Chemical inhibitors of cyclin-dependent kinases

L Meijer - Trends in Cell Biology, 1996 - Elsevier
Trends in Cell Biology, 1996Elsevier
Transient activation of cyclin-dependent kinases (CDKs) is responsible for transition through
the successive phases of the cell-division cycle. Major changes in the expression and
regulation of CDKs have been described in human tumours. Enzymatic screening is starting
to uncover chemical inhibitors of CDKs that arrest the cell cycle at various steps. This review
summarizes our knowledge of the first generation inhibitors, their molecular mechanisms of
action and their effects on the cell cycle and apoptosis, and discusses their potential as …
Transient activation o f cyclin-dependent kinases (CDKs) is responsible for transition through the successive phases of the cell-division cycle. Major changes in the expression and regulation of CDKs have been described in human tumours. Enzymatic screening is starting to uncover chemical inhibitors o f CDKs that arrest the cell cycle at various steps. This review summarizes our knowledge of the first generation inhibitors, their molecular mechanisms of action and their effects on the cell cycle and apoptosis, and discusses their potential as synchronizing agents, as ligands for affinity chromatography and as therapeutic agents.
Elsevier