Target intelligence / Profile preview

E3 Ubiquitin-Protein Ligase (E3)

Target
E3
Molecular classification
Enzyme, Ubiquitin ligase
01

Overview

E3 ubiquitin-protein ligases are a diverse family of enzymes responsible for substrate specificity in the ubiquitination process. They facilitate the attachment of ubiquitin to target proteins, regulating protein degradation, cellular localization, protein interactions, and stability. Dysregulation of E3 ligases is implicated in various diseases, making them potential drug targets.

02

Mechanism of action

Catalyzes the transfer of ubiquitin from an E2 ubiquitin-conjugating enzyme to substrate proteins, marking them for degradation or altering their function/location. Different E3 ligases (RING, HECT, RBR, Cullin-RING) employ distinct mechanisms to achieve this.

03

Biological functions

Protein ubiquitinationProtein degradationCell cycle regulationDNA repairSignal transductionImmune responseStress responseProtein homeostasis
04

Disease associations

CancerNeurodegenerative disease
05

Safety considerations

Off-target effectsUnintended degradation of proteinsPotential for drug resistance
06

Interacting drugs

MDM2 inhibitors

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