Targeting the cell division cycle in cancer: CDK and cell cycle checkpoint kinase inhibitors.
The cyclin-dependent kinase (CDK) family of serine/threonine kinases regulate progression through each stage of the cell division cycle and as such are major targets for deregulation in cancer. This has led to the development of several small-molecule inhibitors of CDKs as potential therapeutic agents for the treatment of this disease. Progression through the cell cycle is also monitored at several positions known as cell cycle checkpoints, two of which occur during G1 and G2 in response to DNA damage. These are often defective in cancer, leading to the suggestion that inhibition of one or both of the cell cycle checkpoint kinases CHK1 and CHK2 may drive a cancer cell that already has defects in its cell cycle checkpoints towards death.
Collins
Ian
I
Cancer Research UK Centre for Cancer Therapeutics at The Institute of Cancer Research, 15 Cotswold Road, Sutton SM2 5NG, UK.
Garrett
Michelle D
MD
D002453:Cell Cycle / Q000187:drug effects* / Q000502:physiology; D018844:Cyclin-Dependent Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D007093:Imidazoles / Q000737:chemistry / Q000627:therapeutic use; D007211:Indoles / Q000737:chemistry / Q000627:therapeutic use; D015394:Molecular Structure; D009369:Neoplasms / Q000188:drug therapy* / Q000201:enzymology / Q000503:physiopathology; D010636:Phenols / Q000737:chemistry / Q000627:therapeutic use; D010879:Piperazines / Q000737:chemistry / Q000627:therapeutic use; D047428:Protein Kinase Inhibitors / Q000737:chemistry / Q000627:therapeutic use*; D011725:Pyridines / Q000737:chemistry / Q000627:therapeutic use; D011743:Pyrimidines / Q000737:chemistry / Q000627:therapeutic use
C480542:BMI 1026; D007093:Imidazoles; D007211:Indoles; D010636:Phenols; D010879:Piperazines; D047428:Protein Kinase Inhibitors; D011725:Pyridines; D011743:Pyrimidines; C433985:SU 9516; D018844:Cyclin-Dependent Kinases; C500026:palbociclib