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Rhotekin is a scaffold protein encoded by the RTKN gene on human chromosome 2. It acts as an effector for GTP-bound Rho proteins, inhibiting their GTPase activity and thereby modulating Rho-mediated signaling pathways. Rhotekin contains several functional domains, including a Rho-binding domain, pleckstrin homology domain, proline-rich regions, and a PDZ-binding motif, enabling it to serve as a hub for protein-protein interactions. Rhotekin is involved in the regulation of the actin cytoskeleton, cell morphology, cell motility, transcription, cytokinesis, and apoptosis resistance. It is highly expressed in the brain and various cancers, where its upregulation correlates with tumor progression and resistance to apoptosis. Dysregulation of Rhotekin and its signaling axis is implicated in the pathogenesis of multiple cancer types, making it a candidate therapeutic target. However, its exact physiological functions, especially outside cancer, remain incompletely understood[1][2][3][4].
Inhibition of Rhotekin-related signaling pathways (such as NF-kappa-B activation) shown to increase apoptosis or decrease proliferation in cancer cell models[4]. Targeted by certain microRNAs (e.g., miRNA-152, let-7a), lowering Rhotekin expression to suppress tumor growth[4].
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