Target intelligence / Profile preview

Rho guanine nucleotide exchange factor TIAM1 (TIAM1)

Target
TIAM1
Molecular classification
Enzyme, Guanine nucleotide exchange factor (GEF), Signaling molecule, Cytoskeletal effector, Other (Rho GTPase regulator)
01

Overview

Rho guanine nucleotide exchange factor TIAM1 (TIAM1) is an enzyme that activates Rho GTPases, primarily RAC1, by facilitating the exchange of GDP for GTP, thereby linking extracellular signals to cytoskeletal dynamics[1][3][5]. TIAM1 is central to processes including cell adhesion, migration, invasion, and polarity in both normal and malignant cells[1][3]. It is highly expressed in many tumor types and has a validated role in promoting cancer cell invasion and metastasis. In the nervous system, TIAM1 regulates synaptic structure and function, particularly contributing to the maturation of glutamatergic synapses in the hippocampus[2]. Structurally, TIAM1 contains several key domains, including DH (DBL-homology), PH (pleckstrin homology), Ras-binding (RBD), and PDZ domains, supporting its role as a scaffold in intracellular signaling and cytoskeletal reorganization[1][5]. There are no approved drugs directly targeting TIAM1, but its function renders it an attractive target for diseases involving abnormal cell motility, invasion, or synaptic regulation[1][5].

Other names
TIAM Rac1 associated GEF 1T-lymphoma invasion and metastasis-inducing protein 1TIAM-1NEDLDST cell lymphoma invasion and metastasis 1human T-lymphoma invasion and metastasis inducing TIAM1 protein
02

Mechanism of action

Guanine nucleotide exchange factor activity for Rac1 and other Rho-like GTPases (facilitates GDP-GTP exchange to activate these proteins)[1][3][4][5].

03

Biological functions

Signal transductionCell migrationCell adhesionCytoskeletal organizationCell proliferationMetastasisSynapse developmentNeuronal plasticity
04

Disease associations

CancerNeurodevelopmental disorderMental retardation/intellectual disabilityOther (tumor metastasis, neuroplasticity deficits)
05

Safety considerations

Off-target effects could impact cytoskeletal functionneuronal developmentor promote unintended changes in cell adhesion/migrationbroad role in cellular physiology creates potential safety challenges for direct therapeutic modulation[5]

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