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 …

Hepsin cooperates with MYC in the progression of adenocarcinoma in a prostate cancer mouse model

S Nandana, K Ellwood‐Yen, C Sawyers, M Wills… - The …, 2010 - Wiley Online Library
BACKGROUND Hepsin is a cell surface protease that is over‐expressed in more than 90%
of human prostate cancer cases. The previously developed Probasin‐hepsin/Large …

[HTML][HTML] Regulation of type II transmembrane serine proteinase TMPRSS6 by hypoxia-inducible factors: new link between hypoxia signaling and iron homeostasis

S Lakhal, J Schödel, ARM Townsend, CW Pugh… - Journal of Biological …, 2011 - ASBMB
Hepcidin is a liver-derived hormone with a key role in iron homeostasis. In addition to iron, it
is regulated by inflammation and hypoxia, although mechanisms of hypoxic regulation …

Clinical relevance of hepsin and hepatocyte growth factor activator inhibitor type 2 expression in renal cell carcinoma

H Betsunoh, S Mukai, Y Akiyama, T Fukushima… - Cancer …, 2007 - Wiley Online Library
Cell surface proteolysis is important for the generation of bioactive proteins mediating tumor
progression. Recent studies suggest that the membrane‐anchored cell surface proteinases …

Allosteric antibody inhibition of human hepsin protease

T Koschubs, S Dengl, H Dürr, K Kaluza… - Biochemical …, 2012 - portlandpress.com
Hepsin is a type II transmembrane serine protease that is expressed in several human
tissues. Overexpression of hepsin has been found to correlate with tumour progression and …

[HTML][HTML] The structure of the extracellular region of human hepsin reveals a serine protease domain and a novel scavenger receptor cysteine-rich (SRCR) domain

JR Somoza, JD Ho, C Luong, M Ghate, PA Sprengeler… - Structure, 2003 - cell.com
Hepsin is an integral membrane protein that may participate in cell growth and in
maintaining proper cell morphology and is overexpressed in a number of primary tumors …

[PDF][PDF] Gene targeting in hemostasis. Hepsin

Q Wu - Front Biosci, 2001 - article.imrpress.com
Introduction 3. Hepsin cDNA and gene structures 3.1. Cloning of hepsin cDNA 3.2. Hepsin
gene structure 3.3. The promoter sequence of the mouse hepsin gene. 4. Hepsin protein 4.1 …

[PDF][PDF] Hepcidin signaling in health and disease: ironing out the details

KV Kowdley, EM Gochanour… - Hepatology …, 2021 - Wiley Online Library
Hepcidin, a peptide hormone produced by hepatocytes, is the central regulator of systemic
iron homeostasis through its interaction with ferroportin, the major cellular iron export …

Hepsin is highly over expressed in and a new candidate for a prognostic indicator in prostate cancer

C Stephan, GM Yousef, A Scorilas, K Jung… - The Journal of …, 2004 - auajournals.org
Purpose: Other cDNA microarray studies have shown that hepsin is one of the highly over
expressed genes in prostate cancer tissue compared with nonmalignant and benign …

[HTML][HTML] Heparanase overexpression reduces hepcidin expression, affects iron homeostasis and alters the response to inflammation

M Asperti, T Stuemler, M Poli, M Gryzik, L Lifshitz… - PloS one, 2016 - journals.plos.org
Hepcidin is the key regulator of systemic iron availability that acts by controlling the
degradation of the iron exporter ferroportin. It is expressed mainly in the liver and regulated …