Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTF45NW)

• DTT Name: Strychnine-binding glycine receptor (GLRA1)
• Synonyms: Strychnine-insensitive glycine receptor; Strychnine binding subunit; Glycine receptor 48 kDa subunit; GLRA1
• Gene Name: GLRA1
• DTT Type: Successful target; [1]
• BioChemical Class: Neurotransmitter receptor
• UniProt ID: GLRA1_HUMAN
• TTD ID: T50269
• Sequence:
  MYSFNTLRLYLWETIVFFSLAASKEAEAARSAPKPMSPSDFLDKLMGRTSGYDARIRPNF
  KGPPVNVSCNIFINSFGSIAETTMDYRVNIFLRQQWNDPRLAYNEYPDDSLDLDPSMLDS
  IWKPDLFFANEKGAHFHEITTDNKLLRISRNGNVLYSIRITLTLACPMDLKNFPMDVQTC
  IMQLESFGYTMNDLIFEWQEQGAVQVADGLTLPQFILKEEKDLRYCTKHYNTGKFTCIEA
  RFHLERQMGYYLIQMYIPSLLIVILSWISFWINMDAAPARVGLGITTVLTMTTQSSGSRA
  SLPKVSYVKAIDIWMAVCLLFVFSALLEYAAVNFVSRQHKELLRFRRKRRHHKSPMLNLF
  QEDEAGEGRFNFSAYGMGPACLQAKDGISVKGANNSNTTNPPPAPSKSPEEMRKLFIQRA
  KKIDKISRIGFPMAFLIFNMFYWIIYKIVRREDVHNQ
• Function: The glycine receptor is a neurotransmitter-gated ion channel. Binding of glycine to its receptor increases the chloride conductance and thus produces hyperpolarization (inhibition of neuronal firing).
• KEGG Pathway: Neuroactive ligand-receptor interaction (hsa04080)
• Reactome Pathway: Ligand-gated ion channel transport (R-HSA-975298)

Molecular Interaction Atlas (MIA) of This DTT

2 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
THIOCOLCHICOSIDE	DMEPWYA	Muscle spasm	MB47.3	Approved	[1]
D-Serine	DM3YH4I	N. A.	N. A.	Phase 4	[2]

1 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
GINKOLIDE B	DMLIM7B	Sepsis	1G40-1G41	Terminated	[3]

12 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
10-methoxy-ginkgolide C	DM2H6KD	Discovery agent	N.A.	Investigative	[3]
3,14-DIDEHYDROGINKGOLIDE A	DMR9WF7	Discovery agent	N.A.	Investigative	[3]
3-demethoxy-3-D-lyxopyranosylaminothiocolchicine	DME8VPC	Discovery agent	N.A.	Investigative	[1]
3-demethoxy-3-D-mannopyranosylaminothiocolchicine	DMALMGH	Discovery agent	N.A.	Investigative	[1]
3-demethoxy-3-D-xylopyranosylaminothiocolchicine	DMXFVD1	Discovery agent	N.A.	Investigative	[1]
3-demethoxy-3-L-fucopyranosylaminothiocolchicine	DM4ERYF	Discovery agent	N.A.	Investigative	[1]
3-demethoxy-3D-glucopyranosylaminothiocolchicine	DMID7TC	Discovery agent	N.A.	Investigative	[1]
GINKGOLIDE A	DMKZJ7T	Discovery agent	N.A.	Investigative	[3]
Ginkgolide C	DMVN374	Discovery agent	N.A.	Investigative	[3]
Ginkgolide J	DMUOMP1	Discovery agent	N.A.	Investigative	[3]
Ginkgolide M	DMHWIG6	Discovery agent	N.A.	Investigative	[3]
[3H]strychnine	DM0Y2SC	Discovery agent	N.A.	Investigative	[1]

References

• [1] 3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds. J Med Chem. 2006 Sep 7;49(18):5571-7.
• [2] Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5.
• [3] Probing the pharmacophore of ginkgolides as glycine receptor antagonists. J Med Chem. 2007 Apr 5;50(7):1610-7.