Activating p53 and Inhibiting Superenhancers to Cure Leukemia
TRENDS IN PHARMACOLOGICAL SCIENCES
Authors: Ball, Brian; Abdel-Wahab, Omar
Abstract
In a recent study, Minzel and colleagues identified a novel series of molecules that inhibit casein kinase 1 alpha(CK1 alpha), CDK7, and CDK9, resulting in p53 activation and preferential inhibition of superenhancer (SE)-driven transcription. This study demonstrates a highly effective therapeutic strategy combining p53 activation with suppression of SEs to promote the cooperative killing of leukemic cells.
Early evidence of dose-dependent pharmacodynamic activity following treatment with SY-5609, a highly selective and potent oral CDK7 inhibitor, in patients with advanced solid tumors
EUROPEAN JOURNAL OF CANCER
Authors: Papadopoulos, K.; Sharma, M.; Hamilton, E.; Richardson, D.; Bashir, B.; Hodgson, G.; Ke, N.; Kang-Fortner, Q.; Zhou, L.; Zamboni, W.; Jolin, H.; Madigan, C.; Kelly, M.; Roth, D.
Abstract