Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT6XFEU)

• DTT Name: GABA(A) receptor rho1 (GABRR1)
• Synonyms: Gamma-aminobutyric acid receptor subunit rho-1; GABA(C) receptor1; GABA(A) receptor subunit rho-1
• Gene Name: GABRR1
• DTT Type: Literature-reported target; [1]
• UniProt ID: GBRR1_HUMAN
• TTD ID: T99665
• Sequence:
  MLAVPNMRFGIFLLWWGWVLATESRMHWPGREVHEMSKKGRPQRQRREVHEDAHKQVSPI
  LRRSPDITKSPLTKSEQLLRIDDHDFSMRPGFGGPAIPVGVDVQVESLDSISEVDMDFTM
  TLYLRHYWKDERLSFPSTNNLSMTFDGRLVKKIWVPDMFFVHSKRSFIHDTTTDNVMLRV
  QPDGKVLYSLRVTVTAMCNMDFSRFPLDTQTCSLEIESYAYTEDDLMLYWKKGNDSLKTD
  ERISLSQFLIQEFHTTTKLAFYSSTGWYNRLYINFTLRRHIFFFLLQTYFPATLMVMLSW
  VSFWIDRRAVPARVPLGITTVLTMSTIITGVNASMPRVSYIKAVDIYLWVSFVFVFLSVL
  EYAAVNYLTTVQERKEQKLREKLPCTSGLPPPRTAMLDGNYSDGEVNDLDNYMPENGEKP
  DRMMVQLTLASERSSPQRKSQRSSYVSMRIDTHAIDKYSRIIFPAAYILFNLIYWSIFS
• Function: GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel. Rho-1 GABA receptor could play a role in retinal neurotransmission.
• KEGG Pathway:
  Neuroactive ligand-receptor interaction (hsa04080)
  Retrograde endocannabinoid signaling (hsa04723)
  GABAergic synapse (hsa04727)
  Morphine addiction (hsa05032)
  Nicotine addiction (hsa05033)
• Reactome Pathway: GABA receptor activation (R-HSA-977443)

Molecular Interaction Atlas (MIA) of This DTT

10 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(+/-)-cis-2-CAMP	DMY3J0B	Discovery agent	N.A.	Investigative	[1]
5-Me-IAA	DMFZN7J	Discovery agent	N.A.	Investigative	[1]
aza-THIP	DML70NC	Discovery agent	N.A.	Investigative	[1]
CACA	DMPKFYZ	Discovery agent	N.A.	Investigative	[2]
cis-3-ACPBPA	DMQ0EA7	Discovery agent	N.A.	Investigative	[1]
Isonipecotic acid	DMO1ZHE	Discovery agent	N.A.	Investigative	[1]
piperidine-4-sulphonic acid	DMMIZWE	Discovery agent	N.A.	Investigative	[1]
TBPS	DMFC3XP	Discovery agent	N.A.	Investigative	[1]
TPMPA	DMBF6KS	Discovery agent	N.A.	Investigative	[1]
trans-3-ACPBPA	DM6HI8W	Discovery agent	N.A.	Investigative	[1]

References

• [1] 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: 420).
• [2] Characterization of bicuculline/baclofen-insensitive (rho-like) gamma-aminobutyric acid receptors expressed in Xenopus oocytes. II. Pharmacology of gamma-aminobutyric acidA and gamma-aminobutyric acidB receptor agonists and antagonists. Mol Pharmacol. 1993 Apr;43(4):609-25.