Cathepsin K inhibitors: a novel target for osteoporosis therapy.
Osteoporosis is characterized by low bone mass with skeletal fragility and an increased risk of fracture. This bone loss is brought about by an imbalance between bone resorption and formation. Cathepsin K is the most abundant cysteine protease expressed in the osteoclast and is believed to be instrumental in bone matrix degradation necessary for bone resorption. Cathepsin K inhibitors represent a novel target for developing agents to treat osteoporosis and other disorders characterized by increased bone resorption.
Stoch
S A
SA
Department of Clinical Pharmacology, Merck Research Laboratories, Rahway, New Jersey, USA. aubrey_stoch@merck.com
Wagner
J A
JA
D000818:Animals; D015519:Bone Density / Q000187:drug effects; D050071:Bone Density Conservation Agents / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D016723:Bone Remodeling / Q000187:drug effects; D056657:Cathepsin K; D002403:Cathepsins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D015853:Cysteine Proteinase Inhibitors / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D004195:Disease Models, Animal; D015195:Drug Design; D006801:Humans; D051379:Mice; D018345:Mice, Knockout; D010026:Osteosclerosis / Q000188:drug therapy* / Q000201:enzymology / Q000503:physiopathology; D010052:Ovariectomy; D011323:Primates; D011817:Rabbits; D051381:Rats; D016896:Treatment Outcome
D050071:Bone Density Conservation Agents; D015853:Cysteine Proteinase Inhibitors; D002403:Cathepsins; C534130:CTSK protein, human; D056657:Cathepsin K; C534132:Ctsk protein, mouse; C534133:Ctsk protein, rat