title: Cathepsin C inhibitors: property optimization and identification of a clinical candidate.
abstract: A lead generation and optimization program delivered the highly selective and potent CatC inhibitor 10 as an in vivo tool compound and potential development candidate. Structural studies were undertaken to generate SAR understanding.
authors.affiliation: AstraZeneca , Pepparedsleden 1, Mölndal 431 83, Sweden.
authors.forename: Mark
authors.initials: M
authors.lastname: Furber
authors.forename: Anna-Karin
authors.initials: AK
authors.lastname: Tiden
authors.forename: Philip
authors.initials: P
authors.lastname: Gardiner
authors.forename: Antonio
authors.initials: A
authors.lastname: Mete
authors.forename: Rhonan
authors.initials: R
authors.lastname: Ford
authors.forename: Ian
authors.initials: I
authors.lastname: Millichip
authors.forename: Linda
authors.initials: L
authors.lastname: Stein
authors.forename: Andrew
authors.initials: A
authors.lastname: Mather
authors.forename: Elizabeth
authors.initials: E
authors.lastname: Kinchin
authors.forename: Christopher
authors.initials: C
authors.lastname: Luckhurst
authors.forename: Simon
authors.initials: S
authors.lastname: Barber
authors.forename: Peter
authors.initials: P
authors.lastname: Cage
authors.forename: Hitesh
authors.initials: H
authors.lastname: Sanganee
authors.forename: Rupert
authors.initials: R
authors.lastname: Austin
authors.forename: Kamaldeep
authors.initials: K
authors.lastname: Chohan
authors.forename: Raj
authors.initials: R
authors.lastname: Beri
authors.forename: Bob
authors.initials: B
authors.lastname: Thong
authors.forename: Alan
authors.initials: A
authors.lastname: Wallace
authors.forename: Victor
authors.initials: V
authors.lastname: Oreffo
authors.forename: Ray
authors.initials: R
authors.lastname: Hutchinson
authors.forename: Steve
authors.initials: S
authors.lastname: Harper
authors.forename: Judit
authors.initials: J
authors.lastname: Debreczeni
authors.forename: Jason
authors.initials: J
authors.lastname: Breed
authors.forename: Lisa
authors.initials: L
authors.lastname: Wissler
authors.forename: Karl
authors.initials: K
authors.lastname: Edman
mesh_terms: D020789:Cathepsin C / Q000037:antagonists & inhibitors*; D006801:Humans; D007202:Indicators and Reagents; D008958:Models, Molecular; D008968:Molecular Conformation; D011480:Protease Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D011994:Recombinant Proteins / Q000737:chemistry; D013050:Spectrometry, Fluorescence; D013329:Structure-Activity Relationship; D013379:Substrate Specificity; D014961:X-Ray Diffraction
chemical_list: D007202:Indicators and Reagents; D011480:Protease Inhibitors; D011994:Recombinant Proteins; D020789:Cathepsin C