2hwq
From Proteopedia
(New page: 200px<br /> <applet load="2hwq" size="450" color="white" frame="true" align="right" spinBox="true" caption="2hwq, resolution 1.97Å" /> '''Structural basis fo...) |
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| - | [[Image:2hwq. | + | [[Image:2hwq.jpg|left|200px]]<br /><applet load="2hwq" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="2hwq" size=" | + | |
caption="2hwq, resolution 1.97Å" /> | caption="2hwq, resolution 1.97Å" /> | ||
'''Structural basis for the structure-activity relationships of Peroxisome Proliferator-Activated Receptor agonists'''<br /> | '''Structural basis for the structure-activity relationships of Peroxisome Proliferator-Activated Receptor agonists'''<br /> | ||
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==Overview== | ==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. | 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. | ||
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| - | ==Disease== | ||
| - | Known diseases associated with this structure: Abdominal body fat distribution, modifier of OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=601487 601487]], Diabetes mellitus, insulin-resistant, with acanthosis nigricans and hypertension OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=601487 601487]], Glioblastoma, susceptibility to OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=601487 601487]], Insulin resistance, severe, digenic OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=601487 601487]], Lipodystrophy, familial partial OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=601487 601487]], Obesity, resistance to OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=601487 601487]], Obesity, severe OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=601487 601487]] | ||
==About this Structure== | ==About this Structure== | ||
| - | 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 DRY as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http:// | + | 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]. |
==Reference== | ==Reference== | ||
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[[Category: ppar]] | [[Category: ppar]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 14:15:29 2008'' |
Revision as of 12:15, 23 January 2008
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Structural basis for the structure-activity relationships of Peroxisome Proliferator-Activated Receptor agonists
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.
About this Structure
2HWQ is a Single protein structure of sequence from Homo sapiens with as ligand. 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
Page seeded by OCA on Wed Jan 23 14:15:29 2008
Categories: Homo sapiens | Single protein | Hsieh, H.P. | Lin, C.H. | Lu, I.L. | Mahindroo, N. | Peng, Y.H. | Wu, S.Y. | DRY | Ligand binding protein | Ppar
