2j9m: Difference between revisions

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[[Image:2j9m.jpg|left|200px]]
{{Seed}}
[[Image:2j9m.png|left|200px]]


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{{STRUCTURE_2j9m|  PDB=2j9m  |  SCENE=  }}  
{{STRUCTURE_2j9m|  PDB=2j9m  |  SCENE=  }}  


'''CRYSTAL STRUCTURE OF CDK2 IN COMPLEX WITH MACROCYCLIC AMINOPYRIMIDINE'''
===CRYSTAL STRUCTURE OF CDK2 IN COMPLEX WITH MACROCYCLIC AMINOPYRIMIDINE===




==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.
The line below this paragraph, {{ABSTRACT_PUBMED_17131463}}, adds the Publication Abstract to the page
(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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