Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

NCOR2 (Q9Y618) - Overview - Molecular Target Synopsis

Protein


NCOR2, Nuclear receptor corepressor 2
UniProt Q9Y618

Also Known as NCOR2_HUMAN, NCOR2, CTG26

Transcriptional corepressor (PubMed:20812024). Mediates the transcriptional repression activity of some nuclear receptors by promoting chromatin condensation, thus preventing access of the basal transcription. Isoform 1 and isoform 4 have different affinities for different nuclear receptors. Involved in the regulation BCL6-dependent of the germinal center (GC) reactions, mainly through the control of the GC B-cells proliferation and survival. Recruited by ZBTB7A to the androgen response elements/ARE on target genes, negatively regulates androgen receptor signaling and androgen-induced cell proliferation (PubMed:20812024). Forms a large corepressor complex that contains SIN3A/B and histone deacetylases HDAC1 and HDAC2. This complex associates with the thyroid (TR) and the retinoid acid receptors (RAR) in the absence of ligand, and may stabilize their interaction with TFIIB. Interacts directly with RARA in the absence of ligand; the interaction represses RARA activity. Interacts (isoform SMRT) with HDAC10. Interacts with MINT. Component of the N-Cor repressor complex, at least composed of NCOR1, NCOR2, HDAC3, TBL1X, TBL1R, CORO2A and GPS2 (PubMed:10809664, PubMed:10944117, PubMed:11931768, PubMed:19858209, PubMed:21240272). Interacts with CBFA2T3 and ATXN1L. Interacts with RARB; the interaction is weak and does not repress RARB transactivational activity. Interacts with HDAC7 and C1D. Interacts with NR4A2; this interaction increases in the absence of PITX3. Interacts with BCL6 (via the BTB domain), required for BCL6 transcriptional repressor activity on a subset of target genes. Forms ternary complexes with BCOR and BCL6 on target gene promoters but, on enhancer elements, interacts with BCL6 and HDAC3 to repress proximal gene expression. May interact with DEAF1. Interacts with RXRA. Interacts with MECP2 (By similarity). Interacts with ZBTB7A (PubMed:20812024). Interacts with AR (PubMed:20812024).

6IVX
14 RESIDUE FRAGMENT OF
NUCLEAR RECEPTOR COREPRESSOR 2
IN THE STRUCTURE OF
DISCOVERY OF THE SECOND GENERATION ROR GAMMA INHIBITORS COMPOSED OF AN AZOLE SCAFFOLD.
RCSB/PDB
Inspect Structure
See all 3D Structures for NCOR2

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: NCOR2 is active in the following subcellular-locations: nucleus.
GO terms: NCOR2 is active in the following subcellular-locations: histone deacetylase complex, membrane, nuclear body, nuclear chromatin, nuclear matrix, nucleoplasm, nucleus, transcriptional repressor complex.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project NCOR2 has gain in 1 cell-lines, loss in 1 cell-lines and no signal in 1003 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: A549, LOXIMVI, ACHN

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: G61, SW 982, COLO 699

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: SK-N-SH, A549, IMR-90

(see details)

3D Structures


For NCOR2 there are:
17 structures (36 chains) solved
1 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


NCOR2 has been screened with 111 compounds (152 bioactivities), 80 compounds have bioactivities that show binding affinity of <= 500nM (106 bioactivities). (see details)