2e9n

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[[Image:2e9n.jpg|left|200px]]
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{{STRUCTURE_2e9n| PDB=2e9n | SCENE= }}
{{STRUCTURE_2e9n| PDB=2e9n | SCENE= }}
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'''Structure of h-CHK1 complexed with A767085'''
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===Structure of h-CHK1 complexed with A767085===
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==Overview==
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A new class of checkpoint kinase 1 (CHK-1) inhibitors bearing a 1,4-dihydroindeno[1,2-c]pyrazole core was developed after initial hits from high throughput screening. The efficient hit-to-lead process was facilitated by X-ray crystallography and led to potent inhibitors (&lt;10nM) against CHK-1. X-ray co-crystal structures of bound inhibitors demonstrated that two sub-series of this class of compounds, exemplified by 21 and 41, exhibit distinctive hydrogen bonding patterns in the specificity pocket of the active site. Two compounds, 41 and 43, were capable of potentiating doxorubicin and camptothecin, both DNA-damaging agents, in cell proliferation assays (MTS and soft agar assays) and abrogating G2/M checkpoint in a mechanism-based FACS assay.
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(as it appears on PubMed at http://www.pubmed.gov), where 17287122 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17287122}}
==About this Structure==
==About this Structure==
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[[Category: Protein-inhibitor complex]]
[[Category: Protein-inhibitor complex]]
[[Category: Transferase]]
[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 02:12:01 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 12:20:43 2008''

Revision as of 09:20, 28 July 2008

Image:2e9n.png

Template:STRUCTURE 2e9n

Structure of h-CHK1 complexed with A767085

Template:ABSTRACT PUBMED 17287122

About this Structure

2E9N is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors., Tong Y, Claiborne A, Stewart KD, Park C, Kovar P, Chen Z, Credo RB, Gu WZ, Gwaltney SL 2nd, Judge RA, Zhang H, Rosenberg SH, Sham HL, Sowin TJ, Lin NH, Bioorg Med Chem. 2007 Apr 1;15(7):2759-67. Epub 2007 Jan 17. PMID:17287122

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