aldo-keto reductase family 1 member B

Target id: 2768

Nomenclature: aldo-keto reductase family 1 member B

Family: 1.-.-.- Oxidoreductases

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for aldo-keto reductase family 1 member B in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 316 7q35 AKR1B1 aldo-keto reductase family 1 member B
Mouse - 316 6 B1 Akr1b3 aldo-keto reductase family 1, member B3 (aldose reductase)
Rat - 316 4q22 Akr1b1 aldo-keto reductase family 1 member B
Previous and Unofficial Names
ALDR1 | AR | aldo-keto reductase family 1, member B1 (aldose reductase | aldo-keto reductase family 1, member B1 (aldose reductase) | aldo-keto reductase family 1
Database Links
BRENDA
CATH/Gene3D
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Human aldose reductase (AKLBR1B1) complexed with tolrestat
PDB Id:  2FZD
Ligand:  tolrestat
Resolution:  1.8Å
Species:  Human
References:  4
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of human AR complexed with NADP+ and AK198.
PDB Id:  4QXI
Ligand:  AK198
Resolution:  0.87Å
Species:  Human
References:  1
Enzyme Reaction
EC Number: 1.1.1.21

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
AK198 Hs Inhibition 8.9 pIC50 1
pIC50 8.9 (IC50 1.3x10-9 M) [1]
lidorestat Hs Inhibition 8.3 pIC50 5
pIC50 8.3 (IC50 5x10-9 M) [5]
Description: In vitro inhibition of recombinant human aldose reductase expressed in E coli.
tolrestat Hs Inhibition 7.3 pIC50 3
pIC50 7.3 (IC50 4.7x10-8 M) [3]
sorbinil Hs Inhibition 5.3 pIC50 2
pIC50 5.3 (IC50 5.4x10-6 M) [2]
zenarestat Hs Inhibition 5.0 pIC50 5
pIC50 5.0 (IC50 9.9x10-6 M) [5]
Description: In vitro inhibition of recombinant human aldehyde reductase
zopolrestat Hs Inhibition 4.4 pIC50 5
pIC50 4.4 (IC50 3.86x10-5 M) [5]
Description: In vitro inhibition of recombinant human aldehyde reductase

References

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1. Fanfrlík J, Ruiz FX, Kadlčíková A, Řezáč J, Cousido-Siah A, Mitschler A, Haldar S, Lepšík M, Kolář MH, Majer P et al.. (2015) The Effect of Halogen-to-Hydrogen Bond Substitution on Human Aldose Reductase Inhibition. ACS Chem. Biol.10 (7): 1637-42. [PMID:25919404]

2. Oka M, Matsumoto Y, Sugiyama S, Tsuruta N, Matsushima M. (2000) A potent aldose reductase inhibitor, (2S,4S)-6-fluoro-2', 5'-dioxospiro[chroman-4,4'-imidazolidine]-2-carboxamide (Fidarestat): its absolute configuration and interactions with the aldose reductase by X-ray crystallography. J. Med. Chem.43 (12): 2479-83. [PMID:10882376]

3. Singh SB, Malamas MS, Hohman TC, Nilakantan R, Carper DA, Kitchen D. (2000) Molecular modeling of the aldose reductase-inhibitor complex based on the X-ray crystal structure and studies with single-site-directed mutants. J. Med. Chem.43 (6): 1062-70. [PMID:10737739]

4. Steuber H, Zentgraf M, Gerlach C, Sotriffer CA, Heine A, Klebe G. (2006) Expect the unexpected or caveat for drug designers: multiple structure determinations using aldose reductase crystals treated under varying soaking and co-crystallisation conditions. J. Mol. Biol.363 (1): 174-87. [PMID:16952371]

5. Van Zandt MC, Jones ML, Gunn DE, Geraci LS, Jones JH, Sawicki DR, Sredy J, Jacot JL, Dicioccio AT, Petrova T et al.. (2005) Discovery of 3-[(4,5,7-trifluorobenzothiazol-2-yl)methyl]indole-N-acetic acid (lidorestat) and congeners as highly potent and selective inhibitors of aldose reductase for treatment of chronic diabetic complications. J. Med. Chem.48 (9): 3141-52. [PMID:15857120]

How to cite this page

1.-.-.- Oxidoreductases: aldo-keto reductase family 1 member B. Last modified on 13/08/2015. Accessed on 23/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2768.