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Biological Chemistry

Editor-in-Chief: Brüne, Bernhard

Editorial Board: Buchner, Johannes / Lei, Ming / Ludwig, Stephan / Thomas, Douglas D. / Turk, Boris / Wittinghofer, Alfred


IMPACT FACTOR 2018: 3.014
5-year IMPACT FACTOR: 3.162

CiteScore 2018: 3.09

SCImago Journal Rank (SJR) 2018: 1.482
Source Normalized Impact per Paper (SNIP) 2018: 0.820

Online
ISSN
1437-4315
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Volume 391, Issue 4

Issues

Prostate-specific antigen: an overlooked candidate for the targeted treatment and selective imaging of prostate cancer

Aaron M. LeBeau
  • Department of Pharmacology and Molecular Science, The Johns Hopkins University School of Medicine, 75 N. Wolfe St., Baltimore, MD 2131, USA
  • Present address: Department of Pharmaceutical Chemistry, University of California, San Francisco, 600 16th St., San Francisco, CA 94158, USA.
  • Other articles by this author:
  • De Gruyter OnlineGoogle Scholar
/ Maya Kostova
  • The Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins, The Johns Hopkins University School of Medicine, 1650 Orleans St., Baltimore, MD 21231, USA
  • Other articles by this author:
  • De Gruyter OnlineGoogle Scholar
/ Charles S. Craik
  • Department of Pharmaceutical Chemistry, University of California, San Francisco, 600 16th St., San Francisco, CA 94158, USA
  • Other articles by this author:
  • De Gruyter OnlineGoogle Scholar
/ Samuel R. Denmeade
  • Department of Pharmacology and Molecular Science, The Johns Hopkins University School of Medicine, 75 N. Wolfe St., Baltimore, MD 2131, USA
  • The Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins, The Johns Hopkins University School of Medicine, 1650 Orleans St., Baltimore, MD 21231, USA
  • Other articles by this author:
  • De Gruyter OnlineGoogle Scholar
Published Online: 2010-02-24 | DOI: https://doi.org/10.1515/bc.2010.044

Abstract

The role of prostate-specific antigen (PSA) or kallikrein-related peptidase 3 (KLK3) as a biomarker for prostate cancer is well known; however, the precise physiological role of it's serine protease activity in prostate cancer remains a mystery. PSA is produced at high levels by both androgen-dependent and -independent prostate cancers. Studies have documented high levels of active PSA in the milieu surrounding osseous and soft tissue metastases. This evidence, coupled with growing experimental evidence, suggests that PSA plays an important role in the pathobiology of prostate cancer. These observations support the development of PSA-selective inhibitors as useful tools for the targeted treatment and imaging of prostate cancer. Here, we review the research that has been conducted to date on developing selective inhibitors for PSA. The different approaches used to determine PSA substrate specificity and for creating inhibitors are discussed. In addition, the unique active site characteristics of PSA and how these motifs aided our research in developing PSA targeted agents are highlighted.

Keywords: human kallikrein-related peptidase 3; inhibition; prostate cancer; prostate-specific antigen; serine protease; small molecule

About the article

Corresponding author


Received: 2009-11-18

Accepted: 2010-01-18

Published Online: 2010-02-24

Published in Print: 2010-04-01


Citation Information: Biological Chemistry, Volume 391, Issue 4, Pages 333–343, ISSN (Online) 1437-4315, ISSN (Print) 1431-6730, DOI: https://doi.org/10.1515/bc.2010.044.

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