The design and synthesis of inhibitors of the cysteinyl protease, Der p I.
Prototype irreversible inhibitors of the cysteinyl protease Der p I were designed, synthesised and evaluated in vitro. Candidates were designed using a modular approach, whereby a peptide sequence was appended with known thiophilic moieties. This hinged on utilizing peptide sequences from substrate specificity data compiled using proprietary RAPiD technology.
Billson
J
J
Peptide Therapeutics Group plc, Cambridge, UK. jeremy.billson@peptide.co.uk
Clark
J
J
Conway
S P
SP
Hart
T
T
Johnson
T
T
Langston
S P
SP
Ramjee
M
M
Quibell
M
M
Scott
R K
RK
D000818:Animals; D039741:Antigens, Dermatophagoides; D001402:B-Lymphocytes; D002460:Cell Line; D003546:Cysteine Endopeptidases / Q000378:metabolism*; D015853:Cysteine Proteinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D005243:Feces; D006023:Glycoproteins / Q000037:antagonists & inhibitors* / Q000302:isolation & purification; D006801:Humans; D008925:Mites / Q000201:enzymology / Q000276:immunology; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D013379:Substrate Specificity; D013450:Sulfones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014753:Vinyl Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
D039741:Antigens, Dermatophagoides; D015853:Cysteine Proteinase Inhibitors; D006023:Glycoproteins; D013450:Sulfones; D014753:Vinyl Compounds; D003546:Cysteine Endopeptidases