ArticleACS medicinal chemistry letters2016
Cathepsin B Inhibitors: Combining Dipeptide Nitriles with an Occluding Loop Recognition Element by Click Chemistry.
Article in ACS medicinal chemistry letters, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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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
11 citing papers in PubMed, 35 citations in OpenAlex.
- Redirecting the Peptide Cleavage Causes Protease Inactivation.Angewandte Chemie (International ed. in English) · 2025Article
- Micellar "Click" Nanoreactors: Spiking Pluronic-Based Micelles with Polymeric Ligands.Macromolecules · 2024Article
- Synthesis of Fluorescent C-C Bonded Triazole-Purine Conjugates.Journal of fluorescence · 2024Article
- Development of a Peptide-Based Nano-Sized Cathepsin B Inhibitor for Anticancer Therapy.Pharmaceutics · 2023Article
- Dipeptide-Derived Alkynes as Potent and Selective Irreversible Inhibitors of Cysteine Cathepsins.Journal of medicinal chemistry · 2023Article
- Nitriles: an attractive approach to the development of covalent inhibitors.RSC medicinal chemistry · 2023Review
- Article
- Mapping the S1 and S1' subsites of cysteine proteases with new dipeptidyl nitrile inhibitors as trypanocidal agents.PLoS neglected tropical diseases · 2020Article
- Modification at the 2'-Position of the 4,5-Series of 2-Deoxystreptamine Aminoglycoside Antibiotics To Resist Aminoglycoside Modifying Enzymes and Increase Ribosomal Target Selectivity.ACS infectious diseases · 2019Article
- Cysteine-type cathepsins promote the effector phase of acute cutaneous delayed-type hypersensitivity reactions.Theranostics · 2019Article
- Addition of 2-(ethylamino)acetonitrile group to nitroxoline results in significantly improved anti-tumor activityOncotarget · 2017Article
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
An active site mapping of human cathepsin B with dipeptide nitrile inhibitors was performed for a combinatorial approach by introducing several points of diversity and stepwise optimizing the inhibitor structure. To address the occluding loop of cathepsin B by a carboxylate moiety, click chemistry to generate linker-connected molecules was applied. Inhibitor 17 exhibited K i values of 41.3 nM, 27.3 nM, or 19.2 nM, depending on the substrate and pH of the assay. Kinetic data were discussed with respect to the conformational selection and induced fit models.
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Registered trials
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