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Updated: Aug 28, 2025

Author Spotlight: Development of a Method for Identifying Small Molecular Antagonists of β2 Integrin Activation
Published on: February 2, 2024
It's the water! The open and shut case of drug-induced integrin activation
1Allen and Frances Adler Laboratory of Blood and Vascular Biology, Rockefeller University, New York, NY 10065, USA.
Abstract:
Integrin receptors are established drug targets, but many of the drugs that have been developed act as partial agonists, inducing the receptor into a high-affinity, ligand-binding state. Lin et al. discovered a general mechanism to circumvent this problem-stabilizing a key water molecule that prevents receptor activation. Their findings are likely to impact future therapeutic development.
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