9MKF

Rat TRPV2 bound to AV2-1 agonist

This is a non-PDB format compatible entry.

Summary for 9MKF

• Entry DOI: 10.2210/pdb9mkf/pdb
• EMDB information: 48325
• Descriptor: Transient receptor potential cation channel subfamily V member 2, 1,2-DIDECANOYL-SN-GLYCERO-3-PHOSPHOETHANOLAMINE, 1-[(4S)-1-(furan-2-sulfonyl)-1,2,3,4-tetrahydroquinolin-4-yl]cyclopropane-1-carboxylic acid (3 entities in total)
• Functional Keywords: trp channel, trpv2, membrane protein
• Biological source: Rattus norvegicus (Norway rat)
• Total number of polymer chains: 4
• Total formula weight: 352766.16

Authors

Rocereta, J.A.,Pumroy, R.A.,Moiseenkova-Bell, V.Y. (deposition date: 2024-12-17, release date: 2026-04-15)

Primary citation

Leipe, A.,Rocereta, J.A.,Pumroy, R.A.,Leffler, A.,Schaefer, M.,Moiseenkova-Bell, V.,Hill, K.
Defining AV2-1 as a novel pharmacological probe to target human and rodent TRPV2.
Br.J.Pharmacol., 2026

PubMed Abstract: Transient receptor potential vanilloid 2 (TRPV2) is a non-selective cation channel implicated in immune cell functions. However, progress in understanding TRPV2 has been limited by a lack of potent and selective pharmacological tools, particularly those targeting the human variant. We aimed to identify and characterise a novel small-molecule activator of TRPV2.

PubMed: 41913383
DOI: 10.1111/bph.70413

Experimental method

ELECTRON MICROSCOPY (2.83 Å)