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

HSD17B1 (P14061) - Overview - Molecular Target Synopsis

Protein


HSD17B1, Estradiol 17-beta-dehydrogenase 1
Enzyme Classification 1.1.1.62
UniProt P14061

Also Known as DHB1_HUMAN, HSD17B1, E17KSR, EDH17B1, EDH17B2, EDHB17, SDR28C1

Favors the reduction of estrogens and androgens. Also has 20-alpha-HSD activity. Uses preferentially NADH. Homodimer.

6MNE
CRYSTAL STRUCTURE OF HUMAN 17BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 COMPLEXED WITH ESTRONE AND NADP+
RCSB/PDB
Inspect Structure
See all 3D Structures for HSD17B1

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: HSD17B1 is active in the following subcellular-locations: cytoplasm.
GO terms: HSD17B1 is active in the following subcellular-locations: cytoplasm, cytosol.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project HSD17B1 has gain in 1 cell-lines, loss in 2 cell-lines and no signal in 1001 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: T47D, NCI_H522, MALME_3M

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: BT-20, UACC-812, ChaGo-K-1

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)

3D Structures


For HSD17B1 there are:
27 structures (40 chains) solved
25 are solved in complex with at least one small molecule ligand
10 are solved with an approved drug

HSD17B1 is solved in complex with the approved drug(s):

EST/ESTRADIOL (1A27_A, 1FDS_A, 1FDT_A, 1FDU_A, 1FDU_B, 1FDU_C, 1FDU_D, 1FDW_A, 1IOL_A),
J3Z/ESTRONE (6MNC_B, 6MNE_A, 6MNE_B),
TES/TESTOSTERONE (1JTV_A),
AND/PRASTERONE (3DHE_A).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


HSD17B1 has been screened with 1153 compounds (1961 bioactivities), 280 compounds have bioactivities that show binding affinity of <= 500nM (381 bioactivities). (see details)