Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTG2UMS)

• DTT Name: Organic cation transporter 3 (OCT3)
• Synonyms: Solute carrier family 22 member 3; Extraneuronal monoamine transporter; EMTH
• Gene Name: SLC22A3
• DTT Type: Literature-reported target; [1]
• UniProt ID: S22A3_HUMAN
• TTD ID: T55948
• Sequence:
  MPSFDEALQRVGEFGRFQRRVFLLLCLTGVTFAFLFVGVVFLGTQPDHYWCRGPSAAALA
  ERCGWSPEEEWNRTAPASRGPEPPERRGRCQRYLLEAANDSASATSALSCADPLAAFPNR
  SAPLVPCRGGWRYAQAHSTIVSEFDLVCVNAWMLDLTQAILNLGFLTGAFTLGYAADRYG
  RIVIYLLSCLGVGVTGVVVAFAPNFPVFVIFRFLQGVFGKGTWMTCYVIVTEIVGSKQRR
  IVGIVIQMFFTLGIIILPGIAYFIPNWQGIQLAITLPSFLFLLYYWVVPESPRWLITRKK
  GDKALQILRRIAKCNGKYLSSNYSEITVTDEEVSNPSFLDLVRTPQMRKCTLILMFAWFT
  SAVVYQGLVMRLGIIGGNLYIDFFISGVVELPGALLILLTIERLGRRLPFAASNIVAGVA
  CLVTAFLPEGIAWLRTTVATLGRLGITMAFEIVYLVNSELYPTTLRNFGVSLCSGLCDFG
  GIIAPFLLFRLAAVWLELPLIIFGILASICGGLVMLLPETKGIALPETVDDVEKLGSPHS
  CKCGRNKKTPVSRSHL
• Function: Mediates potential-dependent transport of a variety of organic cations. May play a significant role in the disposition of cationic neurotoxins and neurotransmitters in the brain.
• KEGG Pathway: Choline metabolism in cancer (hsa05231)
• Reactome Pathway:
  Organic cation transport (R-HSA-549127)
  Abacavir transmembrane transport (R-HSA-2161517)

The Drug Transporter (DTP) Role of This DTT

• DTT DTP Name: Organic cation transporter 3 (SLC22A3) DTP Info
• Gene Name: SLC22A3

10 Approved Drug(s) Transported by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Acetylcholine	DMDF79Z	Cataract	9B10	Approved	[2]
Amphetamine	DMSZQAK	Attention deficit hyperactivity disorder	6A05.Z	Approved	[3]
Clonidine	DM6RZ9Q	Attention deficit hyperactivity disorder	6A05.Z	Approved	[4]
Entecavir	DM7VTQO	Hepatitis B virus infection	1E51.0	Approved	[5]
Epinephrine	DM3KJBC	Acute asthma	CA23	Approved	[6]
Ergotidine	DM78IME	Osteoarthritis	FA00-FA05	Approved	[6]
Metformin	DM89QE1	Colorectal carcinoma		Approved	[7]
Norepinephrine	DMOUC09	Alopecia	ED70	Approved	[6]
Propranolol	DM79NTF	Angina pectoris	BA40	Approved	[4]
Sodium chloride	DMM3950	Skin burns	ME65.0	Approved	[8]

1 Discontinued Drug(s) Transported by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Etilefrine	DM67PWD	Cardiovascular disease	BA00-BE2Z	Withdrawn from market	[9]

1 Preclinical Drug(s) Transported by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
N-methylpyridinium	DMVUKEW	N. A.	N. A.	Preclinical	[10]

1 Investigative Drug(s) Transported by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Guanidine	DM4GO8H	LambertEaton myasthenic syndrome	8C62	Investigative	[10]

References

• [1] Electrophysiological Characterization of Novel Effects of the Uptake-2 Blocker Decynium-22 (D-22) on Dopaminergic Neurons in the Substantia Nigra P... Neuroscience. 2019 Jan 1;396:154-165.
• [2] Organic cation transporters: physiology, toxicology and special focus on ethidium as a novel substrate. Curr Drug Metab. 2009 Jul;10(6):617-31.
• [3] Interaction of organic cation transporter 3 (SLC22A3) and amphetamine. J Neurochem. 2010 Jul;114(1):142-9.
• [4] Influx Transport of Cationic Drug at the Blood-Retinal Barrier: Impact on the Retinal Delivery of Neuroprotectants. Biol Pharm Bull. 2017;40(8):1139-1145.
• [5] Multiple SLC and ABC Transporters Contribute to the Placental Transfer of Entecavir. Drug Metab Dispos. 2017 Mar;45(3):269-278.
• [6] Differential pharmacological in vitro properties of organic cation transporters and regional distribution in rat brain. Neuropharmacology. 2006 Jun;50(8):941-52.
• [7] Expression of organic cation transporters OCT1 (SLC22A1) and OCT3 (SLC22A3) is affected by genetic factors and cholestasis in human liver. Hepatology. 2009 Oct;50(4):1227-40.
• [8] Organic cation transporter 3 (Slc22a3) is implicated in salt-intake regulation. J Neurosci. 2004 Mar 17;24(11):2846-51.
• [9] Drug specificity and intestinal membrane localization of human organic cation transporters (OCT). Biochem Pharmacol. 2005 Dec 5;70(12):1851-60.
• [10] Structure, function, and regional distribution of the organic cation transporter OCT3 in the kidney. Am J Physiol Renal Physiol. 2000 Sep;279(3):F449-58.