Cyclin-dependent kinases
| Cyclin-dependent kinases | ||
|---|---|---|
| Enzyme classification | ||
| EC, category | 2.7.11.22 , protein kinase | |
| Substrate | ATP + protein | |
| Products | ADP + phosphoprotein | |
Cyclin-dependent kinases ( CDKs ) are a family of protein kinases that play a role in both transcription and control of the cell cycle . Protein kinases are enzymes that phosphorylate other proteins at specific locations .
There are 20 different CDKs in humans, but only six to eight in yeast.
CDKs form complexes with the cyclins , which undergo cell cycle-dependent concentration changes. The cyclin-dependent kinases are only active in connection with their associated cyclin. This allows the activity of the CDKs in the cell to be timed and regulated. This enables them to perform their function in certain phases of the cell cycle, which are linked to the cyclical changes in the concentration of the cyclins. One example is the mitosis-promoting factor formed from CDK1 and cyclin B , which controls the initiation of mitosis .
Due to the essential role that cyclin-dependent kinases play in controlling the cell cycle and thus in the proliferation of cells, various substances that inhibit CDKs (so-called CDK inhibitors ) are being tested as potential cancer therapeutics. The first member of the CDK inhibitor group is palbociclib . It inhibits CDK4 and CDK6 and is approved for the treatment of hormone receptor-positive / HER2-negative locally advanced or metastatic breast cancer. Experimental CDK inhibitors are Abemciclib , Briciclib , Dinaciclib , Milciclib , Ribociclib , Riviciclib , Roniciclib , Seliciclib and Voruciclib .
Individual evidence
- ↑ Phylogenetic analysis of CDK and cyclin proteins in premetazoan lineages . Cao et al. (2014), doi: 10.1186 / 1471-2148-14-10
- ↑ Jan Koolman, Klaus-Heinrich Röhm: Pocket Atlas of Biochemistry. 215 color plates by Jürgen Wirth. 3rd completely revised and expanded edition. Georg Thieme Verlag, Stuttgart et al. 2002, ISBN 3-13-759403-0 , p. 394.
- ↑ Marcos Malumbres, Mariano Barbacid : Cell cycle, CDKs and cancer: a changing paradigm. In: Nature Reviews Cancer. 9, 2009, p. 153, doi: 10.1038 / nrc2602 .