2r3k

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{{STRUCTURE_2r3k| PDB=2r3k | SCENE= }}
{{STRUCTURE_2r3k| PDB=2r3k | SCENE= }}
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'''Crystal Structure of Cyclin-Dependent Kinase 2 with inhibitor'''
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===Crystal Structure of Cyclin-Dependent Kinase 2 with inhibitor===
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==Overview==
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CDK2 inhibitors containing the related bicyclic heterocycles pyrazolopyrimidines and imidazopyrazines were discovered through high-throughput screening. Crystal structures of inhibitors with these bicyclic cores and two more related ones show that all but one have a common binding mode featuring two hydrogen bonds (H-bonds) to the backbone of the kinase hinge region. Even though ab initio computations indicated that the imidazopyrazine core would bind more tightly to the hinge, pyrazolopyrimidines gain an advantage in potency through participation of N4 in an H-bond network involving two catalytic residues and bridging water molecules. Further insight into inhibitor/CDK2 interactions was gained from analysis of additional crystal structures. Significant gains in potency were obtained by optimizing the fit of hydrophobic substituents to the gatekeeper region of the ATP binding site. The most potent inhibitors have good selectivity. (c) 2007 Wiley Periodicals, Inc. Biopolymers, 2007.
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{{ABSTRACT_PUBMED_17937404}}
==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 16:11:15 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 16:30:32 2008''

Revision as of 13:30, 29 July 2008

Image:2r3k.png

Template:STRUCTURE 2r3k

Crystal Structure of Cyclin-Dependent Kinase 2 with inhibitor

Template:ABSTRACT PUBMED 17937404

About this Structure

2R3K is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Structure-guided discovery of cyclin-dependent kinase inhibitors., Fischmann TO, Hruza A, Duca JS, Ramanathan L, Mayhood T, Windsor WT, Le HV, Guzi TJ, Dwyer MP, Paruch K, Doll RJ, Lees E, Parry D, Seghezzi W, Madison V, Biopolymers. 2007 Oct 15;. PMID:17937404

Page seeded by OCA on Tue Jul 29 16:30:32 2008

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