Target Information
Target General Infomation | |||||
---|---|---|---|---|---|
Target ID |
T93105
|
||||
Former ID |
TTDR00444
|
||||
Target Name |
Presenilin 1
|
||||
Gene Name |
PSEN1
|
||||
Synonyms |
PS-1; PS1; S182 protein; PSEN1
|
||||
Target Type |
Clinical Trial
|
||||
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.
|
||||
BioChemical Class |
Peptidase
|
||||
Target Validation |
T93105
|
||||
UniProt ID | |||||
EC Number |
EC 3.4.23.-
|
||||
Sequence |
MTELPAPLSYFQNAQMSEDNHLSNTVRSQNDNRERQEHNDRRSLGHPEPLSNGRPQGNSR
QVVEQDEEEDEELTLKYGAKHVIMLFVPVTLCMVVVVATIKSVSFYTRKDGQLIYTPFTE DTETVGQRALHSILNAAIMISVIVVMTILLVVLYKYRCYKVIHAWLIISSLLLLFFFSFI YLGEVFKTYNVAVDYITVALLIWNFGVVGMISIHWKGPLRLQQAYLIMISALMALVFIKY LPEWTAWLILAVISVYDLVAVLCPKGPLRMLVETAQERNETLFPALIYSSTMVWLVNMAE GDPEAQRRVSKNSKYNAESTERESQDTVAENDDGGFSEEWEAQRDSHLGPHRSTPESRAA VQELSSSILAGEDPEERGVKLGLGDFIFYSVLVGKASATASGDWNTTIACFVAILIGLCL TLLLLAIFKKALPALPISITFGLVFYFATDYLVQPFMDQLAFHQFYI |
||||
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. |
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.