ArticleACS medicinal chemistry letters2012
Design and synthesis of potent, selective inhibitors of matriptase.
Article in ACS medicinal chemistry letters, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 31 papers.
What it found
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The trial behind it
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Who cites it
31 citing papers in PubMed, 72 citations in OpenAlex.
- Article
- Structural basis of TMPRSS11D specificity and autocleavage activation.Nature communications · 2025Article
- From N-0385 to N-0920: Unveiling a Host-Directed Protease Inhibitor with Picomolar Antiviral Efficacy against Prevalent SARS-CoV-2 Variants.Journal of medicinal chemistry · 2025Article
- Development of ketobenzothiazole-based peptidomimetic TMPRSS13 inhibitors with low nanomolar potency.bioRxiv : the preprint server for biology · 2024Article
- RationalJournal of medicinal chemistry · 2024Article
- Use of protease substrate specificity screening in the rational design of selective protease inhibitors with unnatural amino acids: Application to HGFA, matriptase, and hepsin.Protein science : a publication of the Protein Society · 2024Article
- Improving binding entropy by higher ligand symmetry? - A case study with human matriptase.RSC medicinal chemistry · 2023Article
- Article
- In Vitro Pharmacokinetic Behavior of Antiviral 3-Amidinophenylalanine Derivatives in Rat, Dog and Monkey Hepatocytes.Biomedicines · 2023Article
- A High-AffinityPharmaceuticals (Basel, Switzerland) · 2022Article
- Peptidomimetic inhibitors of TMPRSS2 block SARS-CoV-2 infection in cell culture.Communications biology · 2022Article
- Article
- In vitro interaction of potential antiviral TMPRSS2 inhibitors with human serum albumin and cytochrome P 450 isoenzymes.Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie · 2022Article
- Proteolytic cleavage of Podocin by Matriptase exacerbates podocyte injury.The Journal of biological chemistry · 2020Article
- 3-Amidinophenylalanine-derived matriptase inhibitors can modulate hepcidin production in vitro.Naunyn-Schmiedeberg's archives of pharmacology · 2020Article
- Cell surface-anchored serine proteases in cancer progression and metastasis.Cancer metastasis reviews · 2019Review
- Piperidine carbamate peptidomimetic inhibitors of the serine proteases HGFA, matriptase and hepsin.MedChemComm · 2019Article
- Membrane-Anchored Serine Proteases and Protease-Activated Receptor-2-Mediated Signaling: Co-Conspirators in Cancer Progression.Cancer research · 2019Review
- Blocking the proteolytic activity of zymogen matriptase with antibody-based inhibitors.The Journal of biological chemistry · 2019Article
- Engineering a potent inhibitor of matriptase from the natural hepatocyte growth factor activator inhibitor type-1 (HAI-1) protein.The Journal of biological chemistry · 2018Article
Corrections and comments
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Matriptase is a member of the type II transmembrane serine protease family. Several studies have reported deregulated matriptase expression in several types of epithelial cancers, suggesting that matriptase constitutes a potential target for cancer therapy. We report herein a new series of slow, tight-binding inhibitors of matriptase, which mimic the P1-P4 substrate recognition sequence of the enzyme. Preliminary structure-activity relationships indicate that this benzothiazole-containing RQAR-peptidomimetic is a very potent inhibitor and possesses a good selectivity for matriptase versus other serine proteases. A molecular model was generated to elucidate the key contacts between inhibitor 1 and matriptase.
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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.