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Related Experiment Videos

A novel Galphaq/11-selective inhibitor.

Jun Takasaki1, Tetsu Saito, Masatoshi Taniguchi

  • 1Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd., 21 Miyukigaoka, Tsukuba-shi, Ibaraki 305-8585, Japan. takasaki@yamanouchi.co.jp

The Journal of Biological Chemistry
|September 2, 2004
PubMed
Summary

YM-254890 is a novel G alpha(q/11) inhibitor that blocks GDP-GTP exchange, offering a new tool for studying G alpha(q/11) signaling pathways. This compound has antithrombotic effects by inhibiting ADP-induced platelet aggregation.

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Area of Science:

  • Pharmacology
  • Molecular Biology
  • Biochemistry

Background:

  • YM-254890, derived from Chromobacterium sp., exhibits antithrombotic and thrombolytic properties.
  • It is known to inhibit ADP-induced platelet aggregation by blocking G alpha(q/11)-coupled P2Y1 receptor-mediated calcium mobilization.

Purpose of the Study:

  • To elucidate the precise molecular mechanism of YM-254890's inhibitory action.
  • To characterize YM-254890 as a selective inhibitor of G alpha(q/11) protein activation.

Main Methods:

  • Investigated YM-254890's effect on calcium mobilization mediated by various G protein-coupled receptors.
  • Assessed YM-254890's impact on serum response factor (SRF)-mediated gene transcription induced by constitutively active and GTPase-deficient G alpha(q) mutants.
  • Analyzed the effect of YM-254890 on specific [(35)S]GTPgammaS binding to G alpha(q/11) stimulated by M1 muscarinic acetylcholine receptor and P2Y1.

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Main Results:

  • YM-254890 selectively inhibited G alpha(q/11)-coupled receptor signaling, sparing G alpha(i)- and G alpha(15)-coupled receptors.
  • The inhibitor blocked SRF-mediated gene transcription induced by a constitutively active G alpha(q) mutant (Galpha(q)R183C) but had a modest effect on a GTPase-deficient mutant (Galpha(q)Q209L).
  • YM-254890 inhibited specific [(35)S]GTPgammaS binding to G alpha(q/11), indicating it blocks the GDP-GTP exchange step in G protein activation.

Conclusions:

  • YM-254890 acts as a selective inhibitor of G alpha(q/11) protein activation by blocking the guanine nucleotide exchange process.
  • This compound is a valuable pharmacological tool for dissecting G alpha(q/11) signaling pathways and related biological functions.