ArticleJournal of medicinal chemistry2013
Novel pyridazinone inhibitors for vascular adhesion protein-1 (VAP-1): old target-new inhibition mode.
Article in Journal of medicinal chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers, 1 of them a synthesis that pooled it.
What it found
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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.
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Who cites it
19 citing papers in PubMed, 1 synthesis or guideline pooled it, 34 citations in OpenAlex.
- Association between female circulating heavy metal concentration and abortion: a systematic review and meta-analysis.Frontiers in endocrinology · 2023Pooled it
- Deep learning of tautomer stability from crystallographic proton positions.Chemical science · 2026Article
- Novel glycine amides, semicarbazides and fluoroallylamines as inhibitors of the amine oxidase vascular adhesion protein-1 (VAP-1).RSC medicinal chemistry · 2026Article
- Exploring the Binding Specificity of Siglec-Derived Peptides to Human Primary Amine Oxidase Using an Integrative Approach to Ligand Epitope Mapping.Computational and structural biotechnology journal · 2026Article
- Targeting vascular adhesion protein-1 and myeloperoxidase with a dual inhibitor SNT-8370 in preclinical models of inflammatory disease.Nature communications · 2025Article
- Pyridazinone: Current Progress in Synthesis of its Derivatives and Biological Activity.Medicinal chemistry (Shariqah (United Arab Emirates)) · 2025Review
- Vascular adhesion protein-1-targeted PET imaging in autoimmune myocarditis.Journal of nuclear cardiology : official publication of the American Society of Nuclear Cardiology · 2023Article
- Effects of Chemical Structures Interacting with Amine Oxidases on Glucose, Lipid and Hydrogen Peroxide Handling by Human Adipocytes.Molecules (Basel, Switzerland) · 2022Article
- The novel visual cycle inhibitor (±)-RPE65-61 protects retinal photoreceptors from light-induced degeneration.PloS one · 2022Article
- Amine oxidase copper-containing 3 (AOC3) inhibition: a potential novel target for the management of diabetic retinopathy.International journal of retina and vitreous · 2021Review
- SSAO/VAP-1 in Cerebrovascular Disorders: A Potential Therapeutic Target for Stroke and Alzheimer's Disease.International journal of molecular sciences · 2021Review
- Pathogenesis and Clinical Management of Mesenteric Fibrosis in Small Intestinal Neuroendocine Neoplasms: A Systematic Review.Journal of clinical medicine · 2020Review
- Human Copper-Containing Amine Oxidases in Drug Design and Development.Molecules (Basel, Switzerland) · 2020Review
- Comparison of Inhibitor and Substrate Selectivity between Rodent and Human Vascular Adhesion Protein-1.Mediators of inflammation · 2020Article
- HPLC-UV assay for the evaluation of inhibitors of plasma amine oxidase using crude bovine plasma.Journal of enzyme inhibition and medicinal chemistry · 2019Article
- Mapping the interaction site and effect of the Siglec-9 inflammatory biomarker on human primary amine oxidase.Scientific reports · 2018Article
- Oligomannosidic glycans at Asn-110 are essential for secretion of human diamine oxidase.The Journal of biological chemistry · 2018Article
- Small Molecule Lysyl Oxidase-like 2 (LOXL2) Inhibitors: The Identification of an Inhibitor Selective for LOXL2 over LOX.ACS medicinal chemistry letters · 2017Article
- Article
Corrections and comments
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Authors and funding
8 authors at 4 institutions in 3 countries.
Funding
Abstract
Vascular adhesion protein-1 (VAP-1) is a primary amine oxidase and a drug target for inflammatory and vascular diseases. Despite extensive attempts to develop potent, specific, and reversible inhibitors of its enzyme activity, the task has proven challenging. Here we report the synthesis, inhibitory activity, and molecular binding mode of novel pyridazinone inhibitors, which show specificity for VAP-1 over monoamine and diamine oxidases. The crystal structures of three inhibitor-VAP-1 complexes show that these compounds bind reversibly into a unique binding site in the active site channel. Although they are good inhibitors of human VAP-1, they do not inhibit rodent VAP-1 well. To investigate this further, we used homology modeling and structural comparison to identify amino acid differences, which explain the species-specific binding properties. Our results prove the potency and specificity of these new inhibitors, and the detailed characterization of their binding mode is of importance for further development of VAP-1 inhibitors.
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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.