Cell Cycle/Checkpoint - PLK
The cell cycle is a regulatory system that controls the proper order and timing of cellular growth and division events. Mutation in the proteins regulating the cell cycle, leads to uncontrolled cell division or propagation of damaged DNA which contributes to genomic instability and oncogenesis.
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.
- B5860 TAK960Target: PLKSummary: Oral and selective PLK1 inhibitor
- B5857 SBE 13 HClTarget: PLKSummary: Inactive Plk1 inhibitor
- B4094 NMS-1286937Target: PLKSummary: PLK1 inhibitor, orally bioavailable
- B1288 RigosertibTarget: PI3K|PLKSummary: PI3K/PLK1 inhibitor
- A8681 Ro3280Target: PLKSummary: PLK1 inhibitor,potent and highly selective
- A8680 MLN0905Target: PLKSummary: Potent PLK1 inhibitor
- A8441 GSK4613643 CitationTarget: PLKSummary: Plk1 inhibitor
- A1404 Rigosertib sodium salt1 CitationTarget: PLKSummary: Plk1 inhibitor
- A3965 BI 25361 CitationTarget: PLK|Bromodomain-containing proteins(BRDs)Summary: Plk1 inhibitor,potent and ATP-competitive
- A3732 PoloxinTarget: PLKSummary: PLK1 inhibitor