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1-amino-4-benzylphthalazines as orally bioavailable smoothened antagonists with antitumor activity.
Miller-Moslin K, Peukert S, Jain RK, McEwan MA, Karki R, Llamas L, Yusuff N, He F, Li Y, Sun Y, Dai M, Perez L, Michael W, Sheng T, Lei H, Zhang R, Williams J, Bourret A, Ramamurthy A, Yuan J, Guo R, Matsumoto M, Vattay A, Maniara W, Amaral A, Dorsch M, Kelleher JF 3rd. Miller-Moslin K, et al. Among authors: jain rk. J Med Chem. 2009 Jul 9;52(13):3954-68. doi: 10.1021/jm900309j. J Med Chem. 2009. PMID: 19469545
Target identification for a Hedgehog pathway inhibitor reveals the receptor GPR39.
Bassilana F, Carlson A, DaSilva JA, Grosshans B, Vidal S, Beck V, Wilmeringwetter B, Llamas LA, Showalter TB, Rigollier P, Bourret A, Ramamurthy A, Wu X, Harbinski F, Plonsky S, Lee L, Ruffner H, Grandi P, Schirle M, Jenkins J, Sailer AW, Bouwmeester T, Porter JA, Myer V, Finan PM, Tallarico JA, Kelleher JF 3rd, Seuwen K, Jain RK, Luchansky SJ. Bassilana F, et al. Among authors: jain rk. Nat Chem Biol. 2014 May;10(5):343-9. doi: 10.1038/nchembio.1481. Epub 2014 Mar 16. Nat Chem Biol. 2014. PMID: 24633354
Discovery of 2-Pyridylpyrimidines as the First Orally Bioavailable GPR39 Agonists.
Peukert S, Hughes R, Nunez J, He G, Yan Z, Jain R, Llamas L, Luchansky S, Carlson A, Liang G, Kunjathoor V, Pietropaolo M, Shapiro J, Castellana A, Wu X, Bose A. Peukert S, et al. ACS Med Chem Lett. 2014 Aug 4;5(10):1114-8. doi: 10.1021/ml500240d. eCollection 2014 Oct 9. ACS Med Chem Lett. 2014. PMID: 25313322 Free PMC article.
Discovery of a ZIP7 inhibitor from a Notch pathway screen.
Nolin E, Gans S, Llamas L, Bandyopadhyay S, Brittain SM, Bernasconi-Elias P, Carter KP, Loureiro JJ, Thomas JR, Schirle M, Yang Y, Guo N, Roma G, Schuierer S, Beibel M, Lindeman A, Sigoillot F, Chen A, Xie KX, Ho S, Reece-Hoyes J, Weihofen WA, Tyskiewicz K, Hoepfner D, McDonald RI, Guthrie N, Dogra A, Guo H, Shao J, Ding J, Canham SM, Boynton G, George EL, Kang ZB, Antczak C, Porter JA, Wallace O, Tallarico JA, Palmer AE, Jenkins JL, Jain RK, Bushell SM, Fryer CJ. Nolin E, et al. Among authors: jain rk. Nat Chem Biol. 2019 Feb;15(2):179-188. doi: 10.1038/s41589-018-0200-7. Epub 2019 Jan 14. Nat Chem Biol. 2019. PMID: 30643281 Free PMC article.
Phenotypic screen identifies calcineurin-sparing FK506 analogs as BMP potentiators for treatment of acute kidney injury.
Larraufie MH, Gao X, Xia X, Devine PJ, Kallen J, Liu D, Michaud G, Harsch A, Savage N, Ding J, Tan K, Mihalic M, Roggo S, Canham SM, Bushell SM, Krastel P, Gao J, Izaac A, Altinoglu E, Lustenberger P, Salcius M, Harbinski F, Williams ET, Zeng L, Loureiro J, Cong F, Fryer CJ, Klickstein L, Tallarico JA, Jain RK, Rothman DM, Wang S. Larraufie MH, et al. Among authors: jain rk. Cell Chem Biol. 2021 Sep 16;28(9):1271-1282.e12. doi: 10.1016/j.chembiol.2021.04.001. Epub 2021 Apr 23. Cell Chem Biol. 2021. PMID: 33894161 Free article.
Previously Uncharacterized Vacuolar-type ATPase Binding Site Discovered from Structurally Similar Compounds with Distinct Mechanisms of Action.
Wang AC, Pham HT, Lipps JM, Brittain SM, Harrington E, Wang Y, King FJ, Russ C, Pan X, Hoepfner D, Tallarico J, Feng Y, Jain RK, Schirle M, Thomas JR. Wang AC, et al. Among authors: jain rk. ACS Chem Biol. 2019 Jan 18;14(1):20-26. doi: 10.1021/acschembio.8b00656. Epub 2018 Dec 18. ACS Chem Biol. 2019. PMID: 30461263
1,369 results