Compound E
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This article, Compound E, was written by RelentlessRecusant. Please do not edit this fiction without the writer's permission. |
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Compound E, IUPAC name (S)-2-(2-(3,5-difluorophenyl)acetamido)-N-((S)-1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)propanamide, is a small-molecule chemical inhibitor of presenilin-1 (PS1), abrogating the activity of the γ-secretase complex with an IC50 = 0.3 in βAPP-overexpressing CHO cells.[1]
The functional role of γ-secretase activity and Aβ1-42 peptide in the etiology of Alzheimer's Disease suggests Compound E as a potential potent treatment for the Alzheimer's pathology.[2]
Compound E is a benzodiazepine analog that was believed to be derived from structure-activity relationship (SAR) studies on DAPT (LY-374973), a 3,5-difluorophenylacetate-capped dipeptide ester originally synthesized and characterized by Elan Pharmaceuticals Inc. and Eli Lilly & Co.[2]
Compound E itself was originally synthesized and characterized by Seiffert et. al in 2000 by a collaboration between DuPont Pharmaceuticals Company at Wilmington, Delaware and Scios Incorporation, California.[1]
[edit] References
- ↑ 1.0 1.1 Seiffert et. al (2000). Presenilin-1 and -2 Are Molecular Targets for γ-Secretase Inhibitors. The Journal of Biological Chemistry (275): 34086–34091.
- ↑ 2.0 2.1 Harrison et. al (2004). γ-Secretase as a target for drug intervention in Alzheimer's disease. Current Opinion in Drug Discovery & Development (5): 709-719.
| Chemical Biology: Small-Molecule Control of Biological Systems (RelentlessRecusant) | ||
|---|---|---|
| | ||
| Receptor Tyrosine Kinases | A-83-01 (TGFβ/Activin) · BPIQ-II (EGFR) · Dorsomorphin/LDN-193189 (TGFβ/BMP) · SU5402 (FGFR) | |
| Signaling Kinases | A-769662 (AMPK) · BMS-354825 (BCR-ABL, Src)· BIO-Acetoxime (GSK3) · CHIR99021 (GSK3) · GO 6976 (PKC) · IMD-0354 (IκBa) · PD184352 (MAPK) · SB203580 (MAPK) · Y-27632 (ROCK) | |
| G Protein-Coupled Receptor | (+)-WIN-55212 (CB1/CB2) · ±-Sulpride (D2) · A 841720 (mGluR1) · BP-554 (5-HT1A) · Hh-Ag1.5 (Smo) · Cyclopamine/KAAD-Cyclopamine (Smo) · SANT1 (Smo) · SB-277011 (D3) | |
| Ion Channels | BAY K8644 (Cav1.2) · Bicuculline (GABAAR) · Cymarin (Na+/H+) · G-strophanthin (Na+/H+) · L-AP4 (Na+/H+) · Oxcarbazepine (Na+) · Resiniferatoxin (TRPV1) · Sarmentogenin (Na+/H+) · Theanine (AMPAR, NMDAR) | |
| Transporters | O-1783 (DAT) · WF-23 (DAT, SERT) | |
| Nuclear Receptor | All-trans retinoic acid (RAR/RXR) · GW501516 (PPARδ) · RU-486 (Nr3c1, Nr3c3) | |
| Protein Phosphatases | Endothall (PP2A) | |
| Polypharmacological | Phosphoserine (mGluR4) · PK115-584 (Tcf4/β-catenin, PKC) · Pluripotin · Reversine | |
| Other | 2C-E (DAT) · 4-methoxyphenyl-HTI-286 (α/β-tubulin) · Compound E/DAPT (presenilin-1) · D-cysteine · D-phenylalanine · Flurbiprofen (COX) · JZL184 (MAGL) · QS11 (RAFGAP1) · RO-28-1675 (glucokinase) · Robotnikinin (Shh) · Selegiline (MAOB) | |
| Uncharacterized | Neuropathiazol | |
| Libraries | Kinase Inhibitor Library | |
| Publications | ||
| Small molecule-mediated manipulation of the adult human induces selective and reversible control of physiological and psychological phenotype (Rubin et. al, 2590. Nature Medicine) | ||
| Source · Edit | ||
