Defining AV2-1 as a novel pharmacological probe to target human and rodent TRPV2
Leipe A, Rocereta JA, Pumroy RA, 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 Mar 30. doi: 10.1111/bph.70413. Epub ahead of print. PMID: 41913383.
Abstract
Background and purpose: 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.