Target intelligence / Profile preview

Ral-interacting protein 1 (RLIP76) (RLIP76)

Target
RLIP76
Molecular classification
GTPase-activating protein, Transporter, Signaling scaffold protein
01

Overview

Ral-interacting protein 1 (RLIP76), also known as RALBP1, is a multifunctional modular protein that serves as a critical effector for Ral GTPases and plays a significant role in clathrin-dependent endocytosis (UniProt: Q15311). Beyond its signaling functions, RLIP76 acts as a non-ATP-binding cassette (non-ABC) transporter, facilitating the efflux of glutathione-conjugates and various chemotherapeutic agents from cells (PubMed: 17452456). In the context of oncology, RLIP76 is frequently overexpressed in multiple cancer types, where it contributes to multidrug resistance, anti-apoptosis, and tumor growth (PubMed: 25613355). Therapeutic strategies targeting RLIP76, including antisense oligonucleotides and monoclonal antibodies, aim to inhibit its transport activity and signaling scaffolds to sensitize tumors to existing treatments (PubMed: 12855586). Its involvement in metabolic pathways also suggests potential roles in treating diabetes and metabolic syndrome. The protein's ability to regulate oxidative stress by transporting lipid peroxidation products makes it a unique target for mitigating cellular damage. However, its broad expression in normal tissues necessitates careful evaluation of safety and specificity in drug development.

Other names
RalA-binding protein 1RALBP1RLIP176 kDa Ral-interacting proteinDinitrophenyl S-glutathione ATPase
02

Mechanism of action

Inhibition of the transport function of RLIP76 or depletion of the protein to sensitize cancer cells to chemotherapy and induce apoptosis.

03

Biological functions

EndocytosisSignal transductionDrug transportStress responseCell proliferationApoptosis regulation
04

Disease associations

CancerMetabolic syndromeDiabetesOxidative stress-related disorders
05

Safety considerations

Potential interference with normal endocytosisSystemic toxicity due to role in xenobiotic detoxificationOff-target effects in metabolic tissues
06

Interacting drugs

RLIP76 antisense oligonucleotides

2 more in the full profile.

07

Biomarkers

RLIP76 protein expressionRALBP1 mRNA levels

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