2io6

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{{STRUCTURE_2io6| PDB=2io6 | SCENE= }}
{{STRUCTURE_2io6| PDB=2io6 | SCENE= }}
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'''Wee1 kinase complexed with inhibitor PD330961'''
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===Wee1 kinase complexed with inhibitor PD330961===
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==Overview==
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A series of N-6 substituted 9-hydroxy-4-phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones were prepared from N-substituted (5-methoxyphenyl)ethenylindoles. The target compounds were tested for their ability to inhibit the G2/M cell cycle checkpoint kinases, Wee1 and Chk1. Analogues with neutral or cationic N-6 side chains were potent dual inhibitors. Acidic side chains provided potent (average IC(50) 0.057muM) and selective (average ratio 223-fold) Wee1 inhibition. Co-crystal structures of inhibitors bound to Wee1 show that the pyrrolo[3,4-c]carbazole scaffold binds in the ATP-binding site, with N-6 substituents involved in H-bonding to conserved water molecules. HT-29 cells treated with doxorubicin and then target compounds demonstrate an active Cdc2/cyclin B complex, inhibition of the doxorubicin-induced phosphorylation of tyrosine 15 of Cdc2 and abrogation of the G2 checkpoint.
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(as it appears on PubMed at http://www.pubmed.gov), where 17869387 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17869387}}
==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 07:42:42 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jul 2 20:54:48 2008''

Revision as of 17:54, 2 July 2008

Image:2io6.png

Template:STRUCTURE 2io6

Wee1 kinase complexed with inhibitor PD330961

Template:ABSTRACT PUBMED 17869387

About this Structure

2IO6 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Synthesis and structure-activity relationships of N-6 substituted analogues of 9-hydroxy-4-phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones as inhibitors of Wee1 and Chk1 checkpoint kinases., Smaill JB, Baker EN, Booth RJ, Bridges AJ, Dickson JM, Dobrusin EM, Ivanovic I, Kraker AJ, Lee HH, Lunney EA, Ortwine DF, Palmer BD, Quin J 3rd, Squire CJ, Thompson AM, Denny WA, Eur J Med Chem. 2007 Aug 6;. PMID:17869387

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