What is a WEE1 inhibitor?

What is a WEE1 inhibitor?

WEE1 is a tyrosine kinase that inhibits the activation of CDK1 and CDK2, and thus, acts as a cell cycle regulator in the G2/M and S phases6,7.

What does WEE1 kinase do?

Wee1 Kinase. Wee1 is a nuclear protein involved in the regulation of the G2/M checkpoint by negatively regulating entry into mitosis by catalyzing an inhibitory tyrosine phosphorylation of the Cdc2/cyclin B kinase complex.

What drugs are PARP inhibitors?

PARP inhibitors. Olaparib (Lynparza), rucaparib (Rubraca), and niraparib (Zejula) are drugs known as a PARP (poly(ADP)-ribose polymerase) inhibitors. PARP enzymes are normally involved in one pathway to help repair damaged DNA inside cells.

What is Zn c3?

Introduction: ZN-c3 is a selective and orally bioavailable small molecule WEE1 inhibitor. WEE1 is a crucial component of the G2/M cell cycle checkpoint preventing cells from entering mitosis to allow repair of DNA damage before cell cycle progression.

Is Wee1 a phosphatase?

Wee1 is a kinase that delays mitosis via inhibitory phosphorylation of Cdk1, while Cdc25 is a phosphatase that promotes mitosis by removing the inhibitory phosphorylation. Although Wee1 and Cdc25 are conserved proteins, it has remained unclear whether their functions and regulation are conserved across diverse species.

How is Wee1 phosphorylated?

It is inactivated by phosphorylation through Wee1 and activated by the phosphatase Cdc25C. Cdc25C in turn is activated by Polo kinase and inactivated by Chk1. Thus in S. pombe Wee1 regulation is mainly under the control of phosphorylation through the polarity kinase, Pom1’s, pathway including Cdr2 and Cdr1.

Is Avastin a PARP inhibitor?

Avastin is an anti-angiogenic drug that interferes with the development of blood vessels that tumors need to thrive. Lynparza is a PARP inhibitor, which can be lethal to cancer cells by hindering their ability to repair their damaged DNA.

Is Zytiga a PARP inhibitor?

The PARP inhibitors will impact “refractory patients who have failed standard-of-care therapies,” notes Mesfin Tegenu, R.Ph., president of PerformRx, LLC. First-line treatment will be with antiandrogens or taxanes, he explains: Zytiga, Yonsa, Jevtana (cabazitaxel), Taxotere (docetaxel) or Xtandi.