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Blog Archives: Nov 2004 - present
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National Cancer Institute
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WEE1 inhibitor AZD1775
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A small molecule inhibitor of the tyrosine kinase WEE1
with potential antineoplastic sensitizing activity. AZD1775 selectively
targets and inhibits WEE1, a tyrosine kinase that phosphorylates
cyclin-dependent kinase 1 (CDK1, CDC2) to inactivate the CDC2/cyclin B
complex. Inhibition of WEE1 activity prevents the phosphorylation of
CDC2 and impairs the G2 DNA damage checkpoint. This may lead to
apoptosis upon treatment with DNA damaging chemotherapeutic agents.
Unlike normal cells, most p53 deficient or mutated human cancers lack
the G1 checkpoint as p53 is the key regulator of the G1 checkpoint and
these cells rely on the G2 checkpoint for DNA repair to damaged cells.
Annulment of the G2 checkpoint may therefore make p53 deficient tumor
cells more vulnerable to antineoplastic agents and enhance their
cytotoxic effect. Check for active clinical trials using this agent. (NCI Thesaurus)
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