2929. doi: 10.1021/acs.jmedchem.9b01439. Epub 2020 Mar 16. J Med Chem. 2020. PMID: 32134643
Characterization of JNJ-2482272 [4-(4-Methyl-2-(4-(Trifluoromethyl)Phenyl)Thiazole-5-yl) Pyrimidine-2-Amine] As a Strong Aryl Hydrocarbon Receptor Activator in Rat and Human.
Coe KJ, Feinstein M, Higgins JW, Leung P, Scott BP, Skaptason J, Tam Y, Volak LP, Kinong J, Bittner A, McAllister H, Lim NM, Hack M, Koudriakova T. Coe KJ, et al. Among authors: koudriakova t. Drug Metab Dispos. 2022 Aug;50(8):1064-1076. doi: 10.1124/dmd.121.000825. Epub 2022 Jun 9. Drug Metab Dispos. 2022. PMID: 35680134
Substituted Azabicyclo[2.2.1]heptanes as Selective Orexin-1 Antagonists: Discovery of JNJ-54717793.
Préville C, Bonaventure P, Koudriakova T, Lord B, Nepomuceno D, Rizzolio M, Mani N, Coe KJ, Ndifor A, Dugovic C, Dvorak CA, Coate H, Pippel DJ, Fitzgerald A, Allison B, Lovenberg TW, Carruthers NI, Shireman BT. Préville C, et al. Among authors: koudriakova t. ACS Med Chem Lett. 2020 Apr 27;11(10):2002-2009. doi: 10.1021/acsmedchemlett.0c00085. eCollection 2020 Oct 8. ACS Med Chem Lett. 2020. PMID: 33062185 Free PMC article.
Pharmacologic Characterization of JNJ-42226314, [1-(4-Fluorophenyl)indol-5-yl]-[3-[4-(thiazole-2-carbonyl)piperazin-1-yl]azetidin-1-yl]methanone, a Reversible, Selective, and Potent Monoacylglycerol Lipase Inhibitor.
Wyatt RM, Fraser I, Welty N, Lord B, Wennerholm M, Sutton S, Ameriks MK, Dugovic C, Yun S, White A, Nguyen L, Koudriakova T, Tian G, Suarez J, Szewczuk L, Bonnette W, Ahn K, Ghosh B, Flores CM, Connolly PJ, Zhu B, Macielag MJ, Brandt MR, Chevalier K, Zhang SP, Lovenberg T, Bonaventure P. Wyatt RM, et al. Among authors: koudriakova t. J Pharmacol Exp Ther. 2020 Mar;372(3):339-353. doi: 10.1124/jpet.119.262139. Epub 2019 Dec 9. J Pharmacol Exp Ther. 2020. PMID: 31818916
Characterization of JNJ-42847922, a Selective Orexin-2 Receptor Antagonist, as a Clinical Candidate for the Treatment of Insomnia.
Bonaventure P, Shelton J, Yun S, Nepomuceno D, Sutton S, Aluisio L, Fraser I, Lord B, Shoblock J, Welty N, Chaplan SR, Aguilar Z, Halter R, Ndifor A, Koudriakova T, Rizzolio M, Letavic M, Carruthers NI, Lovenberg T, Dugovic C. Bonaventure P, et al. Among authors: koudriakova t. J Pharmacol Exp Ther. 2015 Sep;354(3):471-82. doi: 10.1124/jpet.115.225466. Epub 2015 Jul 15. J Pharmacol Exp Ther. 2015. PMID: 26177655
Lead Optimization of 5-Aryl Benzimidazolone- and Oxindole-Based AMPA Receptor Modulators Selective for TARP γ-8.
Ravula S, Savall BM, Wu N, Lord B, Coe K, Wang K, Seierstad M, Swanson DM, Ziff J, Nguyen M, Leung P, Rynberg R, La D, Pippel DJ, Koudriakova T, Lovenberg TW, Carruthers NI, Maher MP, Ameriks MK. Ravula S, et al. Among authors: koudriakova t. ACS Med Chem Lett. 2018 Jul 13;9(8):821-826. doi: 10.1021/acsmedchemlett.8b00215. eCollection 2018 Aug 9. ACS Med Chem Lett. 2018. PMID: 30128074 Free PMC article.
1H-Pyrrolo[3,2-b]pyridine GluN2B-Selective Negative Allosteric Modulators.
Chrovian CC, Soyode-Johnson A, Wall JL, Rech JC, Schoellerman J, Lord B, Coe KJ, Carruthers NI, Nguyen L, Jiang X, Koudriakova T, Balana B, Letavic MA. Chrovian CC, et al. Among authors: koudriakova t. ACS Med Chem Lett. 2019 Jan 10;10(3):261-266. doi: 10.1021/acsmedchemlett.8b00542. eCollection 2019 Mar 14. ACS Med Chem Lett. 2019. PMID: 30891123 Free PMC article.
Discovery of Imidazo[1,2-a]pyrazines and Pyrazolo[1,5-c]pyrimidines as TARP γ-8 Selective AMPAR Negative Modulators.
Savall BM, Wu D, Swanson DM, Seierstad M, Wu N, Vives Martinez J, García Olmos B, Lord B, Coe K, Koudriakova T, Lovenberg TW, Carruthers NI, Maher MP, Ameriks MK. Savall BM, et al. Among authors: koudriakova t. ACS Med Chem Lett. 2018 Dec 26;10(3):267-272. doi: 10.1021/acsmedchemlett.8b00599. eCollection 2019 Mar 14. ACS Med Chem Lett. 2018. PMID: 30891124 Free PMC article.
Design, Synthesis, and Preclinical Evaluation of 3-Methyl-6-(5-thiophenyl)-1,3-dihydro-imidazo[4,5-b]pyridin-2-ones as Selective GluN2B Negative Allosteric Modulators for the Treatment of Mood Disorders.
Chrovian CC, Soyode-Johnson A, Stenne B, Pippel DJ, Schoellerman J, Lord B, Needham AS, Xia C, Coe KJ, Sepassi K, Schoetens F, Scott B, Nguyen L, Jiang X, Koudriakova T, Balana B, Letavic MA. Chrovian CC, et al. Among authors: koudriakova t. J Med Chem. 2020 Sep 10;63(17):9181-9196. doi: 10.1021/acs.jmedchem.9b02113. Epub 2020 Aug 28. J Med Chem. 2020. PMID: 32787105
34 results