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

AKR1B1 (P15121) - Overview - Molecular Target Synopsis

Protein


AKR1B1, Aldose reductase
Enzyme Classification 1.1.1.21
UniProt P15121

Also Known as ALDR_HUMAN, AKR1B1, ALDR1

Catalyzes the NADPH-dependent reduction of a wide variety of carbonyl-containing compounds to their corresponding alcohols with a broad range of catalytic efficiencies. Monomer.

6F8O
AKR1B1 AT 3.45 MGY RADIATION DOSE.
RCSB/PDB
Inspect Structure
See all 3D Structures for AKR1B1

Isoforms / Transcripts (Protein Coding)


Drugs


AKR1B1 is targeted by Approved Drug Tolrestat. (see details)
Tolrestat

Sub-cellular localization


Gene Copy Number Variation


In COSMIC - Cell Lines Project AKR1B1 has gain in 5 cell-lines, loss in 1 cell-lines and no signal in 999 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: TK_10, A498, RXF_393

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: HCC1395, CAL 54, Hs 675.T

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: A549, SK-N-SH, HeLa-S3

(see details)

3D Structures


For AKR1B1 there are:
144 structures (149 chains) solved
143 are solved in complex with at least one small molecule ligand
6 are solved with an approved drug

AKR1B1 is solved in complex with the approved drug(s):

NTI/NITAZOXANIDE (3V35_A),
TOL/TOLRESTAT (2FZB_A, 2FZD_A, 2PDL_A),
TLT/TOLMETIN (3S3G_A),
LPA/THIOCTIC ACID (2IQD_A).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


AKR1B1 has been screened with 839 compounds (1152 bioactivities), 390 compounds have bioactivities that show binding affinity of <= 500nM (487 bioactivities). (see details)