ArticleBioorganic & medicinal chemistry2009
Optimization of peptide-based inhibitors of prostate-specific antigen (PSA) as targeted imaging agents for prostate cancer.
Article in Bioorganic & medicinal chemistry, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
15 citing papers in PubMed, 31 citations in OpenAlex.
- Article
- Non-Canonical Amino Acids in Analyses of Protease Structure and Function.International journal of molecular sciences · 2023Review
- Remodelling of the tumour microenvironment by the kallikrein-related peptidases.Nature reviews. Cancer · 2022Review
- A Suite of Activity-Based Probes To Dissect the KLK Activome in Drug-Resistant Prostate Cancer.Journal of the American Chemical Society · 2021Article
- Mechanism of semen liquefaction and its potential for a novel non-hormonal contraception†.Biology of reproduction · 2020Review
- Hsp70 and gama-Semino protein as possible prognostic marker of prostate cancer.Frontiers in bioscience (Landmark edition) · 2018Review
- Unleashing the therapeutic potential of human kallikrein-related serine proteases.Nature reviews. Drug discovery · 2015Review
- Prostate-specific kallikrein-related peptidases and their relation to prostate cancer biology and detection. Established relevance and emerging roles.Thrombosis and haemostasis · 2013Review
- Peptide-conjugated pterins as inhibitors of ricin toxin A.Journal of medicinal chemistry · 2013Article
- Synthesis and characterization of a novel prostate cancer-targeted phosphatidylinositol-3-kinase inhibitor prodrug.Journal of medicinal chemistry · 2012Article
- Virtual Screening and X-ray Crystallography for Human Kallikrein 6 Inhibitors with an Amidinothiophene P1 Group.ACS medicinal chemistry letters · 2012Article
- Prodrug enzymes and their applications in image-guided therapy of cancer: tracking prodrug enzymes to minimize collateral damage.Drug delivery and translational research · 2012Article
- Review
- Prostate-specific antigen: an overlooked candidate for the targeted treatment and selective imaging of prostate cancer.Biological chemistry · 2010Review
- Prostate cancer-targeted imaging using magnetofluorescent polymeric nanoparticles functionalized with bombesin.Pharmaceutical research · 2010Article
Corrections and comments
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Authors and funding
5 authors at 3 institutions in 1 country.
Funding
Abstract
Prostate-specific antigen (PSA) is a serine protease biomarker that may play a role in prostate cancer development and progression. The inhibition of PSA's enzymatic activity with small molecule inhibitors is an attractive and, as of yet, unexploited target. Previously, we reported a series of peptidyl aldehyde and boronic acid based inhibitors of PSA. In this study, the structural requirements in the P2 and P3 positions of peptide-based PSA inhibitors are explored through the substitution of a series of natural and unnatural amino acids in these positions. This analysis demonstrated a preference for hydrophobic residues in the P2 position and amino acids with the potential to hydrogen bond in the P3 position. Using this information, a peptide boronic acid inhibitor with the sequence Cbz-Ser-Ser-Gln-Nle-(boro)-Leu was identified with a K(i) for PSA of 25nM. The attachment of a bulky metal chelating group to the amino terminal of this peptide did not adversely affect PSA inhibition. This result suggests that a platform of PSA inhibitor chelates could be developed as SPECT or PET-based imaging agents for prostate cancer.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.