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Hurdles in the drug discovery of cathepsin K inhibitors (Review)

Kometani, Motohiko, Nonomura, Kazuhiko, Tomoo, Takashi and Niwa, Satoru (2010) Hurdles in the drug discovery of cathepsin K inhibitors (Review). Current Topics of Medicinal Chemistry, 10 (7). pp. 733-744. ISSN 1568-0266


Abstract: There were many hurdles in the drug discovery of cathepsin K inhibitors such as species differences not only in bone metabolism but also in amino acid sequences in the critical site of the target enzyme, discrepancies between PK/PD due to unique tissue distribution of the inhibitor affecting both efficacy and side effects originated from a characteristic intracellular or tissue distribution of some classes of compounds. The value of this new therapeutic approach over the launched indirect competitors should be further clarified from the efficacy and side effect point of view. The cathepsin K inhibitor drug discovery was initiated based on a strong and osteoclast-specific expression of this enzyme. However, the tissues and cells expressing cathepsin K have been expanding as the investigation on pathological conditions progressed with respect to side effects as well as new possible indications.

Item Type: Article
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Additional Information: This article is a review about cathepsin K inhibitors. Data included in the text originate from published journals, conference abstracts and books. author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Keywords: Cathepsin K inhibitors; Differentiation; Species difference; PK/PD; On and Off-target Side Effects; Osteoporosis; Bone resorption; Osteoclasts.
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Date Deposited: 13 Oct 2015 13:16
Last Modified: 13 Oct 2015 13:16


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