Target intelligence / Profile preview

Rhophilin Rho GTPase binding protein 2 (RHPN2)

Target
RHPN2
Molecular classification
Other (Effector protein of small GTPases; Signal transducer/adaptor protein)
01

Overview

Rhophilin Rho GTPase binding protein 2 (RHPN2) is a cytoplasmic effector protein belonging to the rhophilin family that binds both GDP- and GTP-bound RhoA and GTP-bound RhoB[3]. It contains an N-terminal Rho-binding domain, a Bro1-like domain, and a C-terminal PDZ domain[1][2]. RHPN2 plays a key role in actin cytoskeleton organization, regulates stress fiber formation, and is involved in cell migration and invasion, likely acting within Rho GTPase–mediated signaling cascades[2][3]. Overexpression or mutation of RHPN2 is associated with enhanced tumor cell proliferation, migration, and poor prognosis in several types of cancer, particularly lung adenocarcinoma and hepatocellular carcinoma. RHPN2 may upregulate oncogenic pathways (such as c-Myc or Hippo-YAP) and promote mesenchymal transformation; it is under investigation both as a cancer biomarker and as a candidate target for anti-cancer therapy[2][4]. No direct-acting drugs or inhibitors are currently known.

Other names
Rhophilin-276 kDa RhoB effector proteinGTP-Rho-binding protein 2p76RBEP76RBERHOBPrhophilin-2rhophilin-like Rho-GTPase binding protein
02

Mechanism of action

Not applicable / none described for direct drug targeting (acts as a RhoA/RhoB effector and mediator of Rho GTPase signaling)

03

Biological functions

Actin cytoskeleton organizationSignal transductionRegulation of cell migration and invasionMesenchymal transformationRegulation of apoptosis and proliferation
04

Disease associations

Cancer (notably lung adenocarcinoma, hepatocellular carcinoma, malignant glioma, colorectal cancer)Other (Blepharocheilodontic syndrome 1, Hereditary mixed polyposis syndrome)
05

Safety considerations

No specific therapeutic safety concerns described; target is implicated in cell proliferation and migration, thus theoretical safety concerns may include effects on normal tissue regeneration or wound healing if targeted
06

Biomarkers

Overexpression may serve as a biomarker for tumor progression or adverse prognosis in hepatocellular carcinoma, lung adenocarcinoma, and possibly other cancers

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