Target intelligence / Profile preview

Cat eye syndrome critical region protein 2 (CECR2) (CECR2)

Target
CECR2
Molecular classification
Bromodomain-containing protein, Chromatin remodeler, Epigenetic reader, Transcription factor
01

Overview

Cat eye syndrome critical region protein 2 (CECR2) is a bromodomain-containing protein that serves as an epigenetic reader and a key component of the CECR2-containing remodeling factor (CERF) complex [1.3.2, 1.4.1]. It functions by recognizing acetylated lysine residues on histone tails, particularly H3 and H4, as well as non-histone proteins such as the RelA subunit of NF-kappaB [1.3.4, 1.5.1]. This recognition allows CECR2 to facilitate ATP-dependent chromatin remodeling and regulate the transcription of genes involved in neurulation, DNA damage response, and cell proliferation [1.3.1, 1.3.2]. CECR2 is located in the 22q11 region, which is duplicated in Cat eye syndrome, a developmental disorder characterized by ocular coloboma and other malformations [1.4.3, 1.4.4]. In the context of oncology, CECR2 is frequently overexpressed in various cancers, including breast and colon cancer, where it promotes metastasis and immune evasion [1.1.1, 1.2.4, 1.5.1]. Pharmacological targeting of the CECR2 bromodomain with small-molecule inhibitors like NVS-CECR2-1 and GNE-886 has shown promise in displacing the protein from chromatin, thereby inducing apoptosis in cancer cells and inhibiting pro-metastatic signaling pathways [1.1.1, 1.4.1].

Other names
Cat eye syndrome chromosome region candidate 2CECR2-containing remodeling factor subunitCERF subunit
02

Mechanism of action

Bromodomain inhibition

03

Biological functions

Chromatin remodelingGene expression regulationDNA damage responseNeurulationNF-kappaB signaling
04

Disease associations

CancerCat eye syndromeNeural tube defect
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Safety considerations

Developmental toxicityOff-target effects
06

Interacting drugs

NVS-CECR2-1

4 more in the full profile.

07

Biomarkers

CECR2 expressiongamma-H2AX fociNF-kappaB target genes

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