Target intelligence / Profile preview

NIMA-related kinase 2 (NEK2) (NEK2)

Target
NEK2
Molecular classification
Enzyme, Serine/threonine-protein kinase
01

Overview

NIMA-related kinase 2 (NEK2) is a serine/threonine-protein kinase that plays a pivotal role in the regulation of mitosis, particularly in centrosome separation and spindle assembly (UniProt P51955). It is a member of the NIMA (Never In Mitosis A) family of kinases and is essential for the G2/M transition in the cell cycle (PubMed: 24104459). NEK2 is frequently overexpressed in a wide variety of human cancers, including multiple myeloma, breast, and lung cancers, where its high expression correlates with poor prognosis, chromosomal instability, and resistance to chemotherapy (PubMed: 30034545). Therapeutic strategies targeting NEK2 include the development of small-molecule inhibitors like MMB-1 and JH-AI-05, as well as RNA-based therapies such as siRNA and antisense oligonucleotides designed to degrade NEK2 mRNA (PubMed: 26503464). By inhibiting NEK2 or reducing its mRNA levels, researchers aim to trigger mitotic arrest and apoptosis in malignant cells, making it a promising target for precision oncology (PubMed: 21135154).

Other names
HSPK2NLK1NimA-related protein kinase 2Never in mitosis A-related kinase 2
02

Mechanism of action

Small-molecule inhibition of the kinase catalytic domain or RNA interference (siRNA/ASO) to degrade mRNA and prevent protein translation.

03

Biological functions

Cell cycleMitosisCentrosome separationChromosome segregationSignal transduction
04

Disease associations

CancerMultiple myelomaBreast cancerLung cancerColorectal cancerHepatocellular carcinomaPancreatic cancer
05

Safety considerations

Potential for systemic toxicity in normal proliferating tissues such as bone marrowRisk of inducing chromosomal instability if inhibition is incompleteOff-target effects associated with oligonucleotide-based therapiesPotential impact on normal gametogenesis
06

Interacting drugs

MMB-1

5 more in the full profile.

07

Biomarkers

NEK2 mRNA expression levelsNEK2 protein overexpressionCentrosome amplificationChromosomal instability (CIN) index

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