REVIEW: TRPV1 Ion Channel: Structural Features, Activity Modulators, and Therapeutic Potential

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Irina N. Gladkikh¹, Oksana V. Sintsova¹, Elena V. Leychenko¹, and Sergey A. Kozlov^2,a*

¹Elyakov Pacific Institute of Bioorganic Chemistry, Far East Branch of the Russian Academy of Sciences, 690022 Vladivostok, Russia

²Shemyakin and Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, 117997 Moscow, Russia

^* To whom correspondence should be addressed.

Received August 28, 2020; Revised November 19, 2020; Accepted November 19, 2020

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Although TRPV1 ion channel has been attracting researchers’ attention for many years, its functions in animal organisms, the principles of regulation, and the involvement in pathological processes have not yet been fully clarified. Mutagenesis experiments and structural studies have identified the structural features of the channel and binding sites for its numerous ligands; however, these studies are far from conclusion. This review summarizes recent achievements in the TRPV1 research with special focus on structural and functional studies of the channel and on its ligands, which are extremely diverse in their nature and interaction specificity to TRPV1. Particular attention was given to the effects of numerous endogenous agonists and antagonists that can fine-tune the channel sensitivity to its usual activators, such as capsaicin, heat, acids, or their combination. In addition to the pain sensing not covered in this review, the TRPV1 channel was found to be involved in the regulation of many important physiological and pathological processes and, therefore, can be considered as a promising therapeutic target in the treatment of various diseases, such as pneumonia, ischemia, diabetes, epilepsy, schizophrenia, psoriasis, etc.

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KEY WORDS: TRPV1 ion channel, capsaicin receptor, structural and functional studies, multimodal activation, therapeutic target, vanilloids, drug development

DOI: 10.1134/S0006297921140054

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