What question did this study set out to answer?

Identify and characterize specific peptide inhibitors targeting the RhoA-specific GEFD2 catalytic domain of the Rho-GEF protein Trio.

June 13, 2002FEBS LettersOpen Access

Identification of the first Rho–GEF inhibitor, TRIPα, which targets the RhoA‐specific GEF domain of Trio

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Identify and characterize specific peptide inhibitors targeting the RhoA-specific GEFD2 catalytic domain of the Rho-GEF protein Trio.
Performed an in vivo yeast genetic screen using thioredoxin-coupled peptide aptamers against the Trio GEFD2 domain.
Evaluated aptamer TRIAPalpha and synthetic peptide TRIPalpha using in vitro RhoA exchange assays and cell-based neurite retraction assays in PC12 cells.
TRIAPalpha and its derived peptide TRIPalpha specifically blocked Trio GEFD2 nucleotide exchange activity on RhoA in vitro.
TRIPalpha inhibited TrioGEFD2-mediated RhoA activation in intact cells and reversed the GEFD2-induced neurite retraction phenotype in PC12 cells.

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Implication

Experimental study demonstrates that peptide TRIPalpha inhibits Trio GEFD2 and RhoA activation in cell models, highlighting a new strategy for targeting Rho-GEFs.

Cite This Study

Schmidt et al. (2002) studied this question.

synapsesocial.com/papers/6a94d1d6b1b9682fb47c3d98 https://doi.org/10.1016/s0014-5793(02)02928-9

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Implication

Experimental study demonstrates that peptide TRIPalpha inhibits Trio GEFD2 and RhoA activation in cell models, highlighting a new strategy for targeting Rho-GEFs.

Identification of the first Rho–GEF inhibitor, TRIPα, which targets the RhoA‐specific GEF domain of Trio

Key Points

Discussion

Implication

Cite This Study

Identification of the first Rho–GEF inhibitor, TRIPα, which targets the RhoA‐specific GEF domain of Trio

Key Points

Discussion

Implication

Cite This Study

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