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Targeted kinase degradation via the KLHDC2 ubiquitin E3 ligase.
Kim Y, Seo P, Jeon E, You I, Hwang K, Kim N, Tse J, Bae J, Choi HS, Hinshaw SM, Gray NS, Sim T. Kim Y, et al. Among authors: gray ns. Cell Chem Biol. 2023 Nov 16;30(11):1414-1420.e5. doi: 10.1016/j.chembiol.2023.07.008. Epub 2023 Aug 10. Cell Chem Biol. 2023. PMID: 37567174 Free PMC article.
The rise of degrader drugs.
Teng M, Gray NS. Teng M, et al. Among authors: gray ns. Cell Chem Biol. 2023 Aug 17;30(8):864-878. doi: 10.1016/j.chembiol.2023.06.020. Epub 2023 Jul 25. Cell Chem Biol. 2023. PMID: 37494935 Free article. Review.
Activating p53Y220C with a Mutant-Specific Small Molecule.
Zhu X, Byun WS, Pieńkowska DE, Nguyen KT, Gerhartz J, Geng Q, Qiu T, Zhong J, Jiang Z, Wang M, Sarott RC, Hinshaw SM, Zhang T, Attardi LD, Nowak RP, Gray NS. Zhu X, et al. Among authors: gray ns. bioRxiv [Preprint]. 2024 Oct 28:2024.10.23.619961. doi: 10.1101/2024.10.23.619961. bioRxiv. 2024. PMID: 39554093 Free PMC article. Preprint.
Exploration of the tunability of BRD4 degradation by DCAF16 trans-labelling covalent glues.
Hassan MM, Li YD, Ma MW, Teng M, Byun WS, Puvar K, Lumpkin R, Sandoval B, Rutter JC, Jin CY, Wang MY, Xu S, Schmoker AM, Cheong H, Groendyke BJ, Qi J, Fischer ES, Ebert BL, Gray NS. Hassan MM, et al. Among authors: gray ns. Eur J Med Chem. 2024 Dec 5;279:116904. doi: 10.1016/j.ejmech.2024.116904. Epub 2024 Sep 24. Eur J Med Chem. 2024. PMID: 39341093 Free article.
USP9X mediates an acute adaptive response to MAPK suppression in pancreatic cancer but creates multiple actionable therapeutic vulnerabilities.
Perurena N, Lock R, Davis RA, Raghavan S, Pilla NF, Ng R, Loi P, Guild CJ, Miller AL, Sicinska E, Cleary JM, Rubinson DA, Wolpin BM, Gray NS, Santagata S, Hahn WC, Morton JP, Sansom OJ, Aguirre AJ, Cichowski K. Perurena N, et al. Among authors: gray ns. Cell Rep Med. 2023 Apr 18;4(4):101007. doi: 10.1016/j.xcrm.2023.101007. Epub 2023 Apr 7. Cell Rep Med. 2023. PMID: 37030295 Free PMC article.
Development of a highly potent and selective degrader of LRRK2.
Hatcher JM, Zwirek M, Sarhan AR, Vatsan PS, Tonelli F, Alessi DR, Davies P, Gray NS. Hatcher JM, et al. Among authors: gray ns. Bioorg Med Chem Lett. 2023 Oct 1;94:129449. doi: 10.1016/j.bmcl.2023.129449. Epub 2023 Aug 15. Bioorg Med Chem Lett. 2023. PMID: 37591317
Targeted degradation of oncogenic KRASG12V triggers antitumor immunity in lung cancer models.
Li D, Geng K, Hao Y, Gu J, Kumar S, Olson AT, Kuismi CC, Kim HM, Pan Y, Sherman F, Williams AM, Li Y, Li F, Chen T, Thakurdin C, Ranieri M, Meynardie M, Levin DS, Stephens J, Chafitz A, Chen J, Donald-Paladino MS, Powell JM, Zhang ZY, Chen W, Ploszaj M, Han H, Gu S, Zhang T, Hu B, Nacev BA, Kaiza ME, Berger AH, Wang X, Li J, Sun X, Liu Y, Zhang X, Bruno TC, Gray NS, Nabet B, Wong KK, Zhang H. Li D, et al. Among authors: gray ns. J Clin Invest. 2024 Dec 24:e174249. doi: 10.1172/JCI174249. Online ahead of print. J Clin Invest. 2024. PMID: 39718828 Free article.
560 results