3g0w

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[[Image:3g0w.png|left|200px]]
 
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{{STRUCTURE_3g0w| PDB=3g0w | SCENE= }}
{{STRUCTURE_3g0w| PDB=3g0w | SCENE= }}
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===Crystal structure of the rat androgen receptor ligand binding domain complex with an n-aryl-oxazolidin 2-imine inhibitor===
===Crystal structure of the rat androgen receptor ligand binding domain complex with an n-aryl-oxazolidin 2-imine inhibitor===
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{{ABSTRACT_PUBMED_19351168}}
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{{ABSTRACT_PUBMED_19351168}}
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==Disease==
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[[http://www.uniprot.org/uniprot/ANDR_RAT ANDR_RAT]] Note=Defects in Ar are a cause of androgen insensitivity. Rats with this syndrome are called testicular feminized (TFM).<ref>PMID:2341409</ref>
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==Function==
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[[http://www.uniprot.org/uniprot/ANDR_RAT ANDR_RAT]] Steroid hormone receptors are ligand-activated transcription factors that regulate eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Transcription factor activity is modulated by bound coactivator and corepressor proteins. Transcription activation is down-regulated by NR0B2. Activated, but not phosphorylated, by HIPK3 and ZIPK/DAPK3 (By similarity).<ref>PMID:17181141</ref><ref>PMID:17008401</ref>
==About this Structure==
==About this Structure==
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==Reference==
==Reference==
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<ref group="xtra">PMID:019351168</ref><references group="xtra"/>
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<ref group="xtra">PMID:019351168</ref><references group="xtra"/><references/>
[[Category: Rattus norvegicus]]
[[Category: Rattus norvegicus]]
[[Category: Sack, J S.]]
[[Category: Sack, J S.]]

Revision as of 04:26, 25 March 2013

Template:STRUCTURE 3g0w

Contents

Crystal structure of the rat androgen receptor ligand binding domain complex with an n-aryl-oxazolidin 2-imine inhibitor

Template:ABSTRACT PUBMED 19351168

Disease

[ANDR_RAT] Note=Defects in Ar are a cause of androgen insensitivity. Rats with this syndrome are called testicular feminized (TFM).[1]

Function

[ANDR_RAT] Steroid hormone receptors are ligand-activated transcription factors that regulate eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Transcription factor activity is modulated by bound coactivator and corepressor proteins. Transcription activation is down-regulated by NR0B2. Activated, but not phosphorylated, by HIPK3 and ZIPK/DAPK3 (By similarity).[2][3]

About this Structure

3g0w is a 1 chain structure with sequence from Rattus norvegicus. Full crystallographic information is available from OCA.

Reference

  • Nirschl AA, Zou Y, Krystek SR, Sutton JC, Simpkins LM, Lupisella JA, Kuhns JE, Seethala R, Golla R, Sleph PG, Beehler BC, Grover GJ, Egan D, Fura A, Vyas VP, Li YX, Sack JS, Kish KF, An Y, Bryson JA, Gougoutas JZ, Dimarco J, Zahler R, Ostrowski J, Hamann LG. N-Aryl-oxazolidin-2-imine Muscle Selective Androgen Receptor Modulators Enhance Potency through Pharmacophore Reorientation (dagger) ( big up tri, open). J Med Chem. 2009 Apr 7. PMID:19351168 doi:10.1021/jm801583j
  1. ↑ Yarbrough WG, Quarmby VE, Simental JA, Joseph DR, Sar M, Lubahn DB, Olsen KL, French FS, Wilson EM. A single base mutation in the androgen receptor gene causes androgen insensitivity in the testicular feminized rat. J Biol Chem. 1990 May 25;265(15):8893-900. PMID:2341409
  2. ↑ Sun C, Robl JA, Wang TC, Huang Y, Kuhns JE, Lupisella JA, Beehler BC, Golla R, Sleph PG, Seethala R, Fura A, Krystek SR Jr, An Y, Malley MF, Sack JS, Salvati ME, Grover GJ, Ostrowski J, Hamann LG. Discovery of potent, orally-active, and muscle-selective androgen receptor modulators based on an N-aryl-hydroxybicyclohydantoin scaffold. J Med Chem. 2006 Dec 28;49(26):7596-9. PMID:17181141 doi:10.1021/jm061101w
  3. ↑ Ostrowski J, Kuhns JE, Lupisella JA, Manfredi MC, Beehler BC, Krystek SR Jr, Bi Y, Sun C, Seethala R, Golla R, Sleph PG, Fura A, An Y, Kish KF, Sack JS, Mookhtiar KA, Grover GJ, Hamann LG. Pharmacological and x-ray structural characterization of a novel selective androgen receptor modulator: potent hyperanabolic stimulation of skeletal muscle with hypostimulation of prostate in rats. Endocrinology. 2007 Jan;148(1):4-12. Epub 2006 Sep 28. PMID:17008401 doi:10.1210/en.2006-0843

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