Aug 2026· Nature Chemical Biology· 0 citations· 72 references
Medicine
TL;DR
The adaptive plasticity of cell-cycle control in cancer cells is discussed and current strategies to target newly emerging CDK2 druggable pockets are highlighted, with an emphasis on chemical biology approaches, aiming to inspire the next generation of CDK2 inhibitors and kinase-targeted therapies more broadly.
The molecular functions of the CDK9/positive transcription elongation factor b (P-TEFb) axis, its role in super-enhancer-driven oncogenic programs, and the mechanisms by which CDK9 inhibition promotes apoptosis, epigenetic derepression, and tumor microenvironment remodeling are summarized.
Ti-Yao Liu, Zhongran Liu, Wen-Jing Wei et al.· Expert opinion on therapeuti...· 0 citations
Mechanistic investigations revealed that 8j induces G1 phase cell cycle arrest and promotes apoptosis, which was corroborated by the observed concentration-dependent downregulation of key cell cycle regulators, including CDK4 and cyclin D1.
Chao Lin, Shao-Feng Sun, Hua-Teng Zhang et al.· Journal of Enzyme Inhibition...· 0 citations
Cyclin-dependent kinase 4/6 (CDK4/6), as an important kinase regulating cell cycle progression, exhibits functional abnormalities closely associated with the initiation and progression of various cancers. Consequently, targeted inhibition of CDK4/6 represents a valuable and promising therapeutic strategy for cancer tre...
Cun Wang, Yan-Hua Zhang, Shu-Yun Bao et al.· Bioorganic chemistry (Print)· 0 citations
Simultaneous inhibition of CDK2 and TRKA presents a promising therapeutic avenue for cancer treatment, capitalizing on the critical roles of CDK2 in cell cycle regulation and TRKA in tumor cell survival and progression. In continuation of our previous work on dual CDK2/TRKA inhibitors, two series of pyrazolo[1,5-a]pyri...
Mohamed H. Attia, Deena S. Lasheen, Nermin Samir et al.· RSC Advances· 0 citations
Two main ways in which CDK4/6 inhibitors exert their effects are reviewed, one is to directly block the cell cycle, and the other is to reshape the immune microenvironment.
Qi-Ya Jing· International Journal of Bio...· 0 citations
Competitive docking against the allosteric sites of AKT2 and AKT3 revealed a consistent preference for AKT1 across all three compounds, with a magnitude closely comparable to that of the reference allosteric ligand Inhibitor VIII, whose experimentally determined isoform rank order the protocol reproduced.
Raju Das, Armin Sultana, Kantu Das et al.· Journal of Molecular Graphic...· 0 citations
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