2hwq

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[[Image:2hwq.jpg|left|200px]]<br /><applet load="2hwq" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:2hwq.jpg|left|200px]]
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caption="2hwq, resolution 1.97&Aring;" />
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'''Structural basis for the structure-activity relationships of Peroxisome Proliferator-Activated Receptor agonists'''<br />
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{{Structure
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|PDB= 2hwq |SIZE=350|CAPTION= <scene name='initialview01'>2hwq</scene>, resolution 1.97&Aring;
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|SITE=
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|LIGAND= <scene name='pdbligand=DRY:[(1-{3-[(6-BENZOYL-1-PROPYL-2-NAPHTHYL)OXY]PROPYL}-1H-INDOL-5-YL)OXY]ACETIC ACID'>DRY</scene>
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|ACTIVITY=
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|GENE=
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}}
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'''Structural basis for the structure-activity relationships of Peroxisome Proliferator-Activated Receptor agonists'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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2HWQ is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=DRY:'>DRY</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2HWQ OCA].
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2HWQ is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2HWQ OCA].
==Reference==
==Reference==
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Structural basis for the structure-activity relationships of peroxisome proliferator-activated receptor agonists., Mahindroo N, Peng YH, Lin CH, Tan UK, Prakash E, Lien TW, Lu IL, Lee HJ, Hsu JT, Chen X, Liao CC, Lyu PC, Chao YS, Wu SY, Hsieh HP, J Med Chem. 2006 Oct 19;49(21):6421-4. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=17034149 17034149]
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Structural basis for the structure-activity relationships of peroxisome proliferator-activated receptor agonists., Mahindroo N, Peng YH, Lin CH, Tan UK, Prakash E, Lien TW, Lu IL, Lee HJ, Hsu JT, Chen X, Liao CC, Lyu PC, Chao YS, Wu SY, Hsieh HP, J Med Chem. 2006 Oct 19;49(21):6421-4. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/17034149 17034149]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Single protein]]
[[Category: Single protein]]
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[[Category: ppar]]
[[Category: ppar]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:46:35 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 17:22:33 2008''

Revision as of 15:22, 20 March 2008

Image:2hwq.jpg


PDB ID 2hwq

Drag the structure with the mouse to rotate
, resolution 1.97Å
Ligands:
Coordinates: save as pdb, mmCIF, xml



Structural basis for the structure-activity relationships of Peroxisome Proliferator-Activated Receptor agonists


Contents

Overview

Type 2 diabetes has rapidly reached an epidemic proportion becoming a major threat to global public health. PPAR agonists have emerged as a leading class of oral antidiabetic drugs. We report a structure biology analysis of novel indole-based PPAR agonists to explain the structure-activity relationships and present a critical analysis of reasons for change in selectivity with change in the orientation of the same scaffolds. The results would be helpful in designing novel PPAR agonists.

Disease

Known diseases associated with this structure: Abdominal body fat distribution, modifier of OMIM:[601487], Diabetes mellitus, insulin-resistant, with acanthosis nigricans and hypertension OMIM:[601487], Glioblastoma, susceptibility to OMIM:[601487], Insulin resistance, severe, digenic OMIM:[601487], Lipodystrophy, familial partial OMIM:[601487], Obesity, resistance to OMIM:[601487], Obesity, severe OMIM:[601487]

About this Structure

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

Reference

Structural basis for the structure-activity relationships of peroxisome proliferator-activated receptor agonists., Mahindroo N, Peng YH, Lin CH, Tan UK, Prakash E, Lien TW, Lu IL, Lee HJ, Hsu JT, Chen X, Liao CC, Lyu PC, Chao YS, Wu SY, Hsieh HP, J Med Chem. 2006 Oct 19;49(21):6421-4. PMID:17034149

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