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

HSD11B1 (P28845) - Overview - Molecular Target Synopsis

Protein


HSD11B1, Corticosteroid 11-beta-dehydrogenase isozyme 1
Enzyme Classification 1.1.1.146
UniProt P28845

Also Known as DHI1_HUMAN, HSD11B1, HSD11, HSD11L, SDR26C1

Catalyzes reversibly the conversion of cortisol to the inactive metabolite cortisone. Catalyzes reversibly the conversion of 7-ketocholesterol to 7-beta-hydroxycholesterol. In intact cells, the reaction runs only in one direction, from 7-ketocholesterol to 7-beta-hydroxycholesterol. Homodimer.

5QII
CRYSTAL STRUCTURE OF 11BETA-HSD1 DOUBLE MUTANT (L262R, F278E) COMPLEXED WITH 2-(3-(1-(4-CHLOROPHENYL)CYCLOPROPYL) -[1,2, 4]TRIAZOLO[4,3-A]PYRIDIN-8-YL)PROPAN-2-OL
RCSB/PDB
Inspect Structure
See all 3D Structures for HSD11B1

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
292ENSG00000117594ENST00000367027, ENST00000367028, ENST00000261465ENSP00000355994, ENSP00000355995, ENSP00000261465P28845-1

Sub-cellular localization


UniProt: HSD11B1 is active in the following subcellular-locations: endoplasmic reticulum membrane.
GO terms: HSD11B1 is active in the following subcellular-locations: endoplasmic reticulum membrane, integral component of membrane, membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project HSD11B1 has gain in 2 cell-lines, loss in 1 cell-lines and no signal in 1002 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: HOP_62, SF_268, LOXIMVI

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: Panc 03.27, NUGC-3, NCI-H2347

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, HSMM, HMEC

(see details)

3D Structures


For HSD11B1 there are:
40 structures (145 chains) solved
40 are solved in complex with at least one small molecule ligand
1 are solved with an approved drug

HSD11B1 is solved in complex with the approved drug(s):

CBO/CARBENOXOLONE (2BEL_A, 2BEL_B, 2BEL_C, 2BEL_D).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


HSD11B1 has been screened with 3777 compounds (5638 bioactivities), 2518 compounds have bioactivities that show binding affinity of <= 500nM (3660 bioactivities). (see details)