General Information of Drug Therapeutic Target (DTT) (ID: TTEX6LM)

DTT Name GABA(A) receptor gamma-3 (GABRG3)
Synonyms GABRG3
Gene Name GABRG3
DTT Type
Successful target
[1]
BioChemical Class
Ligand-gated ion channel
UniProt ID
GBRG3_HUMAN
TTD ID
T28722
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAPKLLLLLCLFSGLHARSRKVEEDEYEDSSSNQKWVLAPKSQDTDVTLILNKLLREYDK
KLRPDIGIKPTVIDVDIYVNSIGPVSSINMEYQIDIFFAQTWTDSRLRFNSTMKILTLNS
NMVGLIWIPDTIFRNSKTAEAHWITTPNQLLRIWNDGKILYTLRLTINAECQLQLHNFPM
DEHSCPLIFSSYGYPKEEMIYRWRKNSVEAADQKSWRLYQFDFMGLRNTTEIVTTSAGDY
VVMTIYFELSRRMGYFTIQTYIPCILTVVLSWVSFWIKKDATPARTALGITTVLTMTTLS
TIARKSLPRVSYVTAMDLFVTVCFLFVFAALMEYATLNYYSSCRKPTTTKKTTSLLHPDS
SRWIPERISLQAPSNYSLLDMRPPPTAMITLNNSVYWQEFEDTCVYECLDGKDCQSFFCC
YEECKSGSWRKGRIHIDILELDSYSRVFFPTSFLLFNLVYWVGYLYL
Function
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functionsas receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand- gated chloride channel.
KEGG Pathway
Neuroactive ligand-receptor interaction (hsa04080 )
Retrograde endocannabinoid signaling (hsa04723 )
GABAergic synapse (hsa04727 )
Morphine addiction (hsa05032 )
Nicotine addiction (hsa05033 )
Reactome Pathway
GABA A receptor activation (R-HSA-977441 )
Ligand-gated ion channel transport (R-HSA-975298 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
14 Approved Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Allopregnanolone DMNLHAC Depression 6A70-6A7Z approved [2]
Bentazepam DMRVBWU Anxiety disorder 6B00-6B0Z Approved [1]
Clobazam - Lundbeck DMW1OQ0 Anxiety disorder 6B00-6B0Z Approved [3]
Etomidate DMZI3WO Anaesthesia 9A78.6 Approved [3]
Flumazenil DMPCG2L Benzodiazepine overdose PC91 Approved [4]
Ganaxolone DMXJMKF Epileptic seizures 8A61-8A6Z Approved [2]
Mebutamate DM0KYI4 Anxiety disorder 6B00-6B0Z Approved [3]
Metharbital DM5A38V Epilepsy 8A60-8A68 Approved [3]
Remimazolam DMLVSYX Procedural sedation JB0C.3 Approved [5]
Stiripentol DMMSDOY Dravet syndrome 8A61.11 Approved [6]
Talbutal DM214Q8 Irritability MB24 Approved [3]
Thiamylal DMHDF7B Anaesthesia 9A78.6 Approved [3]
Zolpidem DMWOSKJ Insomnia 7A00-7A0Z Approved [4]
Zuranolone DMGR98T Postpartum depression 6E20.0 Approved [2]
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⏷ Show the Full List of 14 Approved Drug(s)
10 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Arbaclofen placarbil DMO628K Fragile X syndrome LD55 Phase 3 [2]
Clomethiazole DMSPN58 Stroke 8B20 Phase 3 [7]
Pagoclone DMHWY2G Anxiety disorder 6B00-6B0Z Phase 2/3 [8]
Etazolate DMOCID7 Neurodegenerative disorder 8A20-8A23 Phase 2 [9]
EVT-201 DMQGBM1 Insomnia 7A00-7A0Z Phase 2 [4]
SARIPIDEM DM5R89X Anxiety disorder 6B00-6B0Z Phase 2 [10]
T-2007 DMF9Z2T Epilepsy 8A60-8A68 Phase 2 [4]
AZD-3043 DMXFYN0 Anaesthesia 9A78.6 Phase 1 [11]
NSD-788 DM5QHID Anxiety disorder 6B00-6B0Z Phase 1 [4]
Org-25435 DMBG534 Epilepsy 8A60-8A68 Phase 1 [12]
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⏷ Show the Full List of 10 Clinical Trial Drug(s)
21 Discontinued Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Suriclone DMC14HL Anxiety disorder 6B00-6B0Z Discontinued in Preregistration [13]
Ocinaplon DMQN3JX Generalized anxiety disorder 6B00 Discontinued in Phase 3 [14]
Pazinaclone DM1FST8 Anxiety disorder 6B00-6B0Z Discontinued in Phase 3 [15]
Y-23684 DM3EZ68 Anxiety disorder 6B00-6B0Z Discontinued in Phase 3 [16]
LORECLEZOLE DMCZI62 Epileptic seizures 8A61-8A6Z Discontinued in Phase 2 [17]
NGD 91-3 DMDAUCR Anxiety disorder 6B00-6B0Z Discontinued in Phase 2 [18]
RESEQUINIL DM3EAYN Epilepsy 8A60-8A68 Discontinued in Phase 2 [19]
RO-48-6791 DMH912O Anxiety disorder 6B00-6B0Z Discontinued in Phase 2 [20]
SL-65.1498 DMS8AHE Anxiety disorder 6B00-6B0Z Discontinued in Phase 2 [21]
Suritozole DMDZ7AY Major depressive disorder 6A70.3 Discontinued in Phase 2 [22]
CCD-3693 DMMEC1W Anxiety disorder 6B00-6B0Z Discontinued in Phase 1 [23]
CTP-354 DMXY43L Pain MG30-MG3Z Discontinued in Phase 1 [24]
