title: Recent Advances of Hepsin-Targeted Inhibitors.
abstract: 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.
authors.affiliation: College of Pharmacy, Korea University, 2511 Sejong-ro, Sejong 30019, South Korea.
authors.forename: Hongmok
authors.initials: H
authors.lastname: Kwon
authors.affiliation: College of Pharmacy, Korea University, 2511 Sejong-ro, Sejong 30019, South Korea.
authors.forename: JooYeon
authors.initials: J
authors.lastname: Han
authors.affiliation: College of Pharmacy, Korea University, 2511 Sejong-ro, Sejong 30019, South Korea.
authors.forename: Ki-Yong
authors.initials: KY
authors.lastname: Lee
authors.affiliation: College of Pharmacy, Korea University, 2511 Sejong-ro, Sejong 30019, South Korea.
authors.forename: Sang-Hyun
authors.initials: SH
authors.lastname: Son
authors.affiliation: College of Pharmacy, Korea University, 2511 Sejong-ro, Sejong 30019, South Korea.
authors.forename: Youngjoo
authors.initials: Y
authors.lastname: Byun
mesh_terms: D015195:Drug Design; D006801:Humans; D012697:Serine Endopeptidases / Q000378:metabolism*; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D015842:Serine Proteinase Inhibitors; D012697:Serine Endopeptidases; C055645:hepsin
keywords: Hepsin; amidine; peptides; prostate cancer; structure-activity relationship (SAR); type II transmembrane serine protease