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

REN (P00797) - Overview - Molecular Target Synopsis

Protein


REN, Renin
Enzyme Classification 3.4.23.15
UniProt P00797

Also Known as RENI_HUMAN, REN

Renin is a highly specific endopeptidase, whose only known function is to generate angiotensin I from angiotensinogen in the plasma, initiating a cascade of reactions that produce an elevation of blood pressure and increased sodium retention by the kidney. Interacts with ATP6AP2.

6I3F
CRYSTAL STRUCTURE OF THE COMPLEX OF HUMAN ANGIOTENSINOGEN AND RENIN AT 2.55 ANGSTROM
RCSB/PDB
Inspect Structure
See all 3D Structures for REN

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
406ENSG00000143839ENST00000272190ENSP00000272190P00797-1, P60016-1
403ENSG00000143839ENST00000367195ENSP00000356163P00797-2

Drugs


REN is targeted by Approved Drug Aliskiren. (see details)
Aliskiren

Sub-cellular localization


UniProt: REN is active in the following subcellular-locations: membrane, secreted.
GO terms: REN is active in the following subcellular-locations: apical part of cell, cytoplasm, extracellular region, extracellular space, plasma membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project REN 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: HT29, LOXIMVI, SK_MEL_5

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: SW 780, CL-40, Calu-6

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, NHLF, HSMM

(see details)

RNA Interference


REN was reported in the following RNAI studies:

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

3D Structures


For REN there are:
88 structures (181 chains) solved
86 are solved in complex with at least one small molecule ligand
1 are solved with an approved drug

REN is solved in complex with the approved drug(s):

C41/ALISKIREN (2V0Z_C, 2V0Z_O).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


REN has been screened with 3175 compounds (4961 bioactivities), 2356 compounds have bioactivities that show binding affinity of <= 500nM (3598 bioactivities). (see details)