Description

Lead Optimisation - CRT Discovery Laboratories

Cdc7 serine/threonine kinase plays an essential role in assembly of the pre-replicative complex (that renders origins ‘licensed’ for DNA synthesis) and G1/S transition through phosphorylation of MCM proteins (replicative helicases). Inhibition of Cdc7 has been demonstrated to selectively induce cell death in tumours versus induce a reversible cell cycle arrest in non-malignant cells. Two series of novel, selective small molecule inhibitors which exhibit low nM activity against Cdc7 and cellular efficacy (apoptosis) have been developed. Biomarker and phenotypic assays have been established. CRT is now seeking a commercial partner to progress this programme under a licensing or co-development model.

Download the PDF of Inhibitors of Cdc7

For more information please contact

Dr Stephen Myatt

+44 (0) 20 3469 6300 .(JavaScript must be enabled to view this email address)