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TitleStructural insights into TRPV2 modulation by probenecid.
Journal, issue, pagesNat Struct Mol Biol, Vol. 32, Issue 6, Page 1019-1029, Year 2025
Publish dateFeb 19, 2025
AuthorsJulia A Rocereta / Toni Sturhahn / Ruth A Pumroy / Tabea C Fricke / Christine Herzog / Andreas Leffler / Vera Moiseenkova-Bell /
PubMed AbstractThe transient receptor potential vanilloid 2 (TRPV2) cation channel is a key player in cardiovascular physiology and pathophysiology. Probenecid (PBC), an FDA-approved uricosuric agent thought to ...The transient receptor potential vanilloid 2 (TRPV2) cation channel is a key player in cardiovascular physiology and pathophysiology. Probenecid (PBC), an FDA-approved uricosuric agent thought to activate TRPV2, has shown promise in enhancing cardiovascular function in both preclinical and clinical studies. Here our electrophysiological data reveal that PBC significantly potentiates rat TRPV2 to known stimuli, and cryo electron microscopy structures show that PBC directly interacts with rat TRPV2 in a previously unidentified intracellular binding pocket. PBC binding at a conserved TRPV2-specific histidine prevents the channel from taking on the inactivated carboxyl-terminal conformation. This effect extends to TRPV1 and TRPV3 channels when glutamine is substituted with histidine at the corresponding position, increasing their sensitivity to PBC. While PBC alone does not induce TRPV2 opening, its combination with 2-aminoethoxydiphenyl borate enables the channel to adopt an intermediate, potentiated state. Our results offer insights into potential therapeutic advancements for TRPV2 through this pocket.
External linksNat Struct Mol Biol / PubMed:39972168
MethodsEM (single particle)
Resolution2.4 - 4.2 Å
Structure data

44156

9b3u

EMDB-44156, PDB-9b3u:
Rat TRPV2 WT bound to probenecid
Method: EM (single particle) / Resolution: 2.4 Å

44157

9b3v

EMDB-44157, PDB-9b3v:
Rat TRPV2 WT in the presence of probenecid and 2-APB
Method: EM (single particle) / Resolution: 4.2 Å

44158

9b3w

EMDB-44158, PDB-9b3w:
Rat TRPV2 E724A/D725A Apo
Method: EM (single particle) / Resolution: 2.5 Å

44159

9b3x

EMDB-44159, PDB-9b3x:
Rat TRPV2 E724A/D725A bound to 2-APB
Method: EM (single particle) / Resolution: 3.2 Å

44160

9b3y

EMDB-44160, PDB-9b3y:
Rat TRPV2 E724A/D725A bound to probenecid
Method: EM (single particle) / Resolution: 2.7 Å

44161

9b3z

EMDB-44161, PDB-9b3z:
Rat TRPV2 E724A/D725A bound to probenecid and 2-APB
Method: EM (single particle) / Resolution: 3.0 Å

Chemicals

ChemComp-PEX:
1,2-DIDECANOYL-SN-GLYCERO-3-PHOSPHOETHANOLAMINE

ChemComp-RTO:
4-(dipropylsulfamoyl)benzoic acid / medication*YM

ChemComp-FZ4:
2-aminoethyl diphenylborinate

Source
  • rattus norvegicus (Norway rat)
KeywordsMEMBRANE PROTEIN / TRPV2 / TRP channel / ion channel / probenecid / 2-APB

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