2ath

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{{STRUCTURE_2ath| PDB=2ath | SCENE= }}
{{STRUCTURE_2ath| PDB=2ath | SCENE= }}
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'''Crystal structure of the ligand binding domain of human PPAR-gamma im complex with an agonist'''
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===Crystal structure of the ligand binding domain of human PPAR-gamma im complex with an agonist===
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==Overview==
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The synthesis and structure-activity relationship studies of novel indole derivatives as peroxisome proliferator-activated receptor (PPAR) agonists are reported. Indole, a drug-like scaffold, was studied as a core skeleton for the acidic head part of PPAR agonists. The structural features (acidic head, substitution on indole, and linker) were optimized first, by keeping benzisoxazole as the tail part, based on binding and functional activity at PPARgamma protein. The variations in the tail part, by introducing various heteroaromatic ring systems, were then studied. In vitro evaluation led to identification of a novel series of indole compounds with a benzisoxazole tail as potent PPAR agonists with the lead compound 14 (BPR1H036) displaying an excellent pharmacokinetic profile in BALB/c mice and an efficacious glucose lowering activity in KKA(y) mice. Structural biology studies of 14 showed that the indole ring contributes strong hydrophobic interactions with PPARgamma and could be an important moiety for the binding to the protein.
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The line below this paragraph, {{ABSTRACT_PUBMED_16366601}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 16366601 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16366601}}
==About this Structure==
==About this Structure==
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[[Category: Wu, S Y.]]
[[Category: Wu, S Y.]]
[[Category: Ppar]]
[[Category: Ppar]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 19:27:28 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 07:35:50 2008''

Revision as of 04:35, 28 July 2008

Image:2ath.png

Template:STRUCTURE 2ath

Crystal structure of the ligand binding domain of human PPAR-gamma im complex with an agonist

Template:ABSTRACT PUBMED 16366601

About this Structure

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

Reference

Novel indole-based peroxisome proliferator-activated receptor agonists: design, SAR, structural biology, and biological activities., Mahindroo N, Huang CF, Peng YH, Wang CC, Liao CC, Lien TW, Chittimalla SK, Huang WJ, Chai CH, Prakash E, Chen CP, Hsu TA, Peng CH, Lu IL, Lee LH, Chang YW, Chen WC, Chou YC, Chen CT, Goparaju CM, Chen YS, Lan SJ, Yu MC, Chen X, Chao YS, Wu SY, Hsieh HP, J Med Chem. 2005 Dec 29;48(26):8194-208. PMID:16366601

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