ArticleChemistry (Weinheim an der Bergstrasse, Germany)2016
Fragment-Based Drug Design Facilitated by Protein-Templated Click Chemistry: Fragment Linking and Optimization of Inhibitors of the Aspartic Protease Endothiapepsin.
Article in Chemistry (Weinheim an der Bergstrasse, Germany), 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed.
- Inhibitors of GapN-dependent NADPH supply as potential lead compounds for novel therapeutics againstVirulence · 2026Article
- An Orthogonal 'Clickable' Xyloside Scaffold inMolecules (Basel, Switzerland) · 2026Article
- Click Reactions in Kinetic Target-Guided Synthesis: Progress in the Discovery of Inhibitors for Biological Targets.Methods and protocols · 2026Review
- Diradical-singlet character of 1,3-dipoles affects reactivity of 1,3-dipolar cycloaddition reactions and intramolecular cyclization.Journal of molecular modeling · 2019Article
- Proteintemplat-gesteuerte Fragmentligationen - von der molekularen Erkennung zur Wirkstofffindung.Angewandte Chemie (Weinheim an der Bergstrasse, Germany) · 2017Article
- Protein-Templated Fragment Ligations-From Molecular Recognition to Drug Discovery.Angewandte Chemie (International ed. in English) · 2017Review
- Fragment-Based Drug Design Facilitated by Protein-Templated Click Chemistry: Fragment Linking and Optimization of Inhibitors of the Aspartic Protease Endothiapepsin.Chemistry (Weinheim an der Bergstrasse, Germany) · 2016Article
Corrections and comments
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Authors and funding
6 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
There is an urgent need for the development of efficient methodologies that accelerate drug discovery. We demonstrate that the strategic combination of fragment linking/optimization and protein-templated click chemistry is an efficient and powerful method that accelerates the hit-identification process for the aspartic protease endothiapepsin. The best binder, which inhibits endothiapepsin with an IC
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Registered trials
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