Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T99204
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| Former ID |
TTDR00445
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| Target Name |
Presenilin 2
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| Gene Name |
PSEN2
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| Synonyms |
AD3LP; AD5; E5-1; PS-2; PS2; STM-2; PSEN2
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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. May function in the cytoplasmic partitioning of proteins.
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| BioChemical Class |
Peptidase
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| Target Validation |
T99204
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| UniProt ID | |||||
| EC Number |
EC 3.4.23.-
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| Sequence |
MLTFMASDSEEEVCDERTSLMSAESPTPRSCQEGRQGPEDGENTAQWRSQENEEDGEEDP
DRYVCSGVPGRPPGLEEELTLKYGAKHVIMLFVPVTLCMIVVVATIKSVRFYTEKNGQLI YTPFTEDTPSVGQRLLNSVLNTLIMISVIVVMTIFLVVLYKYRCYKFIHGWLIMSSLMLL FLFTYIYLGEVLKTYNVAMDYPTLLLTVWNFGAVGMVCIHWKGPLVLQQAYLIMISALMA LVFIKYLPEWSAWVILGAISVYDLVAVLCPKGPLRMLVETAQERNEPIFPALIYSSAMVW TVGMAKLDPSSQGALQLPYDPEMEEDSYDSFGEPSYPEVFEPPLTGYPGEELEEEEERGV KLGLGDFIFYSVLVGKAAATGSGDWNTTLACFVAILIGLCLTLLLLAVFKKALPALPISI TFGLIFYFSTDNLVRPFMDTLASHQLYI |
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| Drugs and Mode of Action | |||||
| Drug(s) | R-flurbiprofen | Drug Info | Phase 2 | Discovery agent | [1], [2] |
| Inhibitor | (2S,3R)-2-(benzyloxy)-3-methoxycyclohexanone | Drug Info | [3] | ||
| (5R,6S)-5,6-bis(benzyloxy)cyclohex-2-enone | Drug Info | [3] | |||
| (5R,6S)-6-(benzyloxy)-5-methoxycyclohex-2-enone | Drug Info | [3] | |||
| (S)-FLURBIPROFEN | Drug Info | [4] | |||
| 1-benzoyl-2-benzyl-1,2-dihydropyridin-3(6H)-one | Drug Info | [3] | |||
| 1-Chloro-4-(1-phenyl-cyclohexanesulfonyl)-benzene | Drug Info | [5] | |||
| Drug 311383 | Drug Info | [6] | |||
| Drug 311440 | Drug Info | [6] | |||
| Drug 311951 | Drug Info | [6] | |||
| Drug 311952 | Drug Info | [6] | |||
| R-flurbiprofen | Drug Info | [4] | |||
| Pathways | |||||
| KEGG Pathway | Notch signaling pathway | ||||
| Neurotrophin signaling pathway | |||||
| Alzheimer' | |||||
| s disease | |||||
| PANTHER Pathway | Alzheimer disease-amyloid secretase pathway | ||||
| Alzheimer disease-presenilin pathway | |||||
| Notch signaling pathway | |||||
| Pathway Interaction Database | LKB1 signaling events | ||||
| Reactome | Nuclear signaling by ERBB4 | ||||
| Regulated proteolysis of p75NTR | |||||
| NRIF signals cell death from the nucleus | |||||
| Activated NOTCH1 Transmits Signal to the Nucleus | |||||
| Constitutive Signaling by NOTCH1 PEST Domain Mutants | |||||
| Constitutive Signaling by NOTCH1 HD+PEST Domain Mutants | |||||
| NOTCH2 Activation and Transmission of Signal to the Nucleus | |||||
| EPH-ephrin mediated repulsion of cells | |||||
| WikiPathways | Notch Signaling Pathway | ||||
| Signaling by ERBB4 | |||||
| Signaling by NOTCH3 | |||||
| Signaling by NOTCH4 | |||||
| Signaling by NOTCH1 | |||||
| Signaling by NOTCH2 | |||||
| Notch Signaling Pathway | |||||
| Alzheimers Disease | |||||
| Signalling by NGF | |||||
| References | |||||
| REF 1 | ClinicalTrials.gov (NCT00045123) R-Flurbiprofen in Treating Patients With Localized Prostate Cancer at Risk of Recurrence. U.S. National Institutes of Health. | ||||
| REF 2 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7340). | ||||
| REF 3 | Bioorg Med Chem Lett. 2006 Jul 15;16(14):3813-6. Epub 2006 May 8.Novel gamma-secretase inhibitors discovered by library screening of in-house synthetic natural product intermediates. | ||||
| REF 4 | Bioorg Med Chem Lett. 2006 Apr 15;16(8):2219-23. Epub 2006 Feb 7.The geminal dimethyl analogue of Flurbiprofen as a novel Abeta42 inhibitor and potential Alzheimer's disease modifying agent. | ||||
| REF 5 | Bioorg Med Chem Lett. 2005 May 16;15(10):2685-8.Aryl sulfones: a new class of gamma-secretase inhibitors. | ||||
| REF 6 | J Med Chem. 2004 Jul 29;47(16):3931-3.Discovery of a Subnanomolar helical D-tridecapeptide inhibitor of gamma-secretase. | ||||
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