Org-21465 DMMYI9U Anaesthesia 9A78.6 Discontinued in Phase 1 [25]
RO-48-8684 DMOX8AD Anxiety disorder 6B00-6B0Z Discontinued in Phase 1 [26]
Co-152791 DMU5TZD Epilepsy 8A60-8A68 Terminated [28]
Girisopam DMSVMF2 Anxiety disorder 6B00-6B0Z Terminated [29]
NSD-721 DMF2XMA Anxiety disorder 6B00-6B0Z Terminated [4]
Ro-19-8022 DMFRCM2 Anxiety disorder 6B00-6B0Z Terminated [30]
RU-33965 DMSWFMQ Alzheimer disease 8A20 Terminated [31]
ZK-91296 DMJYIVA Alzheimer disease 8A20 Terminated [32]
ZK-93426 DMMDQ5T Alzheimer disease 8A20 Terminated [33]
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⏷ Show the Full List of 21 Discontinued Drug(s)
1 Preclinical Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
RWJ-51204 DMMVS07 Anxiety disorder 6B00-6B0Z Preclinical [27]
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25 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
AA-29504 DMI59T7 Major depressive disorder 6A70.3 Investigative [4]
alpha3IA DM257WX Discovery agent N.A. Investigative [4]
alpha5IA DMTU5QR Discovery agent N.A. Investigative [4]
C-21191 DMCAO3V Anxiety disorder 6B00-6B0Z Investigative [4]
CP-409092 DMROYD7 Discovery agent N.A. Investigative [34]
DMCM DMK3WY4 Discovery agent N.A. Investigative [4]
DOV-51892 DMQIK9S Panic disorder 6B01 Investigative [4]
GIDAZEPAM DMASR6T Anxiety disorder 6B00-6B0Z Investigative [35]
HZ-166 DMLU6VM Neuropathic pain 8E43.0 Investigative [4]
isonipecotic acid DMO1ZHE Discovery agent N.A. Investigative [4]
JM-1232(-) DMWMRO2 Anaesthesia 9A78.6 Investigative [4]
NGD 96-3 DMWD7I3 Insomnia 7A00-7A0Z Investigative [4]
piperidine-4-sulphonic acid DMMIZWE Discovery agent N.A. Investigative [4]
PNU 101017 DMKBCS2 Discovery agent N.A. Investigative [36]
Ro-15-3505 DM4NW3U Discovery agent N.A. Investigative [37]
TBPS DMFC3XP Discovery agent N.A. Investigative [4]
tetrahydrodeoxycorticosterone DMF8M0W Discovery agent N.A. Investigative [4]
TP003 DMRHDGN Discovery agent N.A. Investigative [4]
UC-1011 DMCRFT5 Alzheimer disease 8A20 Investigative [4]
UC-2024 DMJVT4K Premenstrual syndrome GA34.40 Investigative [4]
UC-2029 DMGSOZ7 Premenstrual syndrome GA34.40 Investigative [4]
[18F]fluoroethylflumazenil DMPWART Discovery agent N.A. Investigative [4]
[35S]TBPS DMSD51L Discovery agent N.A. Investigative [4]
[3H]CGS8216 DMLP68J Inflammation 1A00-CA43.1 Investigative [4]
[3H]Ro154513 DMMBWKL Discovery agent N.A. Investigative [4]
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⏷ Show the Full List of 25 Investigative Drug(s)

References

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3 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
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6 Stiripentol, a putative antiepileptic drug, enhances the duration of opening of GABA-A receptor channels. Epilepsia. 2006 Apr;47(4):704-16.
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9 Etazolate, a neuroprotective drug linking GABA(A) receptor pharmacology to amyloid precursor protein processing. J Neurochem. 2008 Jul;106(1):392-404.
10 Behavioural effects of novel benzodiazepine (omega) receptor agonists and partial agonists: increases in punished responding and antagonism of the pentylenetetrazole cue. Behav Pharmacol. 1995 Mar;6(2):116-126.
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22 Chronic postinjury administration of MDL 26,479 (Suritozole), a negative modulator at the GABAA receptor, and cognitive impairment in rats following traumatic brain injury. J Neurosurg. 1995 Nov;83(5):878-83.
23 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
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35 Discriminative effects of phenazepam and gidazepam in rats: comparison with other GABA-related drugs. Pharmacol Biochem Behav. 1999 Oct;64(2):397-401.
36 Neuroprotective effects of the GABA(A) receptor partial agonist U-101017 in 3-acetylpyridine-treated rats. Neurosci Lett. 1997 May 30;228(1):45-9.
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