Target intelligence / Profile preview

Centromere protein E (CENP-E)

Target
CENP-E
Molecular classification
Kinesin motor protein, Kinesin-7 family, Microtubule motor, Enzyme
01

Overview

Centromere protein E (CENP-E) is a kinesin motor protein belonging to the Kinesin-7 family. It localizes to outer kinetochores during mitosis and is essential for proper chromosome alignment (congression) and attachment to spindle microtubules. CENP-E functions as a homodimer and has an N-terminal ATPase motor domain, a long coiled-coil stalk, and a C-terminal tail. Its motor activity is critical for tethering chromosomes to the spindle and facilitating their movement toward the metaphase plate. Dysregulation or inhibition of CENP-E disrupts chromosome alignment, can induce mitotic arrest, and contributes to chromosomal instability—making this protein a validated anticancer drug target.

Other names
Centromere-associated protein EKIF10Kinesin-7 family member
02

Mechanism of action

Inhibition of CENP-E's ATPase activity blocks its motor function, which prevents proper chromosome congression and leads to mitotic arrest. This disruption of chromosome alignment and segregation is the primary mechanism.

03

Biological functions

Chromosome alignmentChromosome congressionSpindle microtubule interactionKinetochore-microtubule attachmentMitotic progressionCell cycle regulation
04

Disease associations

Cancer
05

Safety considerations

Mitotic arrestAneuploidy and chromosome missegregationPotential for myelosuppression and off-target effects
06

Interacting drugs

GSK923295
07

Biomarkers

Mitotic indexChromosome alignment defectsCENP-E protein levels

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