Details of the Target

General Information of Target

Target ID LDTP00912
Target Name Aldo-keto reductase family 1 member B10 (AKR1B10)
Gene Name AKR1B10
Gene ID 57016
Synonyms
AKR1B11; Aldo-keto reductase family 1 member B10; EC 1.1.1.300; EC 1.1.1.54; ARL-1; Aldose reductase-like; Aldose reductase-related protein; ARP; hARP; Small intestine reductase; SI reductase
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MATFVELSTKAKMPIVGLGTWKSPLGKVKEAVKVAIDAGYRHIDCAYVYQNEHEVGEAIQ
EKIQEKAVKREDLFIVSKLWPTFFERPLVRKAFEKTLKDLKLSYLDVYLIHWPQGFKSGD
DLFPKDDKGNAIGGKATFLDAWEAMEELVDEGLVKALGVSNFSHFQIEKLLNKPGLKYKP
VTNQVECHPYLTQEKLIQYCHSKGITVTAYSPLGSPDRPWAKPEDPSLLEDPKIKEIAAK
HKKTAAQVLIRFHIQRNVIVIPKSVTPARIVENIQVFDFKLSDEEMATILSFNRNWRACN
VLQSSHLEDYPFNAEY
Target Bioclass
Enzyme
Family
Aldo/keto reductase family
Subcellular location
Lysosome
Function
Catalyzes the NADPH-dependent reduction of a wide variety of carbonyl-containing compounds to their corresponding alcohols. Displays strong enzymatic activity toward all-trans-retinal, 9-cis-retinal, and 13-cis-retinal. Plays a critical role in detoxifying dietary and lipid-derived unsaturated carbonyls, such as crotonaldehyde, 4-hydroxynonenal, trans-2-hexenal, trans-2,4-hexadienal and their glutathione-conjugates carbonyls (GS-carbonyls). Displays no reductase activity towards glucose.
Uniprot ID
O60218
Ensemble ID
ENST00000359579.5
HGNC ID
HGNC:382
ChEMBL ID
CHEMBL5983

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 11 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
YN-4
 Probe Info  		100.00  LDD0445  [1]
IPM
 Probe Info  		N.A.  LDD0241  [2]
DBIA
 Probe Info  		C45(1.45)  LDD3354  [3]
BTD
 Probe Info  		C187(2.92)  LDD1700  [4]
IA-alkyne
 Probe Info  		C45(0.00); C187(0.00); C200(0.00)  LDD0162  [5]
WYneC
 Probe Info  		N.A.  LDD0014  [6]
WYneN
 Probe Info  		C299(0.00); C187(0.00); C45(0.00)  LDD0021  [6]
WYneO
 Probe Info  		C299(0.00); C187(0.00)  LDD0022  [6]
SF
 Probe Info  		N.A.  LDD0028  [7]
HHS-475
 Probe Info  		Y190(2.32); Y199(1.47); Y47(1.50); Y49(1.60)  LDD2238  [8]
HHS-482
 Probe Info  		Y178(1.16); Y190(1.07); Y210(1.35); Y47(1.12)  LDD2239  [8]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 A2780 C45(1.49)  LDD2254  [3]
 LDCM0023  KB03 A2780 C45(1.52)  LDD2671  [3]
 LDCM0024  KB05 NCI-H2122 C45(1.45)  LDD3354  [3]
 LDCM0500  Nucleophilic fragment 13a MDA-MB-231 C187(1.04); C200(1.05)  LDD2093  [4]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C187(1.36); C200(1.04)  LDD2099  [4]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C187(0.67); C200(0.45)  LDD2109  [4]
 LDCM0518  Nucleophilic fragment 22a MDA-MB-231 C187(1.15); C200(0.94)  LDD2111  [4]
 LDCM0526  Nucleophilic fragment 26a MDA-MB-231 C187(1.12)  LDD2119  [4]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C187(0.98)  LDD2129  [4]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C187(1.64)  LDD2136  [4]
 LDCM0211  Nucleophilic fragment 3b MDA-MB-231 C187(2.92)  LDD1700  [4]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Acetyl-CoA carboxylase 1 (ACACA) . Q13085
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Telomeric repeat-binding factor 2-interacting protein 1 (TERF2IP) RAP1 family Q9NYB0

The Drug(s) Related To This Target

Approved
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Lumateperone Small molecular drug DB06077
Sulindac Small molecular drug DB00605
Investigative
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Exisulind Small molecular drug DB06246
Fidarestat Small molecular drug DB02021
Zopolrestat Small molecular drug DB08772
Nicotinamide Adenine Dinucleotide Phosphate . DB03461
Discontinued
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Tolrestat Small molecular drug DB02383

References

1 Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors. J Med Chem. 2022 Aug 11;65(15):10408-10418. doi: 10.1021/acs.jmedchem.2c00272. Epub 2022 Jul 26.
2 Oxidant-Induced Bioconjugation for Protein Labeling in Live Cells. ACS Chem Biol. 2023 Jan 20;18(1):112-122. doi: 10.1021/acschembio.2c00740. Epub 2022 Dec 21.
3 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
4 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761
5 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060
6 A modification-centric assessment tool for the performance of chemoproteomic probes. Nat Chem Biol. 2022 Aug;18(8):904-912. doi: 10.1038/s41589-022-01074-8. Epub 2022 Jul 21.
Mass spectrometry data entry: PXD027758 , PXD027755 , PXD027760 , PXD027762 , PXD027756 , PXD027591 , PXD007149 , PXD030064 , PXD032392 , PXD027789 , PXD027767 , PXD027764
7 Solid Phase Synthesis of Fluorosulfate Containing Macrocycles for Chemoproteomic Workflows. bioRxiv [Preprint]. 2023 Feb 18:2023.02.17.529022. doi: 10.1101/2023.02.17.529022.
Mass spectrometry data entry: PXD039931
8 Global targeting of functional tyrosines using sulfur-triazole exchange chemistry. Nat Chem Biol. 2020 Feb;16(2):150-159. doi: 10.1038/s41589-019-0404-5. Epub 2019 Nov 25.