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Orally bioavailable CDK9/2 inhibitor shows mechanism-based therapeutic potential in MYCN-driven neuroblastoma.
Poon E, Liang T, Jamin Y, Walz S, Kwok C, Hakkert A, Barker K, Urban Z, Thway K, Zeid R, Hallsworth A, Box G, Ebus ME, Licciardello MP, Sbirkov Y, Lazaro G, Calton E, Costa BM, Valenti M, De Haven Brandon A, Webber H, Tardif N, Almeida GS, Christova R, Boysen G, Richards MW, Barone G, Ford A, Bayliss R, Clarke PA, De Bono J, Gray NS, Blagg J, Robinson SP, Eccles SA, Zheleva D, Bradner JE, Molenaar J, Vivanco I, Eilers M, Workman P, Lin CY, Chesler L. Poon E, et al. Among authors: chesler l. J Clin Invest. 2020 Nov 2;130(11):5875-5892. doi: 10.1172/JCI134132. J Clin Invest. 2020. PMID: 33016930 Free PMC article.
Sulfopin is a covalent inhibitor of Pin1 that blocks Myc-driven tumors in vivo.
Dubiella C, Pinch BJ, Koikawa K, Zaidman D, Poon E, Manz TD, Nabet B, He S, Resnick E, Rogel A, Langer EM, Daniel CJ, Seo HS, Chen Y, Adelmant G, Sharifzadeh S, Ficarro SB, Jamin Y, Martins da Costa B, Zimmerman MW, Lian X, Kibe S, Kozono S, Doctor ZM, Browne CM, Yang A, Stoler-Barak L, Shah RB, Vangos NE, Geffken EA, Oren R, Koide E, Sidi S, Shulman Z, Wang C, Marto JA, Dhe-Paganon S, Look T, Zhou XZ, Lu KP, Sears RC, Chesler L, Gray NS, London N. Dubiella C, et al. Among authors: chesler l. Nat Chem Biol. 2021 Sep;17(9):954-963. doi: 10.1038/s41589-021-00786-7. Epub 2021 May 10. Nat Chem Biol. 2021. PMID: 33972797 Free PMC article.
The ALK inhibitor PF-06463922 is effective as a single agent in neuroblastoma driven by expression of ALK and MYCN.
Guan J, Tucker ER, Wan H, Chand D, Danielson LS, Ruuth K, El Wakil A, Witek B, Jamin Y, Umapathy G, Robinson SP, Johnson TW, Smeal T, Martinsson T, Chesler L, Palmer RH, Hallberg B. Guan J, et al. Among authors: chesler l. Dis Model Mech. 2016 Sep 1;9(9):941-52. doi: 10.1242/dmm.024448. Epub 2016 Jul 7. Dis Model Mech. 2016. PMID: 27483357 Free PMC article.
106 results