Sci Rep
 2017
DOI: 10.1038/s41598-017-08829-7
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The Gαi-GIV binding interface is a druggable protein-protein interaction

Vincent DiGiacomo1,
Alain Ibáñez de Opakua
2
,
Maria P. Papakonstantinou3
et al.

Abstract: Heterotrimeric G proteins are usually activated by the guanine-nucleotide exchange factor (GEF) activity of GPCRs. However, some non-receptor proteins are also GEFs. GIV (a.k.a Girdin) was the first non-receptor protein for which the GEF activity was ascribed to a well-defined protein sequence that directly binds Gαi. GIV expression promotes metastasis and disruption of its binding to Gαi blunts the pro-metastatic behavior of cancer cells. Although this suggests that inhibition of the Gαi-GIV interaction is a … Show more

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Cited by 27 publications

(30 citation statements)
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“…Concentration-dependent binding curves revealed that the affinity of Gαi3 for the dark conformation of LOV2GIVe is orders of magnitude weaker than for the lit conformation ( Figure 2A ), which had an equilibrium dissociation constant (K D ) similar to that previously reported for the GIV-Gαi3 interaction ( DiGiacomo et al, 2017 ). We also found that LOV2GIVe retains the same G-protein specificity as GIV.…”
Section: Resultssupporting
confidence: 77%
Exaggerated anticipatory anxiety is common in social anxiety disorder (SAD). Neuroimaging studies have revealed altered neural activity in response to social stimuli in SAD, but fewer studies have examined neural activity during anticipation of feared social stimuli in SAD. The current study examined the time course and magnitude of activity in threat processing brain regions during speech anticipation in socially anxious individuals and healthy controls (HC). Method Participants (SAD n = 58; HC n = 16) underwent functional magnetic resonance imaging (fMRI) during which they completed a 90s control anticipation task and 90s speech anticipation task.
show abstract
“…Concentration-dependent binding curves revealed that the affinity of Gαi3 for the dark conformation of LOV2GIVe is orders of magnitude weaker than for the lit conformation ( Figure 2A ), which had an equilibrium dissociation constant (K D ) similar to that previously reported for the GIV-Gαi3 interaction ( DiGiacomo et al, 2017 ). We also found that LOV2GIVe retains the same G-protein specificity as GIV.…”
Section: Resultssupporting
confidence: 77%
Exaggerated anticipatory anxiety is common in social anxiety disorder (SAD). Neuroimaging studies have revealed altered neural activity in response to social stimuli in SAD, but fewer studies have examined neural activity during anticipation of feared social stimuli in SAD. The current study examined the time course and magnitude of activity in threat processing brain regions during speech anticipation in socially anxious individuals and healthy controls (HC). Method Participants (SAD n = 58; HC n = 16) underwent functional magnetic resonance imaging (fMRI) during which they completed a 90s control anticipation task and 90s speech anticipation task.
show abstract
“…Concentration-dependent binding curves revealed that the affinity of Gαi3 for the dark conformation of LOV2GIVe is orders of magnitude weaker than for the lit conformation ( Fig. 2A), which had an equilibrium dissociation constant (Kd) similar to that previously reported for the GIV-Gαi3 interaction (DiGiacomo et al, 2017). We also found that LOV2GIVe retains the same G-protein specificity as GIV.…”
Section: Lov2give Binds and Activates G-proteins Efficiently In Vitrosupporting
confidence: 82%
Exaggerated anticipatory anxiety is common in social anxiety disorder (SAD). Neuroimaging studies have revealed altered neural activity in response to social stimuli in SAD, but fewer studies have examined neural activity during anticipation of feared social stimuli in SAD. The current study examined the time course and magnitude of activity in threat processing brain regions during speech anticipation in socially anxious individuals and healthy controls (HC). Method Participants (SAD n = 58; HC n = 16) underwent functional magnetic resonance imaging (fMRI) during which they completed a 90s control anticipation task and 90s speech anticipation task.
show abstract
“…These compounds were frequently associated with modulator properties. Overall, the analysis of this interface has shown that especially the Switch II/α3 region is well exposed and druggable, which has already been described by DiGiacomo et al [188] . in the context of small molecules, but can further be extended to the peptide level.…”
Section: Discussionsupporting
confidence: 61%
Exaggerated anticipatory anxiety is common in social anxiety disorder (SAD). Neuroimaging studies have revealed altered neural activity in response to social stimuli in SAD, but fewer studies have examined neural activity during anticipation of feared social stimuli in SAD. The current study examined the time course and magnitude of activity in threat processing brain regions during speech anticipation in socially anxious individuals and healthy controls (HC). Method Participants (SAD n = 58; HC n = 16) underwent functional magnetic resonance imaging (fMRI) during which they completed a 90s control anticipation task and 90s speech anticipation task.
show abstract
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