Target intelligence / Profile preview

Adhesion regulating molecule 1 (ADRM1) (ADRM1)

Target
ADRM1
Molecular classification
Proteasome subunit, Ubiquitin receptor
01

Overview

Adhesion regulating molecule 1 (ADRM1), also known as Rpn13, is an integral subunit of the 19S regulatory particle of the 26S proteasome [1]. It serves as a crucial ubiquitin receptor that recognizes and binds polyubiquitinated proteins, facilitating their entry into the proteasome for degradation [2]. ADRM1 is frequently overexpressed in various malignancies, including multiple myeloma and ovarian cancer, where it promotes cell survival and proliferation [3]. Because of its pivotal role in the ubiquitin-proteasome system, ADRM1 has emerged as a promising therapeutic target for cancer treatment [4]. Small molecule inhibitors, such as RA190, target the N-terminal pleckstrin homology domain of ADRM1, effectively blocking its ability to bind ubiquitin and triggering apoptosis in cancer cells [2, 5]. This approach provides a distinct mechanism compared to traditional 20S proteasome inhibitors, potentially overcoming resistance in clinical settings [5].

Other names
Rpn13ARM-1GP110Proteasome regulatory particle non-ATPase subunit 13
02

Mechanism of action

Inhibition of the 19S regulatory particle by binding to the Rpn13 subunit, preventing the degradation of polyubiquitinated proteins and inducing proteotoxic stress and apoptosis.

03

Biological functions

Protein degradationUbiquitin bindingCell adhesionProteasome assembly
04

Disease associations

CancerMultiple myelomaOvarian cancerColorectal cancerLiver cancer
05

Safety considerations

Proteotoxicity in healthy cellsOff-target reactivity of electrophilic inhibitorsPotential for peripheral neuropathy
06

Interacting drugs

RA190

2 more in the full profile.

07

Biomarkers

ADRM1 protein expressionADRM1 mRNA levels

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