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Rationally designed chimeric PI3K-BET bromodomain inhibitors elicit curative responses in MYC-driven lymphoma.
Oh DH, Ma X, Hogg SJ, He J, Kearney C, Brasacchio D, Susanto O, Maher B, Jennings IG, Newbold A, Fraser P, Gruber E, Kats LM, Gregory GP, Johnstone RW, Thompson PE, Shortt J. Oh DH, et al. Proc Natl Acad Sci U S A. 2023 Sep 5;120(36):e2306414120. doi: 10.1073/pnas.2306414120. Epub 2023 Aug 29. Proc Natl Acad Sci U S A. 2023. PMID: 37643213 Free PMC article.
Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis.
Nguyen M, Marcellus RC, Roulston A, Watson M, Serfass L, Murthy Madiraju SR, Goulet D, Viallet J, Bélec L, Billot X, Acoca S, Purisima E, Wiegmans A, Cluse L, Johnstone RW, Beauparlant P, Shore GC. Nguyen M, et al. Proc Natl Acad Sci U S A. 2007 Dec 4;104(49):19512-7. doi: 10.1073/pnas.0709443104. Epub 2007 Nov 26. Proc Natl Acad Sci U S A. 2007. PMID: 18040043 Free PMC article.
Reconstitution in yeast confirmed that obatoclax acts on the pathway and overcomes BCL-2-, BCL-XL-, BCL-w-, and MCL-1-mediated resistance to BAX or BAK. The compound potently interfered with the direct interaction between MCL-1 and BAK in intact mitochondrial outer membran …
Reconstitution in yeast confirmed that obatoclax acts on the pathway and overcomes BCL-2-, BCL-XL-, BCL-w-, and MCL-1-mediated resist …