2hvc
From Proteopedia
(New page: 200px<br /> <applet load="2hvc" size="450" color="white" frame="true" align="right" spinBox="true" caption="2hvc, resolution 2.1Å" /> '''The Crystal Structur...) |
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| - | [[Image:2hvc. | + | [[Image:2hvc.jpg|left|200px]]<br /><applet load="2hvc" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="2hvc" size=" | + | |
caption="2hvc, resolution 2.1Å" /> | caption="2hvc, resolution 2.1Å" /> | ||
'''The Crystal Structure of Ligand-binding Domain (LBD) of human Androgen Receptor in Complex with a selective modulator LGD2226'''<br /> | '''The Crystal Structure of Ligand-binding Domain (LBD) of human Androgen Receptor in Complex with a selective modulator LGD2226'''<br /> | ||
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==Overview== | ==Overview== | ||
The androgen receptor (AR) is a ligand-inducible steroid hormone receptor, that mediates androgen action, determining male sexual phenotypes and, promoting spermatogenesis. As the androgens play a dominant role in male, sexual development and function, steroidal androgen agonists have been, used clinically for some years. However, there is a risk of potential side, effects and most steroidal androgens cannot be dosed orally, which limits, the use of these substances., 1,2-Dihydro-6-N,N-bis(2,2,2-trifluoroethyl)amino-4-trifluoromethyl-2-quino, linone (LGD2226) is a synthetic nonsteroidal ligand and a novel selective, AR modulator. The crystal structure of the complex of LGD2226 with the, androgen receptor ligand-binding domain (AR LBD) at 2.1 A was solved and, compared with the structure of the AR LBD-R1881 complex. It is hoped that, this will aid in further explaining the selectivity of LGD2226 observed in, in vitro and in vivo assays and in developing more selective and effective, therapeutic agents. | The androgen receptor (AR) is a ligand-inducible steroid hormone receptor, that mediates androgen action, determining male sexual phenotypes and, promoting spermatogenesis. As the androgens play a dominant role in male, sexual development and function, steroidal androgen agonists have been, used clinically for some years. However, there is a risk of potential side, effects and most steroidal androgens cannot be dosed orally, which limits, the use of these substances., 1,2-Dihydro-6-N,N-bis(2,2,2-trifluoroethyl)amino-4-trifluoromethyl-2-quino, linone (LGD2226) is a synthetic nonsteroidal ligand and a novel selective, AR modulator. The crystal structure of the complex of LGD2226 with the, androgen receptor ligand-binding domain (AR LBD) at 2.1 A was solved and, compared with the structure of the AR LBD-R1881 complex. It is hoped that, this will aid in further explaining the selectivity of LGD2226 observed in, in vitro and in vivo assays and in developing more selective and effective, therapeutic agents. | ||
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| - | ==Disease== | ||
| - | Known diseases associated with this structure: Androgen insensitivity OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=313700 313700]], Breast cancer, male, with Reifenstein syndrome OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=313700 313700]], Hypospadias, perineal OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=313700 313700]], Prostate cancer OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=313700 313700]], Prostate cancer, susceptibility to OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=313700 313700]], Spinal and bulbar muscular atrophy of Kennedy OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=313700 313700]] | ||
==About this Structure== | ==About this Structure== | ||
| - | 2HVC 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 LGD as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http:// | + | 2HVC 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=LGD:'>LGD</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2HVC OCA]. |
==Reference== | ==Reference== | ||
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[[Category: steroid-binding]] | [[Category: steroid-binding]] | ||
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Revision as of 12:20, 23 January 2008
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The Crystal Structure of Ligand-binding Domain (LBD) of human Androgen Receptor in Complex with a selective modulator LGD2226
Overview
The androgen receptor (AR) is a ligand-inducible steroid hormone receptor, that mediates androgen action, determining male sexual phenotypes and, promoting spermatogenesis. As the androgens play a dominant role in male, sexual development and function, steroidal androgen agonists have been, used clinically for some years. However, there is a risk of potential side, effects and most steroidal androgens cannot be dosed orally, which limits, the use of these substances., 1,2-Dihydro-6-N,N-bis(2,2,2-trifluoroethyl)amino-4-trifluoromethyl-2-quino, linone (LGD2226) is a synthetic nonsteroidal ligand and a novel selective, AR modulator. The crystal structure of the complex of LGD2226 with the, androgen receptor ligand-binding domain (AR LBD) at 2.1 A was solved and, compared with the structure of the AR LBD-R1881 complex. It is hoped that, this will aid in further explaining the selectivity of LGD2226 observed in, in vitro and in vivo assays and in developing more selective and effective, therapeutic agents.
About this Structure
2HVC is a Single protein structure of sequence from Homo sapiens with as ligand. Full crystallographic information is available from OCA.
Reference
Structure of the ligand-binding domain (LBD) of human androgen receptor in complex with a selective modulator LGD2226., Wang F, Liu XQ, Li H, Liang KN, Miner JN, Hong M, Kallel EA, van Oeveren A, Zhi L, Jiang T, Acta Crystallograph Sect F Struct Biol Cryst Commun. 2006 Nov 1;62(Pt, 11):1067-71. Epub 2006 Oct 25. PMID:17077481
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