2j9m

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{{STRUCTURE_2j9m| PDB=2j9m | SCENE= }}
{{STRUCTURE_2j9m| PDB=2j9m | SCENE= }}
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'''CRYSTAL STRUCTURE OF CDK2 IN COMPLEX WITH MACROCYCLIC AMINOPYRIMIDINE'''
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===CRYSTAL STRUCTURE OF CDK2 IN COMPLEX WITH MACROCYCLIC AMINOPYRIMIDINE===
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==Overview==
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X-ray structures from CDK2-aminopyrimidine inhibitor complexes led to the idea to stabilize the active conformation of aminopyrimidine inhibitors by incorporating the recognition site into a macrocyclic framework. A modular synthesis approach that relies on a new late-stage macrocyclization protocol that enables fast and efficient synthesis of macrocyclic aminopyrimidines was developed. A set of structurally diverse derivatives was prepared. Macrocyclic aminopyrimidines were shown to be multitarget inhibitors of CDK1/2 and VEGF-RTKs. In addition, potent antiproliferative activities toward various human tumor cells and a human tumor xenograft model were demonstrated.
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(as it appears on PubMed at http://www.pubmed.gov), where 17131463 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17131463}}
==About this Structure==
==About this Structure==
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[[Category: Serine/threonine-protein kinase]]
[[Category: Serine/threonine-protein kinase]]
[[Category: Transferase]]
[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 08:33:44 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 07:15:47 2008''

Revision as of 04:15, 28 July 2008

Image:2j9m.png

Template:STRUCTURE 2j9m

CRYSTAL STRUCTURE OF CDK2 IN COMPLEX WITH MACROCYCLIC AMINOPYRIMIDINE

Template:ABSTRACT PUBMED 17131463

About this Structure

2J9M is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Macrocyclic Aminopyrimidines as Multitarget CDK and VEGF-R Inhibitors with Potent Antiproliferative Activities., Lucking U, Siemeister G, Schafer M, Briem H, Kruger M, Lienau P, Jautelat R, ChemMedChem. 2007 Jan 15;2(1):63-77. PMID:17131463

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