Premium
Evaluation of synthetic thiosemicarbazone containing compounds as inhibitors of cathepsin K
Author(s) -
Wen Lisa,
Feeley Ariel P,
Sexton Buddy K,
Smith Samantha K,
Pallempati Kirthi,
Huang JenqKuen,
McConnell Rose M
Publication year - 2013
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.27.1_supplement.560.10
Subject(s) - cathepsin k , chemistry , cathepsin , cathepsin b , bone resorption , biochemistry , enzyme , cysteine protease , cysteine , in vitro , medicine , osteoclast
Cathepsin K is a cysteine protease that is highly expressed in osteoclasts. Because of its strong collagenolytic activity cathepsin K has been described as the major enzyme responsible for the degradation of organic bone matrix, and is believed to play a fundamental role in bone resorption. Cathepsin K has become an established drug target for osteoporosis. Here, we report screening and evaluation of synthetic thiosemicarbazone containing compounds against cathepsin K. The studies were performed using recombinant human cathepsin K and colorimetric enzyme inhibition assay with N‐Carbobenzoxy‐L‐Phenylalanyl‐Arginine‐4‐nitroanilide hydrochloride as the chromogenic substrate. Data analysis of the effectiveness of these inhibitors will be used to foster future development of newer effective inhibitors for the treatment osteoporosis. Funding provided by National Cancer Institute at NIH (Grant No. 3R15CA086933–04 and 3R15CA086933–04A2S1) and Western Illinois University.