Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T93105
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| Former ID |
TTDR00444
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| Target Name |
Presenilin 1
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| Gene Name |
PSEN1
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| Synonyms |
PS-1; PS1; S182 protein; PSEN1
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| Target Type |
Clinical Trial
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| Function |
Probable catalytic subunit of the gamma-secretase complex, an endoprotease complex that catalyzes the intramembrane cleavage of integral membrane proteins such as Notch receptors and APP (beta-amyloid precursor protein). Requires the other members of the gamma-secretase complex to have a protease activity. May play a role in intracellular signaling and gene expression or in linking chromatin to thenuclear membrane. Stimulates cell-cell adhesion though its association with the E-cadherin/catenin complex. Under conditions of apoptosis or calcium influx, cleaves E-cadherin promoting the disassembly of the E-cadherin/catenin complex and increasing the pool of cytoplasmic beta-catenin, thus negatively regulating Wnt signaling. May also play a role in hematopoiesis.
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| BioChemical Class |
Peptidase
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| Target Validation |
T93105
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| UniProt ID | |||||
| EC Number |
EC 3.4.23.-
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| Sequence |
MTELPAPLSYFQNAQMSEDNHLSNTVRSQNDNRERQEHNDRRSLGHPEPLSNGRPQGNSR
QVVEQDEEEDEELTLKYGAKHVIMLFVPVTLCMVVVVATIKSVSFYTRKDGQLIYTPFTE DTETVGQRALHSILNAAIMISVIVVMTILLVVLYKYRCYKVIHAWLIISSLLLLFFFSFI YLGEVFKTYNVAVDYITVALLIWNFGVVGMISIHWKGPLRLQQAYLIMISALMALVFIKY LPEWTAWLILAVISVYDLVAVLCPKGPLRMLVETAQERNETLFPALIYSSTMVWLVNMAE GDPEAQRRVSKNSKYNAESTERESQDTVAENDDGGFSEEWEAQRDSHLGPHRSTPESRAA VQELSSSILAGEDPEERGVKLGLGDFIFYSVLVGKASATASGDWNTTIACFVAILIGLCL TLLLLAIFKKALPALPISITFGLVFYFATDYLVQPFMDQLAFHQFYI |
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| Drugs and Mode of Action | |||||
| Inhibitor | (2S,3R)-2-(benzyloxy)-3-methoxycyclohexanone | Drug Info | [528191] | ||
| (5R,6S)-5,6-bis(benzyloxy)cyclohex-2-enone | Drug Info | [528191] | |||
| (5R,6S)-6-(benzyloxy)-5-methoxycyclohex-2-enone | Drug Info | [528191] | |||
| (S)-FLURBIPROFEN | Drug Info | [528008] | |||
| 1-benzoyl-2-benzyl-1,2-dihydropyridin-3(6H)-one | Drug Info | [528191] | |||
| 1-Chloro-4-(1-phenyl-cyclohexanesulfonyl)-benzene | Drug Info | [527542] | |||
| Drug 311383 | Drug Info | [527143] | |||
| Drug 311440 | Drug Info | [527143] | |||
| Drug 311951 | Drug Info | [527143] | |||
| Drug 311952 | Drug Info | [527143] | |||
| R-flurbiprofen | Drug Info | [528008] | |||
| Pathways | |||||
| KEGG Pathway | Wnt signaling pathway | ||||
| Notch signaling pathway | |||||
| Neurotrophin signaling pathway | |||||
| Alzheimer' | |||||
| s disease | |||||
| NetPath Pathway | Notch Signaling Pathway | ||||
| PANTHER Pathway | Alzheimer disease-amyloid secretase pathway | ||||
| Alzheimer disease-presenilin pathway | |||||
| Notch signaling pathway | |||||
| Pathway Interaction Database | Notch signaling pathway | ||||
| Presenilin action in Notch and Wnt signaling | |||||
| p75(NTR)-mediated signaling | |||||
| Syndecan-3-mediated signaling events | |||||
| Reactome | Degradation of the extracellular matrix | ||||
| WikiPathways | Notch Signaling Pathway | ||||
| Notch Signaling Pathway | |||||
| Alzheimers Disease | |||||
| References | |||||
| Ref 527143 | J Med Chem. 2004 Jul 29;47(16):3931-3.Discovery of a Subnanomolar helical D-tridecapeptide inhibitor of gamma-secretase. | ||||
| Ref 527542 | Bioorg Med Chem Lett. 2005 May 16;15(10):2685-8.Aryl sulfones: a new class of gamma-secretase inhibitors. | ||||
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