ArticleACS medicinal chemistry letters2019
Novel Small Molecule-Derived, Highly Selective Substrates for Fibroblast Activation Protein (FAP).
Article in ACS medicinal chemistry letters, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 16 papers.
What it found
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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.
The trial behind it
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
16 citing papers in PubMed, 50 citations in OpenAlex.
- Homomultimeric FAP Inhibitor-Based Radioligands for Cancer Theranostics: Design Principles, Structure-Function Relationships, and Preclinical Performance.Molecules (Basel, Switzerland) · 2026Review
- Reduced Activity of Soluble Fibroblast Activation Protein (sFAP) Represents a Biomarker of Aggressive Disease in Lymphoid Malignancies.International journal of molecular sciences · 2025Article
- Preclinical evaluation of [EJNMMI radiopharmacy and chemistry · 2025Article
- Macrocyclic Phage Display for Identification of Selective Protease Substrates.Journal of the American Chemical Society · 2025Article
- Review
- Cosolvent Molecular Dynamics Applied to DPP4, DPP8 and DPP9: Reproduction of Important Binding Features and Use in Inhibitor Design.Journal of chemical information and modeling · 2024Article
- Article
- Establishment of FAP-overexpressing Cells for FAP-targeted Theranostics.Current medical science · 2023Article
- Novel Generation of FAP Inhibitor-Based Homodimers for Improved Application in Radiotheranostics.Cancers · 2023Article
- Role and mechanism of fibroblast-activated protein-α expression on the surface of fibroblast-like synoviocytes in rheumatoid arthritis.Frontiers in immunology · 2023Review
- From Automated Synthesis to In Vivo Application in Multiple Types of Cancer-Clinical Results with [Pharmaceuticals (Basel, Switzerland) · 2022Article
- In Vitro Evaluation of the Squaramide-Conjugated Fibroblast Activation Protein Inhibitor-Based Agents AAZTAMolecules (Basel, Switzerland) · 2021Article
- Review
- Overcoming stromal barriers to immuno-oncological responses via fibroblast activation protein-targeted therapy.Immunotherapy · 2021Article
- Article
- Targeting fibroblast activation protein (FAP): next generation PET radiotracers using squaramide coupled bifunctional DOTA and DATAEJNMMI radiopharmacy and chemistry · 2020Article
Corrections and comments
- Erratum issued
Authors and funding
13 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Fibroblast activation protein (FAP) is a proline-selective serine protease. It is hardly expressed in healthy adult tissue but upregulated in tissue remodeling sites associated with several diseases including epithelial cancer types, atherosclerosis, arthritis and fibrosis. Ongoing research aims at clinical implementation of FAP as a biomarker for these diseases. Several immunochemical methods that quantify FAP expression have been reported. An alternative/complementary approach focuses on quantification of FAP's enzymatic activity. Developing an activity-based assay for FAP has nonetheless proven challenging because of selectivity issues with respect to prolyl oligopeptidase (PREP). Here, we present substrate-type FAP probes that are structurally derived from a FAP-inhibitor (UAMC1110) that we published earlier. Both cleavage efficiency and FAP-selectivity of the best compounds in the series equal or surpass the most advanced peptide-based FAP substrates reported to date. Finally, proof-of-concept is provided that 4-aminonaphthol containing probes can spatially localize FAP activity in biological samples.
Identifiers
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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.