1z95

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Line 1: Line 1:
-
[[Image:1z95.gif|left|200px]]
+
{{Seed}}
 +
[[Image:1z95.png|left|200px]]
<!--
<!--
Line 9: Line 10:
{{STRUCTURE_1z95| PDB=1z95 | SCENE= }}
{{STRUCTURE_1z95| PDB=1z95 | SCENE= }}
-
'''Crystal Structure of the Androgen Receptor Ligand-binding Domain W741L Mutant Complex with R-bicalutamide'''
+
===Crystal Structure of the Androgen Receptor Ligand-binding Domain W741L Mutant Complex with R-bicalutamide===
-
==Overview==
+
<!--
-
Carcinoma of the prostate is the most commonly diagnosed cancer in men. The current pharmacological treatment of choice for progressive androgen-dependent prostate cancer is the nonsteroidal antiandrogen, bicalutamide, either as monotherapy or with adjuvant castration or luteinizing hormone-releasing hormone superagonists to block the synthesis of endogenous testosterone. To date, no nonsteroidal or antagonist-bound androgen receptor (AR) structure is available. We solved the x-ray crystal structure of the mutant W741L AR ligand-binding domain bound to R-bicalutamide at 1.8-A resolution. This mutation confers agonist activity to bicalutamide and is likely involved in bicalutamide withdrawal syndrome. The three-dimensional structure demonstrates that the B ring of R-bicalutamide in the W741L mutant is accommodated at the location of the indole ring of Trp-741 in the WT AR bound to dihydrotestosterone. Knowledge of the binding mechanism for R-bicalutamide will provide molecular rationale for the development of new antiandrogens and selective AR modulators.
+
The line below this paragraph, {{ABSTRACT_PUBMED_15833816}}, adds the Publication Abstract to the page
 +
(as it appears on PubMed at http://www.pubmed.gov), where 15833816 is the PubMed ID number.
 +
-->
 +
{{ABSTRACT_PUBMED_15833816}}
==About this Structure==
==About this Structure==
Line 31: Line 35:
[[Category: Receptor]]
[[Category: Receptor]]
[[Category: Steroid hormone]]
[[Category: Steroid hormone]]
-
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 17:20:07 2008''
+
 
 +
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 04:26:19 2008''

Revision as of 01:26, 28 July 2008

Image:1z95.png

Template:STRUCTURE 1z95

Crystal Structure of the Androgen Receptor Ligand-binding Domain W741L Mutant Complex with R-bicalutamide

Template:ABSTRACT PUBMED 15833816

About this Structure

1Z95 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Structural basis for antagonism and resistance of bicalutamide in prostate cancer., Bohl CE, Gao W, Miller DD, Bell CE, Dalton JT, Proc Natl Acad Sci U S A. 2005 Apr 26;102(17):6201-6. Epub 2005 Apr 15. PMID:15833816

Page seeded by OCA on Mon Jul 28 04:26:19 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/1z95"
Personal tools