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Updated: Aug 13, 2026

Identification of Small Molecule-binding Proteins in a Native Cellular Environment by Live-cell Photoaffinity Labeling
Published on: September 20, 2016
Avermectin chemistry and action: ester- and ether-type candidate photoaffinity probes
Y Tsukamoto1, L M Cole, J E Casida
1Department of Environmental Science, Policy and Management, University of California, Berkeley 94720-3112, USA.
Abstract:
Avermectin B1a (1) is a potent anthelmintic, insecticide, miticide and chloride channel activator on interaction with a specific nerve membrane site analyzed by binding assays with [3H]1. Candidate photoaffinity probes were prepared replacing the dioleandrosyl substituent with potential isosteric esters and ethers approximating the original overall atom length and terminating in a phenyl moiety substituted with azido, iodo or hydroxy. Several of the candidates met the goal of high potency on mouse, housefly and fruit fly brain chloride channels with IC50 values of 7-57 nM in competing for the [3H]1 binding site.
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