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Papers of the Week


Papers: 21 Dec 2019 - 27 Dec 2019


Pharmacology/Drug Development


2020 01 21


Anal Chem


92


2

Visualizing TRPA1 in the plasma membrane for rapidly screening optical control agonists via a photochromic ligand based fluorescent probe.

Authors

Qiao Z, Qi H, Zhang H, Zhou Q, Wei N, Zhang Y, Wang K
Anal Chem. 2020 01 21; 92(2):1934-1939.
PMID: 31855414.

Abstract

Fluorescent probes have been used as effective methods for profiling proteins in biological system because of their high selectivity, sensitivity and temporal-spatial resolution. A specific fluorescent probe for understanding the function of the transient receptor potential ankyrin 1 (TRPA1) channel that is closely related with various diseases like persistent pain, respiratory and chronic itch syndromes, however, is still lacking. Here, we report a "turn-on" fluorescent probe (A1CA) for visualizing TRPA1 channels in the plasma membrane of live cells based on a photochromic ligand derived from 4-(phenylazo)benzenamine. Evaluating of the specificity and sensitivity of A1CA by electrophysiology and confocal imaging showed that A1CA probe displays higher affinity and selectivity to TRPA1 channel versus all other ion channels including TRPV1, TRPV3, Nav1.4, Nav1.5 and hERG. Based on the supporting evidence, A1CA has great potential as a molecular imaging probe for high-throughput screening of novel TRPA1 agonists.