WebJul 13, 2024 · BSJ-4-116 exhibits potent antiproliferative effects in Kelly CDK12 C1039F. It also decreases the level of CDK12 protein, regardless of the mutational status of the cell line. Moreover, it inhibits the growth of T-ALL cells (Jurkat and MOLT-4 cells) and sensitizes them to PARP inhibition. BSJ-4-116 also regulates DDR genes via poly (adenylation ... WebMay 14, 2024 · CDK12 inhibition primarily affects the expression of genes involved in the DNA damage response, although suppression of super-enhancer-associated genes has been observed at high inhibitor ...
Targeting CDK12 for Cancer Therapy: Function, …
WebCDK12 is a known regulator of transcription, specifically involved in transcriptional elongation, rather than at the initiation of transcription . To understand the mechanism by … WebAn increasing number of studies point to CDK12 inhibition as an effective strategy to inhibit tumour growth, and synthetic lethal interactions have been described with MYC, EWS/FLI and PARP/CHK1 inhibition. Herein, we discuss the present literature on CDK12 in cell function and human cancer, highlighting important roles for CDK12 as a clinical ... laundry cottages acklington
Cyclin-Dependent Kinase 12, Immunity, and …
WebApr 8, 2024 · Preclinical Data from Oral CDK12 Inhibitor Program. Syros designed a series of CDK12 inhibitors that were profiled in biochemical and cellular assays. The data presented at AACR detail for the first time the potency, selectivity, and anti-tumor activity from a representative member of the class, which exhibited low nanomolar potency and ... WebNational Center for Biotechnology Information WebAn increasing number of studies point to CDK12 inhibition as an effective strategy to inhibit tumour growth, and synthetic lethal interactions have been described with MYC, … laundry counter sink