Journal
EXPERT OPINION ON INVESTIGATIONAL DRUGS
Volume 17, Issue 9, Pages 1331-1340Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1517/13543784.17.9.1331
Keywords
checkpoint kinase; DNA damage; kinase inhibitor; potentiation; sensitisation
Categories
Ask authors/readers for more resources
Background: Checkpoint kinase 1 (Chk1), a serine/threonine kinase, functions as a regulatory kinase in cell cycle progression and is a critical effector of the DNA-damage response. Inhibitors of Chk1 are known to sensitise tumours to a variety of DNA-damaging agents and increase efficacy in preclinical models. Objective: The most advanced agents are now in Phase I clinical trials; the preclinical profiles of these drugs are compared and contrasted, together with a discussion of some of the opportunities and challenges facing this potentially revolutionary approach to cancer therapy. Methods: A review of the publications and presentations on XL-844, AZD7762 and PF-477736. Results/conclusions: Chk kinases are part of the DNA damage recognition and response pathways and as such represent attractive targets. Agents that target checkpoint kinases have demonstrated impressive evidence preclinically that this approach will provide tumour-specific potentiating agents and may have broad therapeutic utility.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available