We apologize for Proteopedia being slow to respond. For the past two years, a new implementation of Proteopedia has been being built. Soon, it will replace this 18-year old system. All existing content will be moved to the new system at a date that will be announced here.

2z4b

From Proteopedia

Revision as of 21:40, 12 November 2007 by OCA (Talk | contribs)
(diff) ←Older revision | Current revision (diff) | Newer revision→ (diff)
Jump to: navigation, search
Image:2z4b.gif

2z4b, resolution 2.34Å

Drag the structure with the mouse to rotate

Estrogen receptor beta ligand-binding domain complexed to a benzopyran ligand

Overview

Benzopyrans are selective estrogen receptor (ER) beta agonists (SERBAs), which bind the ER subtypes alpha and beta in opposite orientations. Here, we describe the syntheses of cyclopentanone and cyclohexanone, intermediates for SAR studies of the C-ring on the benzopyran scaffold., Modification of the C-ring disrupts binding to ERalpha, thus improving, ERbeta selectivity up to 100-fold. X-ray cocrystal structures confirm, previously observed binding modes.

About this Structure

2Z4B is a Single protein structure of sequence from Homo sapiens with DC8 as ligand. Full crystallographic information is available from OCA.

Reference

Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 3: Synthesis of cyclopentanone and cyclohexanone intermediates for C-ring modification., Richardson TI, Dodge JA, Durst GL, Pfeifer LA, Shah J, Wang Y, Durbin JD, Krishnan V, Norman BH, Bioorg Med Chem Lett. 2007 Sep 1;17(17):4824-8. Epub 2007 Jun 20. PMID:17614275

Page seeded by OCA on Mon Nov 12 23:46:45 2007

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/2z4b"
Personal tools