title: Fluorescent nitrile-based inhibitors of cysteine cathepsins.
abstract: Cysteine cathepsins play an important role in many (patho)physiological conditions. Among them, cathepsins L, S, K and B are subjects of several drug discovery programs. Besides their role as drug targets, cysteine cathepsins are additionally considered to be possible biomarkers for inflammation and cancer. Herein, we describe the design, synthesis, biological evaluation and spectral properties of fluorescently labeled dipeptide- and azadipeptide nitriles.
authors.affiliation: Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn, An der Immenburg 4, D-53121 Bonn, Germany.
authors.forename: Maxim
authors.initials: M
authors.lastname: Frizler
authors.forename: Matthias D
authors.initials: MD
authors.lastname: Mertens
authors.forename: Michael
authors.initials: M
authors.lastname: Gütschow
mesh_terms: D002403:Cathepsins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D015853:Cysteine Proteinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004151:Dipeptides / Q000737:chemistry*; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D005453:Fluorescence; D015394:Molecular Structure; D009570:Nitriles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D015853:Cysteine Proteinase Inhibitors; D004151:Dipeptides; D009570:Nitriles; D002403:Cathepsins