Current Medicinal Chemistry

Atta-ur-Rahman, FRS
Honorary Life Fellow
Kings College
University of Cambridge


Recent advances of hepsin-targeted inhibitors

(E-pub Abstract Ahead of Print)

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


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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Article Details

Year: 2017
(E-pub Abstract Ahead of Print)
DOI: 10.2174/0929867324666170227115835
Price: $95