Linked Life Data

18855964

Source:http://linkedlifedata.com/resource/pubmed/id/18855964

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
16
pubmed:dateCreated
2008-11-4
pubmed:abstractText
Monoglyceride lipase (MGL) plays a major role in the metabolism of the lipid transmitter 2-arachidonoylglycerol (2-AG). This endocannabinoid is known to mediate a large number of physiological processes, and its regulation is thought to be of great therapeutic potential. However, the number of available monoglyceride lipase inhibitors is limited, mostly due to the lack of rapid and accurate pharmacological assays for the enzyme. We have developed a 96-well-format assay for MGL using a nonradiolabeled substrate, 4-nitrophenylacetate. The IC(50) values that were obtained for known inhibitors of MGL using 4-nitrophenylacetate were similar to those reported by using the radiolabeled form of an endogenous substrate, 2-oleoylglycerol. In a first small-scale screening, we identified CAY10499 as a novel monoglyceride lipase inhibitor. Thus, we report here the characterization of this submicromolar inhibitor, which acts on MGL through an unprecedented mechanism for inhibitors of this enzyme.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Nov
pubmed:issn
1439-7633
pubmed:author
pubmed:issnType
Electronic
pubmed:day
3
pubmed:volume
9
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
2704-10
pubmed:meshHeading
pubmed:year
2008
pubmed:articleTitle
CAY10499, a novel monoglyceride lipase inhibitor evidenced by an expeditious MGL assay.
pubmed:affiliation
Unité de Chimie Pharmaceutique et de Radiopharmacie, Ecole de Pharmacie, Faculté de Médecine, Université Catholique de Louvain, Avenue E. Mounier 73.40, 1200 Bruxelles, Belgium. giulio.muccioli@uclouvain.be
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't