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Updated: Apr 19, 2026

Avidity-based Extracellular Interaction Screening AVEXIS for the Scalable Detection of Low-affinity Extracellular Receptor-Ligand Interactions
Published on: March 5, 2012
Rationally designed cooperatively enhanced receptors to magnify host-guest binding in water
Roshan W Gunasekara1, Yan Zhao
1Department of Chemistry, Iowa State University , Ames, Iowa 50011-3111, United States.
Abstract:
When disengaged interactions within a receptor are turned on by its guest, these intrahost interactions will contribute to the overall binding energy. Although such receptors are common in biology, their synthetic mimics are rare and difficult to design. By engineering conflictory requirements between intrareceptor electrostatic and hydrophobic interactions, we enabled complementary guests to eliminate the "electrostatic frustration" within the host and turn on the intrahost interactions. The result was a binding constant of Ka >10(5) M(-1) from ammonium-carboxylate salt bridges that typically function poorly in water. These cooperatively enhanced receptors displayed excellent selectivity in binding, despite a large degree of conformational flexibility in the structure.
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