1oky

From Proteopedia

Revision as of 13:52, 30 October 2007

STRUCTURE OF HUMAN PDK1 KINASE DOMAIN IN COMPLEX WITH STAUROSPORINE

Overview

PDK1 (3-phosphoinositide-dependent protein kinase-1) is a member of the, AGC (cAMP-dependent, cGMP-dependent, protein kinase C) family of protein, kinases, and has a key role in insulin and growth-factor signalling, through phosphorylation and subsequent activation of a number of other AGC, kinase family members, such as protein kinase B. The staurosporine, derivative UCN-01 (7-hydroxystaurosporine) has been reported to be a, potent inhibitor for PDK1, and is currently undergoing clinical trials for, the treatment of cancer. Here, we report the crystal structures of, staurosporine and UCN-01 in complex with the kinase domain of PDK1. We, show that, although staurosporine and UCN-01 interact with the PDK1 active, site in an overall similar manner, the UCN-01 7-hydroxy group, which is, not ... [(full description)]

About this Structure

1OKY is a [Single protein] structure of sequence from [Homo sapiens] with SO4, STU and GOL as [ligands]. Active as [Transferred entry: 2.7.11.1], with EC number [2.7.1.37]. Structure known Active Site: AC9. Full crystallographic information is available from [OCA].

Reference

Structural basis for UCN-01 (7-hydroxystaurosporine) specificity and PDK1 (3-phosphoinositide-dependent protein kinase-1) inhibition., Komander D, Kular GS, Bain J, Elliott M, Alessi DR, Van Aalten DM, Biochem J. 2003 Oct 15;375(Pt 2):255-62. PMID:12892559

Page seeded by OCA on Tue Oct 30 15:57:34 2007