YM-254890

YM-254890 is a G protein-coupled receptor antagonist that is derived from the bacterium Chromobacterium violaceum. It is a highly selective inhibitor of the Gq alpha subunit of the G protein, and it has been used in the study of G protein signaling.

Structure and Function

The structure of YM-254890 is unique among G protein antagonists. It is a cyclic depsipeptide, meaning it contains both peptide and ester bonds. The molecule has a complex structure that includes a 22-membered ring and several unusual amino acids.

YM-254890 functions by binding to the Gq alpha subunit of the G protein, preventing it from interacting with G protein-coupled receptors on the cell surface. This inhibits the activation of the G protein and the subsequent intracellular signaling pathways it would normally initiate.

Pharmacological Applications

Because of its specificity for the Gq alpha subunit, YM-254890 has been used in research to study the role of this protein in various cellular processes. It has been particularly useful in studying G protein-coupled receptor signaling, as it allows researchers to selectively inhibit this pathway and observe the resulting effects on the cell.

In addition to its research applications, YM-254890 has potential therapeutic applications. Its ability to inhibit G protein signaling could make it useful in the treatment of diseases that are caused by overactive G protein-coupled receptor signaling, such as certain types of cancer.

See Also

• G protein
• G protein-coupled receptor
• Chromobacterium violaceum
• Gq alpha subunit