Second messenger Ap<sub>4</sub>A polymerizes target protein HINT1 to transduce signals in FcεRI-activated mast cells.

Yu, Jing; Liu, Zaizhou; Liang, Yuanyuan; Luo, Feng; Zhang, Jie; Tian, Cuiping; Motzik, Alex; Zheng, Mengmeng et al. · Nat Commun · 2019

basic_science · Level V

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Abstract

Signal transduction systems enable organisms to monitor their external environments and accordingly adjust the cellular processes. In mast cells, the second messenger Ap<sub>4</sub>A binds to the histidine triad nucleotide-binding protein 1 (HINT1), disrupts its interaction with the microphthalmia-associated transcription factor (MITF), and eventually activates the transcription of genes downstream of MITF in response to immunostimulation. How the HINT1 protein recognizes and is regulated by Ap<sub>4</sub>A remain unclear. Here, using eight crystal structures, biochemical experiments, negative stain electron microscopy, and cellular experiments, we report that Ap<sub>4</sub>A specifically polymerizes HINT1 in solution and in activated rat basophilic leukemia cells. The polymerization interface overlaps with the area on HINT1 for MITF interaction, suggesting a possible competitive mechanism to release MITF for transcriptional activation. The mechanism depends precisely on the length of the phosphodiester linkage of Ap<sub>4</sub>A. These results highlight a direct polymerization signaling mechanism by the second messenger.

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