ArticleThe Biochemical journal1993
The synthesis of inhibitors for processing proteinases and their action on the Kex2 proteinase of yeast.
Article in The Biochemical journal, 1993. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 64 citations in OpenAlex.
- Development and Prospects of Furin Inhibitors for Therapeutic Applications.International journal of molecular sciences · 2024Review
- Inhibition of the galactosyltransferase C1GALT1 reduces osteosarcoma cell proliferation by interfering with ERK signaling and cell cycle progression.Cancer gene therapy · 2024Article
- Permethrin as a Potential Furin Inhibitor through a Novel Non-Competitive Allosteric Inhibition.Molecules (Basel, Switzerland) · 2023Article
- Discovery of diminazene as a dual inhibitor of SARS-CoV-2 human host proteases TMPRSS2 and furin using cell-based assays.Current research in chemical biology · 2022Article
- Analysis of cathepsin and furin proteolytic enzymes involved in viral fusion protein activation in cells of the bat reservoir host.PloS one · 2015Article
- Proteolysis during tumor cell extravasation in vitro: metalloproteinase involvement across tumor cell types.PloS one · 2013Article
- Inhibition of prohormone convertases PC1/3 and PC2 by 2,5-dideoxystreptamine derivatives.Molecular pharmacology · 2012Article
- Furin overexpression suppresses tumor growth and predicts a better postoperative disease-free survival in hepatocellular carcinoma.PloS one · 2012Article
- On the cutting edge of proprotein convertase pharmacology: from molecular concepts to clinical applications.Biomolecular concepts · 2011Article
- Proprotein convertase inhibition results in decreased skin cell proliferation, tumorigenesis, and metastasis.Neoplasia (New York, N.Y.) · 2010Article
- Selective and potent furin inhibitors protect cells from anthrax without significant toxicity.The international journal of biochemistry & cell biology · 2010Article
- Comparative study of the binding pockets of mammalian proprotein convertases and its implications for the design of specific small molecule inhibitors.International journal of biological sciences · 2010Article
- Synthetic small-molecule prohormone convertase 2 inhibitors.Molecular pharmacology · 2009Article
- Subtilisin-like proprotein convertase activity is necessary for left-right axis determination in Xenopus neurula embryos.Development genes and evolution · 2006Article
- Protection from anthrax toxin-mediated killing of macrophages by the combined effects of furin inhibitors and chloroquine.Antimicrobial agents and chemotherapy · 2005Article
- Increased furin activity enhances the malignant phenotype of human head and neck cancer cells.The American journal of pathology · 2003Article
- Effects of L- and D-REKR amino acid-containing peptides on HIV and SIV envelope glycoprotein precursor maturation and HIV and SIV replication.The Biochemical journal · 2002Article
- Endocytic delivery of intramolecularly quenched substrates and inhibitors to the intracellular yeast Kex2 protease1.The Biochemical journal · 1999Article
- Characterization of structural determinants and molecular mechanisms involved in pro-stromelysin-3 activation by 4-aminophenylmercuric acetate and furin-type convertases.The Biochemical journal · 1996Article
- The neuroendocrine polypeptide 7B2 is an endogenous inhibitor of prohormone convertase PC2.Proceedings of the National Academy of Sciences of the United States of America · 1994Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
Peptidyl chloromethane and sulphonium salts containing multiple Arg and Lys residues were synthesized as potential inhibitors of prohormone and pro-protein processing proteinases. The potencies of these compounds were assayed by measuring the kinetics of inactivation of the yeast Kex2 proteinase, the prototype of a growing family of eukaryotic precursor processing proteinases. The most potent inhibitor, Pro-Nvl-Tyr-Lys-Arg-chloromethane, was based on cleavage sites in the natural Kex2 substrate pro-alpha-factor. This inhibitor exhibited a Ki of 3.7 nM and a second-order inactivation rate constant (k2/Ki) of 1.3 x 10(7) M-1.s-1 comparable with the value of kcat./Km obtained with Kex2 for the corresponding peptidyl methylcoumarinylamide substrate. The enzyme exhibited sensitivity to the other peptidyl chloromethanes over a range of concentrations, depending on peptide sequence and alpha-amino decanoylation, but was completely resistant to peptidyl sulphonium salts. Kinetics of inactivation by these new inhibitors of a set of 'control' proteinases, including members of both the trypsin and subtilisin families, underscored the apparent specificity of the compounds most active against Kex2 proteinase.
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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.