This old version of Proteopedia is provided for student assignments while the new version is undergoing repairs. Content and edits done in this old version of Proteopedia after March 1, 2026 will eventually be lost when it is retired in about June of 2026.

Apply for new accounts at the new Proteopedia. Your logins will work in both the old and new versions.


1urw

From Proteopedia

Revision as of 17:31, 12 November 2007 by OCA (Talk | contribs)
Jump to: navigation, search
Image:1urw.gif

1urw, resolution 1.6Å

Drag the structure with the mouse to rotate

CDK2 IN COMPLEX WITH AN IMIDAZO[1,2-B]PYRIDAZINE

Overview

Modification of imidazo[1,2-a]pyridine CDK inhibitors lead to, identification of less lipophilic imidazo[1,2-b]pyridazine series of CDK, inhibitors. Although several equivalent compounds from these two series, have similar structure and show similar CDK activity, the SAR of the two, series differs significantly. Protein inhibitor structure determination, has confirmed differences in binding mode and given some understanding of, these differences in SAR. Potent and selective imidazo[1,2-b]pyridazine, inhibitors of CDK2 have been identified, which show >1 microM plasma, levels following a 2mg/kg oral dose to mice.

About this Structure

1URW is a Single protein structure of sequence from Homo sapiens with ACE and I1P as ligands. Active as Transferred entry: 2.7.11.1, with EC number 2.7.1.37 Structure known Active Site: AC2. Full crystallographic information is available from OCA.

Reference

Imidazo[1,2-b]pyridazines: a potent and selective class of cyclin-dependent kinase inhibitors., Byth KF, Cooper N, Culshaw JD, Heaton DW, Oakes SE, Minshull CA, Norman RA, Pauptit RA, Tucker JA, Breed J, Pannifer A, Rowsell S, Stanway JJ, Valentine AL, Thomas AP, Bioorg Med Chem Lett. 2004 May 3;14(9):2249-52. PMID:15081018

Page seeded by OCA on Mon Nov 12 19:38:03 2007

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/1urw"
Personal tools