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1ljt

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{{STRUCTURE_1ljt| PDB=1ljt | SCENE= }}
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'''Crystal Structure of Macrophage Migration Inhibitory Factor complexed with (S,R)-3-(4-hydroxyphenyl)-4,5-dihydro-5-isoxazole-acetic acid methyl ester (ISO-1)'''
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===Crystal Structure of Macrophage Migration Inhibitory Factor complexed with (S,R)-3-(4-hydroxyphenyl)-4,5-dihydro-5-isoxazole-acetic acid methyl ester (ISO-1)===
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==Overview==
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Macrophage migration inhibitory factor (MIF) is an immunoregulatory protein that is a potential therapeutic target for a number of inflammatory diseases. Evidence exists that an unexpected catalytic active site of MIF may have a biological function. To gain further insight into the role of the catalytic active site, a series of mutational, structural, and biological activity studies were performed. The insertion of an alanine between Pro-1 and Met-2 (PAM) abolishes a non-physiological catalytic activity, and this mutant is defective in the in vitro glucocorticoid counter-regulatory activity of MIF. The crystal structure of MIF complexed to (S,R)-3-(4-hydroxyphenyl)-4,5-dihydro-5-isoxazole acetic acid methyl ester (ISO-1), an inhibitor of MIF d-dopachrome tautomerase activity, reveals that ISO-1 binds to the same position of the active site as p-hydroxyphenylpyruvic acid, a substrate of MIF. ISO-1 inhibits several MIF biological activities, further establishing a role for the catalytic active site of MIF.
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(as it appears on PubMed at http://www.pubmed.gov), where 11997397 is the PubMed ID number.
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{{ABSTRACT_PUBMED_11997397}}
==About this Structure==
==About this Structure==
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[[Category: Ruzsicska, B.]]
[[Category: Ruzsicska, B.]]
[[Category: Protein-inhibitor complex]]
[[Category: Protein-inhibitor complex]]
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Revision as of 18:02, 2 July 2008

Image:1ljt.png

Template:STRUCTURE 1ljt

Crystal Structure of Macrophage Migration Inhibitory Factor complexed with (S,R)-3-(4-hydroxyphenyl)-4,5-dihydro-5-isoxazole-acetic acid methyl ester (ISO-1)

Template:ABSTRACT PUBMED 11997397

About this Structure

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

Reference

The tautomerase active site of macrophage migration inhibitory factor is a potential target for discovery of novel anti-inflammatory agents., Lubetsky JB, Dios A, Han J, Aljabari B, Ruzsicska B, Mitchell R, Lolis E, Al-Abed Y, J Biol Chem. 2002 Jul 12;277(28):24976-82. Epub 2002 May 7. PMID:11997397

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