title: The identification of beta-hydroxy carboxylic acids as selective MMP-12 inhibitors.
abstract: A new class of selective MMP-12 inhibitors have been identified via high throughput screening. Crystallization with MMP-12 confirmed the mode of binding and allowed initial optimization to be carried out using classical structure based design.
authors.affiliation: GSK Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, United Kingdom.
authors.forename: Ian P
authors.initials: IP
authors.lastname: Holmes
authors.forename: Simon
authors.initials: S
authors.lastname: Gaines
authors.forename: Steve P
authors.initials: SP
authors.lastname: Watson
authors.forename: Olivier
authors.initials: O
authors.lastname: Lorthioir
authors.forename: Adam
authors.initials: A
authors.lastname: Walker
authors.forename: Suzanne J
authors.initials: SJ
authors.lastname: Baddeley
authors.forename: Shane
authors.initials: S
authors.lastname: Herbert
authors.forename: Danielle
authors.initials: D
authors.lastname: Egan
authors.forename: Máire A
authors.initials: MA
authors.lastname: Convery
authors.forename: Onkar M P
authors.initials: OM
authors.lastname: Singh
authors.forename: Jeffrey W
authors.initials: JW
authors.lastname: Gross
authors.forename: John M
authors.initials: JM
authors.lastname: Strelow
authors.forename: Robert H
authors.initials: RH
authors.lastname: Smith
authors.forename: Augustin J
authors.initials: AJ
authors.lastname: Amour
authors.forename: David
authors.initials: D
authors.lastname: Brown
authors.forename: Stephen L
authors.initials: SL
authors.lastname: Martin
mesh_terms: D000818:Animals; D001665:Binding Sites; D002264:Carboxylic Acids / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D018360:Crystallography, X-Ray; D015195:Drug Design; D006168:Guinea Pigs; D006801:Humans; D053508:Matrix Metalloproteinase 12 / Q000378:metabolism; D061965:Matrix Metalloproteinase Inhibitors; D011480:Protease Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D002264:Carboxylic Acids; D061965:Matrix Metalloproteinase Inhibitors; D011480:Protease Inhibitors; D053508:Matrix Metalloproteinase 12