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TitleStructural insights into TRPV2 activation by small molecules.
Journal, issue, pagesNat Commun, Vol. 13, Issue 1, Page 2334, Year 2022
Publish dateApr 28, 2022
AuthorsRuth A Pumroy / Anna D Protopopova / Tabea C Fricke / Iris U Lange / Ferdinand M Haug / Phuong T Nguyen / Pamela N Gallo / Bárbara B Sousa / Gonçalo J L Bernardes / Vladimir Yarov-Yarovoy / Andreas Leffler / Vera Y Moiseenkova-Bell /
PubMed AbstractTransient receptor potential vanilloid 2 (TRPV2) is involved in many critical physiological and pathophysiological processes, making it a promising drug target. Here we present cryo-electron ...Transient receptor potential vanilloid 2 (TRPV2) is involved in many critical physiological and pathophysiological processes, making it a promising drug target. Here we present cryo-electron microscopy (cryo-EM) structures of rat TRPV2 in lipid nanodiscs activated by 2-aminoethoxydiphenyl borate (2-APB) and propose a TRPV2-specific 2-ABP binding site at the interface of S5 of one monomer and the S4-S5 linker of the adjacent monomer. In silico docking and electrophysiological studies confirm the key role of His521 and Arg539 in 2-APB activation of TRPV2. Additionally, electrophysiological experiments show that the combination of 2-APB and cannabidiol has a synergetic effect on TRPV2 activation, and cryo-EM structures demonstrate that both drugs were able to bind simultaneously. Together, our cryo-EM structures represent multiple functional states of the channel, providing a native picture of TRPV2 activation by small molecules and a structural framework for the development of TRPV2-specific activators.
External linksNat Commun / PubMed:35484159 / PubMed Central
MethodsEM (single particle)
Resolution3.5 - 4.15 Å
Structure data

24109

7n0m

EMDB-24109, PDB-7n0m:
Inactivated state of 2-APB-bound wildtype rat TRPV2 in nanodiscs
Method: EM (single particle) / Resolution: 3.5 Å

24110

7n0n

EMDB-24110, PDB-7n0n:
Activated state of 2-APB-bound wildtype rat TRPV2 in nanodiscs
Method: EM (single particle) / Resolution: 4.15 Å

25650

7t37

EMDB-25650, PDB-7t37:
Activated state of 2-APB and CBD-bound wildtype rat TRPV2 in nanodiscs
Method: EM (single particle) / Resolution: 3.7 Å

25651

7t38

EMDB-25651, PDB-7t38:
Inactivated state of 2-APB and CBD-bound wildtype rat TRPV2 in nanodiscs
Method: EM (single particle) / Resolution: 3.8 Å

Chemicals

ChemComp-FZ4:
2-aminoethyl diphenylborinate

ChemComp-P0T:
cannabidiol

Source
  • rattus norvegicus (Norway rat)
KeywordsTRANSPORT PROTEIN / TRP channel / ion channel / TRPV

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