Details of Drug-Metabolizing Enzyme (DME)

General Information of Drug-Metabolizing Enzyme (DME) (ID: DEI8NGH)

• DME Name: UDP-glucuronosyltransferase 2B10 (UGT2B10)
• Synonyms: UDP-glucuronosyltransferase family 2 member B10; UDPGT 2B10; UGT2B10; OMIM: 600070; MGI: 2140962; HomoloGene: 117389; GeneCards: UGT2B10
• Gene Name: UGT2B10
• UniProt ID: UDB10_HUMAN
• INTEDE ID: DME0205
• Gene ID: 7365
• EC Number:
  EC: 2.4.1.17
  Transferase
  Glycosyltransferases
  Hexosyltransferase
  EC: 2.4.1.17
• Lineage:
  Species: Homo sapiens
  Kingdom: Metazoa
  Phylum: Chordata
  Class: Mammalia
  Order: Primates
  Family: Hominidae
  Genus: Homo
  Species: Homo sapiens
• Sequence:
  MALKWTTVLLIQLSFYFSSGSCGKVLVWAAEYSLWMNMKTILKELVQRGHEVTVLASSAS
  ILFDPNDSSTLKLEVYPTSLTKTEFENIIMQLVKRLSEIQKDTFWLPFSQEQEILWAIND
  IIRNFCKDVVSNKKLMKKLQESRFDIVFADAYLPCGELLAELFNIPFVYSHSFSPGYSFE
  RHSGGFIFPPSYVPVVMSKLSDQMTFMERVKNMLYVLYFDFWFQIFNMKKWDQFYSEVLG
  RPTTLSETMRKADIWLMRNSWNFKFPHPFLPNVDFVGGLHCKPAKPLPKEMEEFVQSSGE
  NGVVVFSLGSMVSNMTEERANVIATALAKIPQKVLWRFDGNKPDALGLNTRLYKWIPQND
  LLGHPKTRAFITHGGANGIYEAIYHGIPMVGIPLFFDQPDNIAHMKAKGAAVRVDFNTMS
  STDLLNALKTVINDPSYKENIMKLSRIQHDQPVKPLDRAVFWIEFVMRHKGAKHLRVAAH
  NLTWFQYHSLDVIGFLLACVATVLFIITKCCLFCFWKFARKGKKGKRD
• Function: This enzyme is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds.
• KEGG Pathway:
  Ascorbate and aldarate metabolism (hsa00053)
  Chemical carcinogenesis (hsa05204)
  Drug metabolism - cytochrome P450 (hsa00982)
  Drug metabolism - other enzymes (hsa00983)
  Metabolic pathways (hsa01100)
  Metabolism of xenobiotics by cytochrome P450 (hsa00980)
  Pentose and glucuronate interconversions (hsa00040)
  Porphyrin and chlorophyll metabolism (hsa00860)
  Retinol metabolism (hsa00830)
  Steroid hormone biosynthesis (hsa00140)
• Reactome Pathway: Glucuronidation (R-HSA-156588)

Molecular Interaction Atlas (MIA) of This DME

4 Approved Drug(s) Metabolized by This DME

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Cotinine	DMCEZ1B	Insecticide	N.A.	Approved	[1]
Desloratadine	DM56YN7	Allergic rhinitis	CA08.0	Approved	[2]
Ketotifen	DM74XKS	Allergic conjunctivitis	9A60.02	Approved	[]
Pizotyline	DMV74ZH	Headache	8A80-8A84	Approved	[3]

Experimental Enzyme Kinetic Data of Drugs

Drug Name	Indication	Highest Status	Kinetic Data	REF
Cotinine	Insecticide [N.A.]	Approved	Km = 0.0278 microM	[1]

References

• [1] Human UDP-glucuronosyltransferase (UGT) 2B10: validation of cotinine as a selective probe substrate, inhibition by UGT enzyme-selective inhibitors and antidepressant and antipsychotic drugs, and structural determinants of enzyme inhibition. Drug Metab Dispos. 2016 Mar;44(3):378-88.
• [2] Further characterization of the metabolism of desloratadine and its cytochrome P450 and UDP-glucuronosyltransferase inhibition potential: identification of desloratadine as a relatively selective UGT2B10 inhibitor. Drug Metab Dispos. 2015 Sep;43(9):1294-302.
• [3] Human UDP-glucuronosyltransferase (UGT) 2B10 in drug N-glucuronidation: substrate screening and comparison with UGT1A3 and UGT1A4. Drug Metab Dispos. 2013 Jul;41(7):1389-97.