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Exploring the target scope of KEAP1 E3 ligase-based PROTACs.
Du G, Jiang J, Henning NJ, Safaee N, Koide E, Nowak RP, Donovan KA, Yoon H, You I, Yue H, Eleuteri NA, He Z, Li Z, Huang HT, Che J, Nabet B, Zhang T, Fischer ES, Gray NS. Du G, et al. Cell Chem Biol. 2022 Oct 20;29(10):1470-1481.e31. doi: 10.1016/j.chembiol.2022.08.003. Epub 2022 Sep 6. Cell Chem Biol. 2022. PMID: 36070758 Free PMC article.
Structure-guided development of covalent TAK1 inhibitors.
Tan L, Gurbani D, Weisberg EL, Hunter JC, Li L, Jones DS, Ficarro SB, Mowafy S, Tam CP, Rao S, Du G, Griffin JD, Sorger PK, Marto JA, Westover KD, Gray NS. Tan L, et al. Among authors: du g. Bioorg Med Chem. 2017 Feb 1;25(3):838-846. doi: 10.1016/j.bmc.2016.11.035. Epub 2016 Dec 9. Bioorg Med Chem. 2017. PMID: 28011204 Free PMC article.
Studies of TAK1-centered polypharmacology with novel covalent TAK1 inhibitors.
Tan L, Gurbani D, Weisberg EL, Jones DS, Rao S, Singer WD, Bernard FM, Mowafy S, Jenney A, Du G, Nonami A, Griffin JD, Lauffenburger DA, Westover KD, Sorger PK, Gray NS. Tan L, et al. Among authors: du g. Bioorg Med Chem. 2017 Feb 15;25(4):1320-1328. doi: 10.1016/j.bmc.2016.11.034. Epub 2016 Dec 7. Bioorg Med Chem. 2017. PMID: 28038940 Free PMC article.
Specific covalent inhibition of MALT1 paracaspase suppresses B cell lymphoma growth.
Fontán L, Qiao Q, Hatcher JM, Casalena G, Us I, Teater M, Durant M, Du G, Xia M, Bilchuk N, Chennamadhavuni S, Palladino G, Inghirami G, Philippar U, Wu H, Scott DA, Gray NS, Melnick A. Fontán L, et al. Among authors: du g. J Clin Invest. 2018 Oct 1;128(10):4397-4412. doi: 10.1172/JCI99436. Epub 2018 Jul 19. J Clin Invest. 2018. PMID: 30024860 Free PMC article.
Peptide-based covalent inhibitors of MALT1 paracaspase.
Hatcher JM, Du G, Fontán L, Us I, Qiao Q, Chennamadhavuni S, Shao J, Wu H, Melnick A, Gray NS, Scott DA. Hatcher JM, et al. Among authors: du g. Bioorg Med Chem Lett. 2019 Jun 1;29(11):1336-1339. doi: 10.1016/j.bmcl.2019.03.046. Epub 2019 Mar 29. Bioorg Med Chem Lett. 2019. PMID: 30954428
Leveraging Compound Promiscuity to Identify Targetable Cysteines within the Kinome.
Rao S, Gurbani D, Du G, Everley RA, Browne CM, Chaikuad A, Tan L, Schröder M, Gondi S, Ficarro SB, Sim T, Kim ND, Berberich MJ, Knapp S, Marto JA, Westover KD, Sorger PK, Gray NS. Rao S, et al. Among authors: du g. Cell Chem Biol. 2019 Jun 20;26(6):818-829.e9. doi: 10.1016/j.chembiol.2019.02.021. Epub 2019 Apr 11. Cell Chem Biol. 2019. PMID: 30982749 Free PMC article.
Quinoline and thiazolopyridine allosteric inhibitors of MALT1.
Scott DA, Hatcher JM, Liu H, Fu M, Du G, Fontán L, Us I, Casalena G, Qiao Q, Wu H, Melnick A, Gray NS. Scott DA, et al. Among authors: du g. Bioorg Med Chem Lett. 2019 Jul 15;29(14):1694-1698. doi: 10.1016/j.bmcl.2019.05.040. Epub 2019 May 20. Bioorg Med Chem Lett. 2019. PMID: 31129051
3,902 results