In April 2016 Manchester eScholar was replaced by the University of Manchester’s new Research Information Management System, Pure. In the autumn the University’s research outputs will be available to search and browse via a new Research Portal. Until then the University’s full publication record can be accessed via a temporary portal and the old eScholar content is available to search and browse via this archive.

Related resources

Full-text held externally

University researcher(s)

Academic department(s)

Optimized chemical probes for REV-ERBα.

Trump, Ryan P; Bresciani, Stefano; Cooper, Anthony W J; Tellam, James P; Wojno, Justyna; Blaikley, John; Orband-Miller, Lisa A; Kashatus, Jennifer A; Boudjelal, Mohamed; Dawson, Helen C; Loudon, Andrew; Ray, David; Grant, Daniel; Farrow, Stuart N; Willson, Timothy M; Tomkinson, Nicholas C O

Journal of medicinal chemistry. 2013;56(11):4729-37.

Access to files

Full-text and supplementary files are not available from Manchester eScholar. Full-text is available externally using the following links:

Full-text held externally

Abstract

REV-ERBα has emerged as an important target for regulation of circadian rhythm and its associated physiology. Herein, we report on the optimization of a series of REV-ERBα agonists based on GSK4112 (1) for potency, selectivity, and bioavailability. (1) Potent REV-ERBα agonists 4, 10, 16, and 23 are detailed for their ability to suppress BMAL and IL-6 expression from human cells while also demonstrating excellent selectivity over LXRα. Amine 4 demonstrated in vivo bioavailability after either iv or oral dosing.

Bibliographic metadata

Type of resource:
Content type:
Publication type:
Published date:
Abbreviated journal title:
ISSN:
Place of publication:
United States
Volume:
56
Issue:
11
Pagination:
4729-37
Digital Object Identifier:
10.1021/jm400458q
Pubmed Identifier:
23656296
Access state:
Active

Institutional metadata

University researcher(s):
Academic department(s):

Record metadata

Manchester eScholar ID:
uk-ac-man-scw:210679
Created by:
Barnes, Louise
Created:
11th October, 2013, 12:29:23
Last modified by:
Barnes, Louise
Last modified:
11th October, 2013, 12:29:23

Can we help?

The library chat service will be available from 11am-3pm Monday to Friday (excluding Bank Holidays). You can also email your enquiry to us.