Target Information
Target General Infomation | |||||
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Target ID |
T04507
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Former ID |
TTDR00806
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Target Name |
Presynaptic density protein 95
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Gene Name |
DLG4
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Synonyms |
Discs, large homolog 4; PSD-95; Postsynaptic density-95; DLG4
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Target Type |
Clinical Trial
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Disease | Cerebrovascular ischaemia [ICD9: 434.91; ICD10: I61-I63] | ||||
Function |
Interacts with the cytoplasmictail of NMDA receptor subunits and shaker-type potassium channels. Required for synaptic plasticity associated with NMDA receptor signaling. Overexpression or depletion of DLG4 changes the ratio of excitatory to inhibitory synapses in hippocampal neurons. May reduce the amplitude of ASIC3 acid-evoked currents by retaining the channel intracellularly. May regulate the intracellular trafficking of ADR1B (By similarity).
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BioChemical Class |
Membrane-associated guanylate kinase
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Target Validation |
T04507
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UniProt ID | |||||
Sequence |
MDCLCIVTTKKYRYQDEDTPPLEHSPAHLPNQANSPPVIVNTDTLEAPGYELQVNGTEGE
MEYEEITLERGNSGLGFSIAGGTDNPHIGDDPSIFITKIIPGGAAAQDGRLRVNDSILFV NEVDVREVTHSAAVEALKEAGSIVRLYVMRRKPPAEKVMEIKLIKGPKGLGFSIAGGVGN QHIPGDNSIYVTKIIEGGAAHKDGRLQIGDKILAVNSVGLEDVMHEDAVAALKNTYDVVY LKVAKPSNAYLSDSYAPPDITTSYSQHLDNEISHSSYLGTDYPTAMTPTSPRRYSPVAKD LLGEEDIPREPRRIVIHRGSTGLGFNIVGGEDGEGIFISFILAGGPADLSGELRKGDQIL SVNGVDLRNASHEQAAIALKNAGQTVTIIAQYKPEEYSRFEAKIHDLREQLMNSSLGSGT ASLRSNPKRGFYIRALFDYDKTKDCGFLSQALSFRFGDVLHVIDASDEEWWQARRVHSDS ETDDIGFIPSKRRVERREWSRLKAKDWGSSSGSQGREDSVLSYETVTQMEVHYARPIIIL GPTKDRANDDLLSEFPDKFGSCVPHTTRPKREYEIDGRDYHFVSSREKMEKDIQAHKFIE AGQYNSHLYGTSVQSVREVAEQGKHCILDVSANAVRRLQAAHLHPIAIFIRPRSLENVLE INKRITEEQARKAFDRATKLEQEFTECFSAIVEGDSFEEIYHKVKRVIEDLSGPYIWVPA RERL |
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Drugs and Mode of Action | |||||
Inhibitor | 2-Methyl-2,4-Pentanediol | Drug Info | [551393] | ||
FETAV | Drug Info | [529713] | |||
Guanosine-5'-Monophosphate | Drug Info | [551393] | |||
KSG-LDTKNYKQTSV | Drug Info | [529713] | |||
KSG-YEKLSSIESDV | Drug Info | [529713] | |||
N-(3,4-Dichlorophenyl)propyl-ETAV | Drug Info | [529713] | |||
N-(3,4-Difluorophenyl)propyl-ETAV | Drug Info | [529713] | |||
N-(Naphthalene-2-yl)ethyl-ETAV | Drug Info | [529713] | |||
N-Benzyl-ETAV | Drug Info | [529713] | |||
N-Butyl-ETAV | Drug Info | [529713] | |||
N-Cyclohexylethyl-ETAV | Drug Info | [529713] | |||
N-Cyclohexylmethyl-ETAV | Drug Info | [529713] | |||
N-Ethyl-ETAV | Drug Info | [529713] | |||
N-Methyl-ETAV | Drug Info | [529713] | |||
N-Phenylethyl-ETAV | Drug Info | [529713] | |||
N-Phenylpropyl-ETAV | Drug Info | [529713] | |||
N-Propyl-ETAV | Drug Info | [529713] | |||
Tat-NR2B9c | Drug Info | [525512], [531828], [533640] | |||
YGRKKRRQRRR-KLSSIESDV | Drug Info | [529713] | |||
Pathways | |||||
KEGG Pathway | Hippo signaling pathway | ||||
Glutamatergic synapse | |||||
Huntington' | |||||
s disease | |||||
Cocaine addiction | |||||
PANTHER Pathway | Huntington disease | ||||
Pathway Interaction Database | ErbB4 signaling events | ||||
Reactome | Trafficking of AMPA receptors | ||||
Unblocking of NMDA receptor, glutamate binding and activation | |||||
CREB phosphorylation through the activation of CaMKII | |||||
Ras activation uopn Ca2+ infux through NMDA receptor | |||||
RHO GTPases activate CIT | |||||
RAF/MAP kinase cascade | |||||
WikiPathways | Neurotransmitter Receptor Binding And Downstream Transmission In The Postsynaptic Cell | ||||
L1CAM interactions | |||||
References | |||||
Ref 525512 | Specific coupling of NMDA receptor activation to nitric oxide neurotoxicity by PSD-95 protein. Science. 1999 Jun 11;284(5421):1845-8. | ||||
Ref 529713 | J Med Chem. 2008 Oct 23;51(20):6450-9. Epub 2008 Sep 24.Modified peptides as potent inhibitors of the postsynaptic density-95/N-methyl-D-aspartate receptor interaction. | ||||
Ref 531828 | Treatment of stroke with a PSD-95 inhibitor in the gyrencephalic primate brain. Nature. 2012 Feb 29;483(7388):213-7. |
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