Cell Cycle/Checkpoint
The cell cycle is consisted of 4 main phases: Gap 1 (G1), DNA replication (S), Gap 2 (G2), and mitosis (M). There are “checkpoints” mechanism regulates the transition between these phases, at the G1/S boundary, in the S-phase and during G2/M phases. Cell can only pass through these checkpoints when signaling factors are activated and free of DNA damage. Important proteins that control cell cycle events and checkpoints are cullins, cyclins, cyclin-dependent kinases (Cdks), p53 and their inhibitors etc. Cdks family (Cdk2, Cdk3, Cdk4 and Cdk6) are Ser/Thr kinases that regulate cell cycle progression in association with cyclin binding partners (cyclin D, cyclin E and cyclin A) during all four phases. p53 halts the cell cycle if the DNA is damaged and allowing time for DNA repair to progress; it can also initiate apoptosis if DNA damage is too severe to be repaired.
- A8717 THZ21 CitationTarget: Cyclin-Dependent KinasesSummary: CDK7 inhibitor
- B4892 TAI-1Target: Hec1Summary: Hec1 inhibitor, potent, first-in-class
- B5860 TAK960Target: PLKSummary: Oral and selective PLK1 inhibitor
- B5880 CCT244747Target: ChkSummary: Potent and selective CHK1 inhibitor
- B5881 RI-2Target: RAD51Summary: Optimized reversible RAD51 inhibitor
- B1162 FRAX5971 CitationTarget: PAKSummary: PAK inhibitor,potent and ATP-competitive
- B2169 IPA-31 CitationTarget: PAKSummary: Non-ATP competitive Pak1 inhibitor
- B1463 KPT-276Target: nuclear export|CRM1Summary: inhibitor of nuclear export (SINE) and CRM1, orally bioavailable
- B1088 LY2606368Target: ChkSummary: CHK1 inhibitor
- A8882 THZ112 CitationTarget: Cyclin-Dependent KinasesSummary: Covalent CDK7 inhibitor,potent and selective