Target intelligence / Profile preview

Proto-oncogene DBL (MCF2)

Target
MCF2
Molecular classification
Enzyme (specifically: Guanine nucleotide exchange factor, GEF), Rho guanine nucleotide exchange factor (RhoGEF family)
01

Overview

Proto-oncogene DBL (MCF2) encodes a guanine nucleotide exchange factor (GEF) for the Rho family of small GTPases, primarily RhoA, Rac1, and Cdc42[1][2][3][8][9]. DBL functions by catalyzing the exchange of GDP for GTP, thereby activating downstream signaling pathways that regulate cytoskeleton dynamics, cell migration, cell adhesion, neurite extension, and synaptic development[2][8][9]. Alternative splicing generates multiple isoforms with distinct substrate specificities and tissue distributions[2][9]. Aberrant expression or mutation of MCF2 is associated with oncogenic transformation and progression in cancers (notably diffuse B-cell lymphoma), as well as roles in neurodevelopmental disorders and drug resistance[1][2][3][9][10]. MCF2 is part of the RhoGEF family and its activity is context-dependent, affecting developmental signaling and pathological processes.

Other names
DBLARHGEF21MCF2-transforming proteinDBL-transforming proteinMCF.2 cell line derived transforming sequenceProto-oncogene MCF-2Oncogene MCF2 (oncogene DBL)
02

Mechanism of action

Not applicable for direct therapeutic drugs. Drugs modulating Rho GTPase pathways typically act by influencing upstream GEFs like MCF2, interrupting exchange factor activity and preventing GTPase activation[2][3][8][9].

03

Biological functions

Signal transductionActivation of Rho family small GTPases (RhoA, Rac1, Cdc42)Cytoskeletal remodelingCell migrationRegulation of cell adhesionNeurite outgrowth and synaptic function
04

Disease associations

Cancer (B-cell lymphoma, neuroblastoma, testicular cancer, Ewing’s sarcoma, skin granular cell tumor, melanoma)Neurodevelopmental disorders (autism spectrum disorder, schizophrenia)Potential role in drug resistance in melanoma
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Safety considerations

Targeting Rho GEFs like MCF2 could disrupt normal cytoskeletal function, cell migration, and neuronal development, posing risks for off-target effects including altered immune response, cell adhesion, and neurotoxicity
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Interacting drugs

No approved drugs directly targeting MCF2/Proto-oncogene DBL are currently listed. Research compounds targeting Rho GTPase signaling may interact indirectly
07

Biomarkers

Expression of MCF2 may serve as a biomarker for certain cancers (B-cell lymphoma, neuroblastoma, testicular cancer, Ewing’s sarcoma) and possibly for neurodevelopmental disorders

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