Identification and characterization of small-molecule inhibitors of hepsin

JR Chevillet, GJ Park, A Bedalov, JA Simon… - Molecular cancer …, 2008 - AACR
Hepsin is a type II transmembrane serine protease overexpressed in the majority of human
prostate cancers. We recently demonstrated that hepsin promotes prostate cancer …

Structure-guided discovery of 2-aryl/pyridin-2-yl-1H-indole derivatives as potent and selective hepsin inhibitors

R Goswami, G Wohlfahrt, O Törmäkangas… - Bioorganic & Medicinal …, 2015 - Elsevier
Hepsin, a type II transmembrane serine protease, is upregulated in prostate cancer and
known to be involved in the progression of metastasis. Here we report a structure-guided …

[HTML][HTML] Targeted inhibition of cell-surface serine protease Hepsin blocks prostate cancer bone metastasis

X Tang, SS Mahajan, LT Nguyen, F Béliveau… - Oncotarget, 2014 - ncbi.nlm.nih.gov
The development of effective therapies inhibiting prostate cancer progression and
metastasis may substantially impact prostate cancer mortality and potentially reduce the …

Antibodies neutralizing hepsin protease activity do not impact cell growth but inhibit invasion of prostate and ovarian tumor cells in culture

JA Xuan, D Schneider, P Toy, R Lin, A Newton, Y Zhu… - Cancer research, 2006 - AACR
Hepsin is a type II transmembrane serine protease that is expressed in normal liver, and at
lower levels in kidney, pancreas, and testis. Several studies have shown that hepsin mRNA …

HEPSIN Inhibits Cell Growth/Invasion in Prostate Cancer Cells

V Srikantan, M Valladares, JS Rhim, JW Moul… - Cancer research, 2002 - AACR
Expression of HEPSIN, a type II transmembrane serine protease in prostate cancer (CaP),
has been highlighted by several studies analyzing CaP-specific gene expression alterations …

[HTML][HTML] Hepsin promotes prostate cancer progression and metastasis

O Klezovitch, J Chevillet, J Mirosevich, RL Roberts… - Cancer cell, 2004 - cell.com
The majority of cancer-related deaths are associated with metastasis; however, little is
known about the mechanisms of this process. Hepsin is a cell surface serine protease that is …

[HTML][HTML] Clinical significance of hepsin and underlying signaling pathways in prostate cancer

L Lu, A Cole, D Huang, Q Wang, Z Guo, W Yang, J Lu - Biomolecules, 2022 - mdpi.com
The hepsin gene encodes a type II transmembrane serine protease. Previous studies have
shown the overexpression of hepsin in prostate cancer, and the dysregulation of hepsin …

Expression profiling reveals hepsin overexpression in prostate cancer

JA Magee, T Araki, S Patil, T Ehrig, L True… - Cancer research, 2001 - AACR
Prostate cancer is the most commonly diagnosed noncutaneous cancer in men. Despite this
fact, many of the genetic changes that coincide with prostate cancer progression remain …

Hepatocyte growth factor is a preferred in vitro substrate for human hepsin, a membrane-anchored serine protease implicated in prostate and ovarian cancers

S Herter, DE Piper, W Aaron, T Gabriele… - Biochemical …, 2005 - portlandpress.com
Hepsin is a membrane-anchored, trypsin-like serine protease with prominent expression in
the human liver and tumours of the prostate and ovaries. To better understand the biological …

Design, synthesis, and testing of potent, selective hepsin inhibitors via application of an automated closed-loop optimization platform

SM Pant, A Mukonoweshuro, B Desai… - Journal of medicinal …, 2018 - ACS Publications
Hepsin is a membrane-anchored serine protease whose role in hepatocyte growth factor
(HGF) signaling and epithelial integrity makes it a target of therapeutic interest in …