Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTWME23)

• DTT Name: Regulator of G-protein signaling 8 (RGS8)
• Synonyms: RGS8
• Gene Name: RGS8
• DTT Type: Patented-recorded target; [1]
• UniProt ID: RGS8_HUMAN
• TTD ID: T03529
• Sequence:
  MAALLMPRRNKGMRTRLGCLSHKSDSCSDFTAILPDKPNRALKRLSTEEATRWADSFDVL
  LSHKYGVAAFRAFLKTEFSEENLEFWLACEEFKKTRSTAKLVSKAHRIFEEFVDVQAPRE
  VNIDFQTREATRKNLQEPSLTCFDQAQGKVHSLMEKDSYPRFLRSKMYLDLLSQSQRRLS
• Function: Regulates G protein-coupled receptor signaling cascades, including signaling via muscarinic acetylcholine receptor CHRM2 and dopamine receptor DRD2 (By similarity). Inhibits signal transduction by increasing the GTPase activity of G protein alpha subunits, thereby driving them into their inactive GDP-bound form. Modulates the activity of potassium channels that are activated in response to DRD2 and CHRM2 signaling (By similarity).
• Reactome Pathway: G alpha (i) signalling events (R-HSA-418594)

Molecular Interaction Atlas (MIA) of This DTT

2 Patented Agent(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
1-Benzyl-3-bromo-1H-pyrrole-2,5-dione	DML8RVS	N. A.	N. A.	Patented	[2]
1-Benzyl-3-p-tolyl-1H-pyrrole-2,5-dione	DMWY9GM	N. A.	N. A.	Patented	[2]

3 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CCG-50014	DMUQJ6X	Discovery agent	N.A.	Investigative	[1]
RGS4 inhibitor 13	DM4XVLB	Discovery agent	N.A.	Investigative	[1]
thiadiazolidinone (TDZD) deriv. 6	DM9CF45	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: 2813).
• [2] Small molecule inhibitors of RGS proteins. US8865750.