Target intelligence / Profile preview

Ras GTPase-activating-like protein IQGAP1 (IQGAP1)

Target
IQGAP1
Molecular classification
Scaffold protein, Signal transduction molecule, Cytoskeleton-associated protein, RasGAP-like protein (lacks true GTPase-activating function)
01

Overview

IQGAP1 is a multifunctional molecular scaffold found throughout human tissues that interacts directly with actin, microtubules, Rho family GTPases (like CDC42 and Rac1), β-catenin, E-cadherin, and components of the MAPK signaling pathway. Unlike classical GTPase-activating proteins, IQGAP1 does not stimulate GTP hydrolysis on Ras GTPases but instead stabilizes their active GTP-bound forms. By orchestrating assembly and localization of a wide variety of signaling complexes, IQGAP1 couples extracellular signals (from growth factors and chemokines) to cytoskeletal rearrangements, gene expression, cell adhesion, and migration. Its crucial role in signal integration makes it a central regulator in cancer progression, cell morphogenesis, wound repair, and potentially immune responses. IQGAP1 is considered a “node” in multiple signaling networks and its dysregulation or overexpression is implicated in aggressive tumor growth and metastasis.

Other names
IQGAP1KIAA0051p195SAR1HUMORFA01RasGAP-like with IQ motifsRas GTPase-activating-like protein IQGAP1
02

Mechanism of action

For hypothetical drugs: Modulation of scaffold function, inhibition of protein-protein interactions (disrupting IQGAP1 interactions with actin, small GTPases, β-catenin, MAPK proteins), blocking downstream signaling cascades, or altering cytoskeletal organization

03

Biological functions

Actin cytoskeleton organizationCell cycle regulationCell adhesionCell migration and invasionTranscriptional regulation (notably via Wnt/β-catenin pathway)Integration of receptor signals (including receptor tyrosine kinases, chemokine receptors, GPCRs)
04

Disease associations

Cancer (facilitates tumor progression, metastasis, cell invasion, and altered transcriptional programs)Inflammation (modulates immune cell migration via chemokine receptors)Other (potentially involved in developmental and morphogenetic disorders)
05

Safety considerations

Potential off-target effects due to IQGAP1's involvement in many essential cellular processes (proliferation, adhesion, migration).Therapeutic challenges include risk of disruption to normal tissue architecture, impaired wound healing, or immunological dysfunction if IQGAP1 is broadly inhibited
06

Biomarkers

Overexpression in tumor tissues (as a biomarker for certain cancers, especially colorectal, gastric, and breast cancer)Changes in IQGAP1 localization or interaction with β-catenin and E-cadherin as indicators of invasive or migratory cellular programs

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