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

AKR1C2 (P52895) - Overview - Molecular Target Synopsis

Protein


AKR1C2, Aldo-keto reductase family 1 member C2
Enzyme Classification 1.-.-.-
UniProt P52895

Also Known as AK1C2_HUMAN, AKR1C2, DDH2

Works in concert with the 5-alpha/5-beta-steroid reductases to convert steroid hormones into the 3-alpha/5-alpha and 3-alpha/5-beta-tetrahydrosteroids. Catalyzes the inactivation of the most potent androgen 5-alpha-dihydrotestosterone (5-alpha-DHT) to 5-alpha-androstane-3-alpha,17-beta-diol (3-alpha-diol). Has a high bile-binding ability.

4XO7
CRYSTAL STRUCTURE OF HUMAN 3-ALPHA HYDROXYSTEROID DEHYDROGENASE TYPE 3 IN COMPLEX WITH NADP+, 5ALPHA-ANDROSTAN-3,17-DIONE AND (3BETA, 5ALPHA)-3-HYDROXYANDROSTAN-17-ONE
RCSB/PDB
Inspect Structure
See all 3D Structures for AKR1C2

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: AKR1C2 is active in the following subcellular-locations: cytoplasm.
GO terms: AKR1C2 is active in the following subcellular-locations: cytosol.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project AKR1C2 has gain in 3 cell-lines, loss in 6 cell-lines and no signal in 996 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: NCI_H460, A549, HCC_2998

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: NCI-H1437, NCI-H2023, NCI-H2110

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, HSMM

(see details)

3D Structures


For AKR1C2 there are:
16 structures (32 chains) solved
16 are solved in complex with at least one small molecule ligand
8 are solved with an approved drug

AKR1C2 is solved in complex with the approved drug(s):

ZOM/ZOMEPIRAC (4JQ3_A, 4JQ3_B),
STR/PROGESTERONE (4L1W_A, 4L1W_B, 4L1X_A, 4L1X_B),
IMN/INDOMETHACIN (4JQ4_A, 4JQ4_B),
TES/TESTOSTERONE (1J96_A, 1J96_B),
ID8/MEFENAMIC ACID (4JQA_A, 4JQA_B),
IBP/DEXIBUPROFEN (4JTR_A),
NPS/NAPROXEN (4JQ1_A, 4JQ1_B).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


AKR1C2 has been screened with 409 compounds (494 bioactivities), 40 compounds have bioactivities that show binding affinity of <= 500nM (47 bioactivities). (see details)