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Small-molecule inhibitors directly target CARD9 and mimic its protective variant in inflammatory bowel disease.
Leshchiner ES, Rush JS, Durney MA, Cao Z, Dančík V, Chittick B, Wu H, Petrone A, Bittker JA, Phillips A, Perez JR, Shamji AF, Kaushik VK, Daly MJ, Graham DB, Schreiber SL, Xavier RJ. Leshchiner ES, et al. Among authors: kaushik vk. Proc Natl Acad Sci U S A. 2017 Oct 24;114(43):11392-11397. doi: 10.1073/pnas.1705748114. Epub 2017 Oct 9. Proc Natl Acad Sci U S A. 2017. PMID: 29073062 Free PMC article.
A small-molecule allosteric inhibitor of Mycobacterium tuberculosis tryptophan synthase.
Wellington S, Nag PP, Michalska K, Johnston SE, Jedrzejczak RP, Kaushik VK, Clatworthy AE, Siddiqi N, McCarren P, Bajrami B, Maltseva NI, Combs S, Fisher SL, Joachimiak A, Schreiber SL, Hung DT. Wellington S, et al. Among authors: kaushik vk. Nat Chem Biol. 2017 Sep;13(9):943-950. doi: 10.1038/nchembio.2420. Epub 2017 Jul 3. Nat Chem Biol. 2017. PMID: 28671682 Free PMC article.
Multimodal small-molecule screening for human prion protein binders.
Reidenbach AG, Mesleh MF, Casalena D, Vallabh SM, Dahlin JL, Leed AJ, Chan AI, Usanov DL, Yehl JB, Lemke CT, Campbell AJ, Shah RN, Shrestha OK, Sacher JR, Rangel VL, Moroco JA, Sathappa M, Nonato MC, Nguyen KT, Wright SK, Liu DR, Wagner FF, Kaushik VK, Auld DS, Schreiber SL, Minikel EV. Reidenbach AG, et al. Among authors: kaushik vk. J Biol Chem. 2020 Sep 25;295(39):13516-13531. doi: 10.1074/jbc.RA120.014905. Epub 2020 Jul 28. J Biol Chem. 2020. PMID: 32723867 Free PMC article.
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: kaushik vk. 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
Genetic analysis in UK Biobank links insulin resistance and transendothelial migration pathways to coronary artery disease.
Klarin D, Zhu QM, Emdin CA, Chaffin M, Horner S, McMillan BJ, Leed A, Weale ME, Spencer CCA, Aguet F, Segrè AV, Ardlie KG, Khera AV, Kaushik VK, Natarajan P; CARDIoGRAMplusC4D Consortium; Kathiresan S. Klarin D, et al. Among authors: kaushik vk. Nat Genet. 2017 Sep;49(9):1392-1397. doi: 10.1038/ng.3914. Epub 2017 Jul 17. Nat Genet. 2017. PMID: 28714974 Free PMC article.
Discovery of a First-in-Class Inhibitor of the PRMT5-Substrate Adaptor Interaction.
McKinney DC, McMillan BJ, Ranaghan MJ, Moroco JA, Brousseau M, Mullin-Bernstein Z, O'Keefe M, McCarren P, Mesleh MF, Mulvaney KM, Robinson F, Singh R, Bajrami B, Wagner FF, Hilgraf R, Drysdale MJ, Campbell AJ, Skepner A, Timm DE, Porter D, Kaushik VK, Sellers WR, Ianari A. McKinney DC, et al. Among authors: kaushik vk. J Med Chem. 2021 Aug 12;64(15):11148-11168. doi: 10.1021/acs.jmedchem.1c00507. Epub 2021 Aug 3. J Med Chem. 2021. PMID: 34342224 Free PMC article.
Small-molecule WNK inhibition regulates cardiovascular and renal function.
Yamada K, Park HM, Rigel DF, DiPetrillo K, Whalen EJ, Anisowicz A, Beil M, Berstler J, Brocklehurst CE, Burdick DA, Caplan SL, Capparelli MP, Chen G, Chen W, Dale B, Deng L, Fu F, Hamamatsu N, Harasaki K, Herr T, Hoffmann P, Hu QY, Huang WJ, Idamakanti N, Imase H, Iwaki Y, Jain M, Jeyaseelan J, Kato M, Kaushik VK, Kohls D, Kunjathoor V, LaSala D, Lee J, Liu J, Luo Y, Ma F, Mo R, Mowbray S, Mogi M, Ossola F, Pandey P, Patel SJ, Raghavan S, Salem B, Shanado YH, Trakshel GM, Turner G, Wakai H, Wang C, Weldon S, Wielicki JB, Xie X, Xu L, Yagi YI, Yasoshima K, Yin J, Yowe D, Zhang JH, Zheng G, Monovich L. Yamada K, et al. Among authors: kaushik vk. Nat Chem Biol. 2016 Nov;12(11):896-898. doi: 10.1038/nchembio.2168. Epub 2016 Sep 5. Nat Chem Biol. 2016. PMID: 27595330
Systematic identification of biomarker-driven drug combinations to overcome resistance.
Rees MG, Brenan L, do Carmo M, Duggan P, Bajrami B, Arciprete M, Boghossian A, Vaimberg E, Ferrara SJ, Lewis TA, Rosenberg D, Sangpo T, Roth JA, Kaushik VK, Piccioni F, Doench JG, Root DE, Johannessen CM. Rees MG, et al. Among authors: kaushik vk. Nat Chem Biol. 2022 Jun;18(6):615-624. doi: 10.1038/s41589-022-00996-7. Epub 2022 Mar 24. Nat Chem Biol. 2022. PMID: 35332332
39 results