title: Dipeptidyl nitrile inhibitors of Cathepsin L.
abstract: A series of potent Cathepsin L inhibitors with good selectivity with respect to other cysteine Cathepsins is described and SAR is discussed with reference to the crystal structure of a protein-ligand complex.
authors.affiliation: Respiratory & Inflammation Research Area, AstraZeneca, Mereside, Alderley Park, Macclesfield SK10 4TG, UK.
authors.forename: Nabil
authors.initials: N
authors.lastname: Asaad
authors.forename: Paul A
authors.initials: PA
authors.lastname: Bethel
authors.forename: Michelle D
authors.initials: MD
authors.lastname: Coulson
authors.forename: Jack E
authors.initials: JE
authors.lastname: Dawson
authors.forename: Susannah J
authors.initials: SJ
authors.lastname: Ford
authors.forename: Stefan
authors.initials: S
authors.lastname: Gerhardt
authors.forename: Matthew
authors.initials: M
authors.lastname: Grist
authors.forename: Gordon A
authors.initials: GA
authors.lastname: Hamlin
authors.forename: Michael J
authors.initials: MJ
authors.lastname: James
authors.forename: Emma V
authors.initials: EV
authors.lastname: Jones
authors.forename: Galith I
authors.initials: GI
authors.lastname: Karoutchi
authors.forename: Peter W
authors.initials: PW
authors.lastname: Kenny
authors.forename: Andrew D
authors.initials: AD
authors.lastname: Morley
authors.forename: Keith
authors.initials: K
authors.lastname: Oldham
authors.forename: Neil
authors.initials: N
authors.lastname: Rankine
authors.forename: David
authors.initials: D
authors.lastname: Ryan
authors.forename: Stuart L
authors.initials: SL
authors.lastname: Wells
authors.forename: Linda
authors.initials: L
authors.lastname: Wood
authors.forename: Martin
authors.initials: M
authors.lastname: Augustin
authors.forename: Stephan
authors.initials: S
authors.lastname: Krapp
authors.forename: Hannes
authors.initials: H
authors.lastname: Simader
authors.forename: Stefan
authors.initials: S
authors.lastname: Steinbacher
mesh_terms: D000818:Animals; D002358:Cartilage, Articular / Q000473:pathology; D002384:Catalysis; D056668:Cathepsin L / Q000037:antagonists & inhibitors* / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D018360:Crystallography, X-Ray / Q000379:methods; D015195:Drug Design; D006801:Humans; D008024:Ligands; D051379:Mice; D008822:Mice, Transgenic; D009570:Nitriles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D010455:Peptides / Q000138:chemical synthesis / Q000494:pharmacology; D011506:Proteins / Q000737:chemistry; D013329:Structure-Activity Relationship
chemical_list: D008024:Ligands; D009570:Nitriles; D010455:Peptides; D011506:Proteins; D056668:Cathepsin L