SET2 is a drug which acts as a selective antagonist for the

TRPV2 TRPV is a family of transient receptor potential cation channels (TRP channels) in animals. All TRPVs are highly calcium selective. TRP channels are a large group of ion channels consisting of six protein families, located mostly on the plasma ...

receptor. It is moderately potent with an IC₅₀ of 460nM, but is highly selective for TRPV2 over the other subtypes of

TRPV TRPV is a family of transient receptor potential cation channels (TRP channels) in animals. All TRPVs are highly calcium selective. TRP channels are a large group of ion channels consisting of six protein families, located mostly on the plasm ...

, and is the first such compound to be developed. A role has been suggested for TRPV2 in tumor

metastasis Metastasis is a pathogenic agent's spread from an initial or primary site to a different or secondary site within the host's body; the term is typically used when referring to metastasis by a cancerous tumor. The newly pathological sites, then ...

, making this a target of interest in the treatment of cancer.

References

Thioethers Pyrimidines {{pharm-stub

See also

References