Hongmok Kwon, JooYeon Han, Ki-Yong Lee, Sang-Hyun Son* and Youngjoo Byun* Pages 2294 - 2311 ( 18 )
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.
Hepsin, prostate cancer, type II transmembrane serine protease, structure-activity relationship (SAR), amidine, peptides.
College of Pharmacy, Korea University, 2511 Sejong-ro, Sejong 30019, College of Pharmacy, Korea University, 2511 Sejong-ro, Sejong 30019, College of Pharmacy, Korea University, 2511 Sejong-ro, Sejong 30019, College of Pharmacy, Faculty of Pharmacy, Korea University, P.O. Box: 30019, Sejong City, College of Pharmacy, Faculty of Pharmacy, Korea University, P.O. Box: 30019, Sejong City