1tvo

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[[Image:1tvo.gif|left|200px]]
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{{Seed}}
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[[Image:1tvo.png|left|200px]]
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{{STRUCTURE_1tvo| PDB=1tvo | SCENE= }}
{{STRUCTURE_1tvo| PDB=1tvo | SCENE= }}
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'''The structure of ERK2 in complex with a small molecule inhibitor'''
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===The structure of ERK2 in complex with a small molecule inhibitor===
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==Overview==
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Selective inhibition of extracellular signal-regulated kinase (ERK) represents a potential approach for the treatment of cancer and other diseases; however, no selective inhibitors are currently available. Here, we describe an ERK-selective inhibitor, FR180204, and determine the structural basis of its selectivity. FR180204 inhibited the kinase activity of ERK1 and ERK2, with K(i) values 0.31 and 0.14microM, respectively. Lineweaver-Burk analysis of the binding interaction revealed that FR180204 acted as competitive inhibitor of ATP. In mink lung epithelial Mv1Lu cells, FR180204 inhibited TGFbeta-induced luciferase-expression. X-ray crystal structure analysis of the human ERK2/FR180204 complex revealed that Q105, D106, L156, and C166, which form the ATP-binding pocket on ERK, play important roles in the drug/protein interaction. These results suggest that FR180204 is an ERK-selective and cell-permeable inhibitor, and could be useful for elucidating the roles of ERK as well as for drug development.
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The line below this paragraph, {{ABSTRACT_PUBMED_16139248}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 16139248 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16139248}}
==About this Structure==
==About this Structure==
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[[Category: Kinase]]
[[Category: Kinase]]
[[Category: Protein-inhibitor complex]]
[[Category: Protein-inhibitor complex]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 10:25:42 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 02:20:36 2008''

Revision as of 23:20, 28 July 2008

Image:1tvo.png

Template:STRUCTURE 1tvo

The structure of ERK2 in complex with a small molecule inhibitor

Template:ABSTRACT PUBMED 16139248

About this Structure

1TVO is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Identification of a selective ERK inhibitor and structural determination of the inhibitor-ERK2 complex., Ohori M, Kinoshita T, Okubo M, Sato K, Yamazaki A, Arakawa H, Nishimura S, Inamura N, Nakajima H, Neya M, Miyake H, Fujii T, Biochem Biophys Res Commun. 2005 Oct 14;336(1):357-63. PMID:16139248

Page seeded by OCA on Tue Jul 29 02:20:36 2008

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