ACS chemical neuroscience molecule spotlight on BMS-708163

ACS Chemical Neuroscience

Volumn 3, Issue 3, 2012, Pages 149-150

  Hopkins, Corey R ^a  

^a VANDERBILT UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

Alzheimer's disease; amyloid hypothesis; gamma secretase inhibitors; GSI

Indexed keywords

AVAGACESTAT; BETA SECRETASE; GAMMA SECRETASE; PLACEBO;

ALZHEIMER DISEASE; DOUBLE BLIND PROCEDURE; DRUG WITHDRAWAL; ENZYME INHIBITION; GASTROINTESTINAL SYMPTOM; HIGH THROUGHPUT SCREENING; HUMAN; NEUROSCIENCE; NONHUMAN; PHASE 2 CLINICAL TRIAL; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL (TOPIC); REVIEW; SKIN DISEASE;

ALZHEIMER'S DISEASE; AMYLOID HYPOTHESIS; GAMMA-SECRETASE INHIBITORS; GSI;

ALZHEIMER DISEASE; AMYLOID PRECURSOR PROTEIN SECRETASES; ANIMALS; CLINICAL TRIALS, PHASE II AS TOPIC; DRUG DISCOVERY; HUMANS; NEUROSCIENCES; OXADIAZOLES; SOCIETIES, SCIENTIFIC; SULFONAMIDES;

EID: 84858760430     PISSN: None     EISSN: 19487193     Source Type: Journal    
DOI: 10.1021/cn3000179     Document Type: Review

References (12)

1. Hopkins, C. R. (2010) ACS Chemical Neuroscience Molecule Spotlight on Semagacestat (LY450139) ACS Chem. Neurosci. 1 (8) 533-534
2. Hopkins, C. R. (2011) ACS Chemical Neuroscience Molecule Spotlight on ELND006: Another γ-Secretase Inhibitor Fails in the Clinic ACS Chem. Neurosci. 2 (6) 279-280
3. Hopkins, C. R. (2012) ACS Chemical Neuroscience Molecule Spotlight on Begacestat (GSI-953) ACS Chem. Neurosci. 3 (1) 3-4
4. Imbimbo, B. P. (2008) Alzheimer's disease: γ-secretase inhibitors Drug Discovery Today 5 (3) 169-175
5. Jakob-Roetne, R. and Jacobsen, H. (2009) Alzheimer's disease: from pathology to therapeutic approaches Ang. Chem., Int. Ed. 48, 3030-3059
6. Hardy, J. and Selkoe, D. J. (2002) The amyloid hypothesis of Alzheimer's disease: progress and problems on the road to therapeutics Science 297, 353-356 (Pubitemid 34790756)
7. Hardy, J. A. and Higgins, G. A. (1992) Alzheimer's disease: the amyloid cascade hypothesis Science 256, 184-185
8. Selkoe, D. J. (1991) The molecular pathology of Alzheimer's disease Neuron 6, 487-498
9. Vassar, R., Bennett, B. D., Babu-Khan, S., Kahn, S., Mendiaz, E. A., Denis, P., Teplow, D. B., Ross, S., Amarante, P., Loeloff, R., Luo, Y., Fisher, S., Fuller, J., Edenson, S., Lile, J., Jarosinski, M. A., Biere, A. L., Curran, E., Burgess, T., Louis, J.-C., Collins, F., Treanor, J., Rogers, G., and Citron, M. (1999) β-Secretase cleavage of Alzheimer's amyloid precursor protein by the transmembrane aspartic protease BACE Science 286 (5440) 735-741
10. http://www.merck.com/newsroom/news-release-archive/research-and- development/2011-1110.html.
11. Gillman, K. W., Starrett, J. E., Jr., Parker, M. F., Xie, K., Bronson, J. J., Marcin, L. R., McElhone, K. E., Bergstrom, C. P., Mate, R. A., Williams, R., Meredith, J. E., Jr., Burton, C. R., Barten, D. M., Toyn, J. H., Roberts, S. B., Lentz, K. A., Houston, J. G., Zaczek, R., Albright, C. F., Decicco, C. P., Macor, J. E., and Olson, R. E. (2010) Discovery and Evaluation of BMS-708163, a Potent, Selective and Orally Bioavailable γ-Secretase Inhibitor ACS Med. Chem. Lett. 1, 120-124
12. http://www.bms.com/news/press-releases/pages/default.aspx.