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

INSRR (P14616) - Overview - Molecular Target Synopsis

Protein


INSRR, Insulin receptor-related protein
Enzyme Classification 2.7.10.1
UniProt P14616

Also Known as INSRR_HUMAN, INSRR, IRR

Receptor with tyrosine-protein kinase activity. Functions as a pH sensing receptor which is activated by increased extracellular pH. Activates an intracellular signaling pathway that involves IRS1 and AKT1/PKB. Probable tetramer of 2 alpha and 2 beta chains linked by disulfide bonds. The alpha chains contribute to the formation of the ligand-binding domain, while the beta chains carry the kinase domain.

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
1297ENSG00000027644ENST00000368195ENSP00000357178P14616-1

Sub-cellular localization


UniProt: INSRR is active in the following subcellular-locations: membrane.
GO terms: INSRR is active in the following subcellular-locations: axon, insulin receptor complex, integral component of plasma membrane, receptor complex.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project INSRR has gain in 4 cell-lines, loss in 0 cell-lines and no signal in 1001 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SK_MEL_5, HL_60, LOXIMVI

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: CPC-N, SK-N-SH, SCLC-22H

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: NHLF, HSMM, HMEC

(see details)

RNA Interference


INSRR was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: DU4475, NY. (see details)

3D Structures


At greater than 75% identity similarity to INSRR there are:
20 structures (55 chains) solved
18 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


INSRR has been screened with 721 compounds (1320 bioactivities), 8 compounds have bioactivities that show binding affinity of <= 500nM (13 bioactivities). (see details)