How Selective Are Pharmacological Inhibitors of Cell Biology Diagrams Keywords: cyclin-dependent kinase inhibitors, cancer, cell cycle, CDKs, CDK inhibitors. 1. Cyclin-Dependent Kinases (CDKs) Protein phosphorylation is a necessary mechanism to drive numerous cellular processes such as cell division, migration, differentiation and programmed cell death. This process is regulated by many enzymes, including cyclin
Cell cycle inhibitors prevent unchecked proliferation by inhibiting CDKs. These inhibitors fall into two families: INK4 (p15, p16, p18, p19) and Cip/Kip (p21, p27, p57). INK4 proteins inhibit CDK4 and CDK6, blocking cyclin D interaction and preventing G1 progression. Cip/Kip proteins have broader specificity, inhibiting multiple CDKs and
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Cell Cycle Inhibitors Biology Diagrams
First identified as cell cycle inhibitors mediating the growth inhibitory cues of upstream signaling pathways, the cyclin-CDK inhibitors of the Cip/Kip family p21Cip1, p27Kip1, and p57Kip2 have emerged as multifaceted proteins with functions beyond cell cycle regulation. In addition to regulating the cell cycle, Cip/Kip proteins play important roles in apoptosis, transcriptional regulation Example of inhibitors that, in early clinical trials, are targeting cyclin-dependent kinases (cdk s) acting in or outside of the cell cycle.Inhibitors of cdk also inhibit transcription. A key enzyme in the transcription machinery, rna polymerase ii, is phosphorylated by several cdk s 34, 35.The most important regulator is cdk 9/cyclin T. Inhibition of cdk 9/cyclin T by a cdki such as The cell cycle blockade imposed by CDK4/CDK6 inhibitors is not necessarily irreversible 64,66, and this may contribute to disease progression not only upon the recovery of tumour cell

Decision to enter the cell cycle. The E2F inhibitor RB plays a central role in the 'decision' to enter a new cell cycle 2,3. During the prereplicative G1 phase, RB keeps E2F-dependent

Nature Reviews Molecular Cell Biology Biology Diagrams
Major cell cycle regulatory proteins inhibitors (CDK inhibitors) under clinical evaluation. Cyclin-dependent kinases (CDKs) and the regulatory components of these enzymes, called cyclins, regulate the cell cycle by temporally controlling kinase activity and substrate selectivity. (A) CDK-cyclin complexes, comprising 10 cyclins from 4 different
