Target intelligence / Profile preview

Anaphase-promoting complex (APC/C)

Target
APC/C
Molecular classification
Enzyme, E3 ubiquitin ligase, Multi-subunit protein complex
01

Overview

The Anaphase-promoting complex (APC/C) is a multi-subunit E3 ubiquitin ligase that serves as a master regulator of the eukaryotic cell cycle, particularly during the transition from metaphase to anaphase (NIH, 2023; UniProt, 2024). By targeting specific substrates like securin and B-type cyclins for degradation via the 26S proteasome, the APC/C facilitates the separation of sister chromatids and the exit from mitosis (Wikipedia, 2024). In oncogenesis, the complex is often dysregulated, leading to aneuploidy and chromosomal instability, making it a focal point for cancer research (Nature Reviews Molecular Cell Biology, 2020). Therapeutic strategies involve small-molecule inhibitors such as ProTAME and Apcin, which aim to induce mitotic arrest and subsequent cell death in rapidly dividing cancer cells (PubMed, 2021). However, the essential role of APC/C in normal cell division presents a narrow therapeutic window and significant safety concerns regarding systemic toxicity and potential genomic damage (Journal of Biological Chemistry, 2022).

Other names
CyclosomeAPC/CAnaphase-promoting complex/cyclosomeE3 ubiquitin-protein ligase APC complex
02

Mechanism of action

E3 ubiquitin ligase inhibition; prevents the degradation of cell cycle regulators (Securin, Cyclin B1), leading to mitotic arrest and subsequent apoptosis.

03

Biological functions

Cell cycle regulationMitosisMetaphase-to-anaphase transitionProteolysisUbiquitinationMeiosis
04

Disease associations

CancerChromosomal instabilityAneuploidyNeurodegenerative disease
05

Safety considerations

Systemic toxicity due to essential role in all dividing cellsInduction of genomic instabilityPotential for aneuploidy in healthy tissuesNarrow therapeutic window
06

Interacting drugs

ProTAME

2 more in the full profile.

07

Biomarkers

CDC20 expressionCDH1 expressionSecurin levelsCyclin B1 levelsBubR1 status

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