ArticleAngewandte Chemie (International ed. in English)2019
Single-Molecule Force Measurement Guides the Design of Multivalent Ligands with Picomolar Affinity.
Article in Angewandte Chemie (International ed. in English), 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.
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Who cites it
2 citing papers in PubMed, 14 citations in OpenAlex.
- Single-Molecule Imaging of Membrane Proteins on Vascular Endothelial Cells.Journal of lipid and atherosclerosis · 2023Review
- Multivalent Benzamidine Molecules for Plasmin Inhibition: Effect of Valency and Linker Length.ChemMedChem · 2022Article
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Authors and funding
9 authors at 3 institutions in 2 countries.
Funding
Abstract
Interaction of multiple entities and receptors, or multivalency is widely applied to achieve high affinity ligands for diagnostic and therapeutic purposes. However, lack of knowledge on receptor distribution in living subjects remains a challenge for rational structure design. Herein, we develop a force measurement platform to probe the distribution and separation of the cell surface vascular endothelial growth factor receptors (VEGFR) in live cells, and use this to assess the geometry of appropriate linkers for distinct multivalent binding modes. A tetravalent lead ZD-4, which was developed from an antitumor drug ZD6474 (Vandetanib) with combined hybrid binding effects, yielded a 2000-fold improvement in the binding affinity to VEGFR with IC
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Registered trials
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