Linked Life Data

15267235

Source:http://linkedlifedata.com/resource/pubmed/id/15267235

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
16
pubmed:dateCreated
2004-7-22
pubmed:abstractText
Melanin-concentrating hormone (MCH) has been known to be an appetite-stimulating peptide for a number of years. However, it is only recently that MCH has been discovered to be the natural ligand for a previously "orphan" G-protein-coupled receptor, now designated MCH-1R. This receptor has been shown to mediate the effects of MCH on appetite and body weight, and consequently, drug discovery programs have begun to exploit this information in the search for MCH-1R antagonists for the treatment of obesity. In this paper, we report the rapid discovery of multiple, structurally distinct series of MCH-1R antagonists using a variety of virtual screening techniques. The most potent of these compounds (12) demonstrated an IC(50) value of 55 nM in the primary screen and exhibited antagonist properties in a functional cellular assay measuring Ca(2+) release. More potent compounds were identified by follow-up searches around the initial hit. A proposed binding mode for compound 12 in a homology model of the MCH-1R is also presented.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jul
pubmed:issn
0022-2623
pubmed:author
pubmed:issnType
Print
pubmed:day
29
pubmed:volume
47
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
3962-71
pubmed:dateRevised
2006-6-1
pubmed:meshHeading
pubmed:year
2004
pubmed:articleTitle
A virtual screening approach to finding novel and potent antagonists at the melanin-concentrating hormone 1 receptor.
pubmed:affiliation
Argenta Discovery Ltd., 8/9 Spire Green Centre, Flex Meadow, Harlow, Essex, CM19 5TR, UK. david.clark @argentadiscovery.com
pubmed:publicationType
Journal Article