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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Review Article

Recent Advances of Hepsin-Targeted Inhibitors

Author(s): Hongmok Kwon, JooYeon Han, Ki-Yong Lee, Sang-Hyun Son* and Youngjoo Byun*

Volume 24, Issue 21, 2017

Page: [2294 - 2311] Pages: 18

DOI: 10.2174/0929867324666170227115835

Price: $65


Hepsin is a type II transmembrane serine protease (TTSP) that plays a crucial role in cell growth and development. Hepsin is highly expressed in prostate cancer (PCa) and associated with its progression and metastasis. Therefore, it has been considered as an attractive biomarker of PCa. Recently, low molecular weight inhibitors targeting hepsin have been developed. Based on the key chemical scaffold, they can be classified into four classes: Indolecarboxamidines, benzamidines, peptide-based analogs, and 2,3-dihydro- 1H-perimidines. In this review, we discuss design strategy, structure-activity relationship (SAR), and binding mode of the four classes of hepsin inhibitors.

Keywords: Hepsin, prostate cancer, type II transmembrane serine protease, structure-activity relationship (SAR), amidine, peptides.

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