Details of the Drug Therapeutic Target (DTT)

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

• DTT Name: Na(+)/Cl(-) betaine/GABA transporter (SLC6A12)
• Synonyms: Solute carrier family 6 member 12; Sodium- and chloride-dependent betaine transporter; BGT-1
• Gene Name: SLC6A12
• DTT Type: Literature-reported target; [1]
• UniProt ID: S6A12_HUMAN
• TTD ID: T08446
• Sequence:
  MDGKVAVQECGPPAVSWVPEEGEKLDQEDEDQVKDRGQWTNKMEFVLSVAGEIIGLGNVW
  RFPYLCYKNGGGAFFIPYFIFFFVCGIPVFFLEVALGQYTSQGSVTAWRKICPLFQGIGL
  ASVVIESYLNVYYIIILAWALFYLFSSFTSELPWTTCNNFWNTEHCTDFLNHSGAGTVTP
  FENFTSPVMEFWERRVLGITSGIHDLGSLRWELALCLLLAWVICYFCIWKGVKSTGKVVY
  FTATFPYLMLVILLIRGVTLPGAYQGIIYYLKPDLFRLKDPQVWMDAGTQIFFSFAICQG
  CLTALGSYNKYHNNCYKDCIALCFLNSATSFVAGFVVFSILGFMSQEQGVPISEVAESGP
  GLAFIAFPKAVTMMPLSQLWSCLFFIMLIFLGLDSQFVCVECLVTASIDMFPRQLRKSGR
  RELLILTIAVMCYLIGLFLVTEGGMYIFQLFDYYASSGICLLFLSLFEVVCISWVYGADR
  FYDNIEDMIGYRPWPLVKISWLFLTPGLCLATFLFSLSKYTPLKYNNVYVYPPWGYSIGW
  FLALSSMVCVPLFVVITLLKTRGPFRKRLRQLITPDSSLPQPKQHPCLDGSAGRNFGPSP
  TREGLIAGEKETHL
• Function: Transports betaine and GABA. May have a role in regulation of GABAergic transmission in the brain through the reuptake of GABA into presynaptic terminals, as well as in osmotic regulation.
• KEGG Pathway:
  Synaptic vesicle cycle (hsa04721)
  GABAergic synapse (hsa04727)
• Reactome Pathway:
  Na+/Cl- dependent neurotransmitter transporters (R-HSA-442660)
  Creatine metabolism (R-HSA-71288)
  Reuptake of GABA (R-HSA-888593)
  Amino acid transport across the plasma membrane (R-HSA-352230)

Molecular Interaction Atlas (MIA) of This DTT

5 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(R)-EF-1520	DM297MU	Discovery agent	N.A.	Investigative	[2]
(R/S) EF-1500	DMYDG27	Discovery agent	N.A.	Investigative	[2]
(S)-EF-1520	DM0EQTM	Discovery agent	N.A.	Investigative	[2]
LU32-176B	DM2YOVC	Discovery agent	N.A.	Investigative	[3]
NNC052090	DMCGF3U	Discovery agent	N.A.	Investigative	[1]

The Drug Transporter (DTP) Role of This DTT

• DTT DTP Name: Na(+)/Cl(-) betaine/GABA transporter (SLC6A12) DTP Info
• Gene Name: SLC6A12

4 Approved Drug(s) Transported by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Betaine	DMGRZW2	Cystitis	GC00	Approved	[4]
Glycine	DMIOZ29	Allergic rhinitis	CA08.0	Approved	[5]
L-Proline	DMKSTWR	Malnutrition	5B50-5B71	Approved	[5]
Quinine	DMSWYF5	Malaria	1F40-1F45	Approved	[6]

1 Investigative Drug(s) Transported by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CHOLINE	DM5D9YK	Insomnia	7A00-7A0Z	Investigative	[5]

References

• [1] 1-(3-(9H-carbazol-9-yl)-1-propyl)-4-(2-methoxyphenyl)-4-piperidinol, a novel subtype selective inhibitor of the mouse type II GABA-transporter. Br J Pharmacol. 1997 Mar;120(6):983-5.
• [2] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 932).
• [3] First demonstration of a functional role for central nervous system betaine/{gamma}-aminobutyric acid transporter (mGAT2) based on synergistic anti... J Pharmacol Exp Ther. 2005 Feb;312(2):866-74.
• [4] Deletion of the betaine-GABA transporter (BGT1; slc6a12) gene does not affect seizure thresholds of adult mice. Epilepsy Res. 2011 Jun;95(1-2):70-81.
• [5] Interpreting metabolomic profiles using unbiased pathway models. PLoS Comput Biol. 2010 Feb 26;6(2):e1000692.
• [6] The Transporter Classification Database (TCDB): recent advances. Nucleic Acids Res. 2016 Jan 4;44(D1):D372-9. (ID: 2.A.22.3.1)