ArticleProceedings of the National Academy of Sciences of the United States of America2006
Synthetic small molecule furin inhibitors derived from 2,5-dideoxystreptamine.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2006. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 42 papers.
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Who cites it
42 citing papers in PubMed, 87 citations in OpenAlex.
- Design, Synthesis, and Characterization of Dichlorobiphenyl-Derived Inhibitors of the Proprotein Convertase Furin.Journal of medicinal chemistry · 2025Article
- In Vitro Evaluation of Antipseudomonal Activity and Safety Profile of Peptidomimetic Furin Inhibitors.Biomedicines · 2024Article
- Development and Prospects of Furin Inhibitors for Therapeutic Applications.International journal of molecular sciences · 2024Review
- Functional Roles of Furin in Cardio-Cerebrovascular Diseases.ACS pharmacology & translational science · 2024Review
- The Role of Proprotein Convertases in Upper Airway Remodeling.Molecules and cells · 2022Review
- Dichlorophenylpyridine-Based Molecules Inhibit Furin through an Induced-Fit Mechanism.ACS chemical biology · 2022Article
- A perspective on the applications of furin inhibitors for the treatment of SARS-CoV-2.Pharmacological reports : PR · 2022Article
- The Path to Therapeutic Furin Inhibitors: From Yeast Pheromones to SARS-CoV-2.International journal of molecular sciences · 2022Review
- OFF-State-Specific Inhibition of the Proprotein Convertase Furin.ACS chemical biology · 2021Article
- The interactions of folate with the enzyme furin: a computational study.RSC advances · 2021Article
- Design and Structure-Activity Relationship of a Potent Furin Inhibitor Derived from Influenza Hemagglutinin.ACS medicinal chemistry letters · 2021Article
- Role of proteolytic enzymes in the COVID-19 infection and promising therapeutic approaches.Biochemical pharmacology · 2020Review
- Potential Therapeutic Agents and Associated Bioassay Data for COVID-19 and Related Human Coronavirus Infections.ACS pharmacology & translational science · 2020Review
- Involvement of Spike Protein, Furin, and ACE2 in SARS-CoV-2-Related Cardiovascular Complications.SN comprehensive clinical medicine · 2020Review
- The Proteolytic Regulation of Virus Cell Entry by Furin and Other Proprotein Convertases.Viruses · 2019Review
- Proprotein convertase inhibition: Paralyzing the cell's master switches.Biochemical pharmacology · 2017Review
- Structure of the unliganded form of the proprotein convertase furin suggests activation by a substrate-induced mechanism.Proceedings of the National Academy of Sciences of the United States of America · 2016Article
- Highly predictive support vector machine (SVM) models for anthrax toxin lethal factor (LF) inhibitors.Journal of molecular graphics & modelling · 2016Article
- Identification of potent and compartment-selective small molecule furin inhibitors using cell-based assays.Biochemical pharmacology · 2015Article
- Small molecule proprotein convertase inhibitors for inhibition of embryo implantation.PloS one · 2013Article
Corrections and comments
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Authors and funding
10 authors at 5 institutions in 2 countries.
Funding
Abstract
Furin plays a crucial role in embryogenesis and homeostasis and in diseases such as Alzheimer's disease, cancer, and viral and bacterial infections. Thus, inhibition of furin may provide a feasible and promising approach for therapeutic intervention of furin-mediated disease mechanisms. Here, we report on a class of small molecule furin inhibitors based on 2,5-dideoxystreptamine. Derivatization of 2,5-dideoxystreptamine by the addition of guanidinylated aryl groups yielded a set of furin inhibitors with nanomolar range potency against furin when assayed in a biochemical cleavage assay. Moreover, a subset of these furin inhibitors protected RAW 264.7 macrophage cells from toxicity caused by furin-dependent processing of anthrax protective antigen. These inhibitors were found to behave as competitive inhibitors of furin and to be relatively specific for furin. Molecular modeling revealed that these inhibitors may target the active site of furin as they showed site occupancy similar to the alkylating inhibitor decanoyl-Arg-Val-Lys-Arg-CH(2)Cl. The compounds presented here are bona fide synthetic small molecule furin inhibitors that exhibit potency in the nanomolar range, suggesting that they may serve as valuable tools for studying furin action and potential therapeutics agents for furin-dependent diseases.
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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.