Target intelligence / Profile preview

Rhomboid-like protein 1 (RHBDL1)

Target
RHBDL1
Molecular classification
Enzyme, Intramembrane serine protease, Peptidase S54 family
01

Overview

Rhomboid-like protein 1 is a member of the rhomboid family of intramembrane serine proteases, which are responsible for regulated proteolysis of membrane proteins within the lipid bilayer. RHBDL1 possesses a characteristic topology with multiple transmembrane domains forming a protease ring, allowing it to cleave substrates such as growth factor precursors at specific sites. It is most closely related to secretase-type rhomboid proteases, participating in the release of functional peptides from their membrane anchors and modulating cell signaling cascades, including those relevant in cancer pathogenesis (e.g., trafficking of pro-transforming growth factor alpha). While RHBDL1 is considered a valid molecular target for research in oncology and cell biology, no approved drugs or clinical interventions specifically target this protein to date. Early structural studies have revealed its architectural details, including the arrangement of catalytic residues and transmembrane segments.

Other names
Rhomboid-related protein 1RHBDL1RHBDLRRPRhomboid-like protein 1rhomboid, drosophila, homolog ofveinlet-like 1
02

Mechanism of action

Inhibition of RHBDL1 would block regulated cleavage of membrane proteins, potentially altering growth factor or cytokine signaling. Targeting RHBDL1 may modulate cleavage-dependent signaling pathways relevant in cancer.

03

Biological functions

Proteolytic cleavage of membrane-bound substratesRegulated intramembrane proteolysisRelease of polypeptides from membrane anchorsRegulation of cell signalingPossible role in growth factor signaling
04

Disease associations

Cancer (particularly breast cancer; modulates membrane trafficking related to EGFR/transforming growth factor)Other potential roles under investigation
05

Safety considerations

Therapeutic targeting of intramembrane proteases may impact broad cellular signaling pathways, risking off-target effects and disruption of normal cell homeostasisLack of selective inhibitors may pose challenges for safety and specificity
06

Interacting drugs

No clinically approved drugs directly targeting RHBDL1 as of current literature

1 more in the full profile.

07

Biomarkers

No validated biomarkers for patient selection or efficacy monitoring for RHBDL1 therapies currently available

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