Matthew E Kennedy
Affiliation: Schering-Plough Research Institute
- Measuring human beta-secretase (BACE1) activity using homogeneous time-resolved fluorescenceMatthew E Kennedy
CNS Cardiovascular Research, Schering Plough Research Institute, Kenilworth, NJ 07033, USA
Anal Biochem 319:49-55. 2003....
- Application of fragment-based NMR screening, X-ray crystallography, structure-based design, and focused chemical library design to identify novel microM leads for the development of nM BACE-1 (beta-site APP cleaving enzyme 1) inhibitorsYu Sen Wang
Schering Plough Research Institute, 320 Bent Street, Cambridge, Massachusetts 02141, USA
J Med Chem 53:942-50. 2010..The structure-based design of a cyclic acylguanidine lead series and its optimization into nanomolar BACE-1 inhibitors are the subject of the companion paper..
- Structure based design of iminohydantoin BACE1 inhibitors: identification of an orally available, centrally active BACE1 inhibitorJared N Cumming
Merck Research Laboratories, 2000 Galloping Hill Road, Kenilworth, NJ 07033, USA
Bioorg Med Chem Lett 22:2444-9. 2012..Herein we report SAR development in the S3 and F' subsites of BACE1 for this series, the synthetic approaches employed in this effort, and in vivo data for the optimized compound...
- The BACE1 inhibitor verubecestat (MK-8931) reduces CNS β-amyloid in animal models and in Alzheimer's disease patientsMatthew E Kennedy
Department of Neuroscience, Merck Research Laboratories, Kenilworth, NJ 07033, USA
Sci Transl Med 8:363ra150. 2016..The human data were fit to an amyloid pathway model that provided insight into the Aβ pools affected by BACE1 inhibition and guided the choice of doses for subsequent clinical trials...
- Design and development of BACE-1 inhibitorsJared N Cumming
Department of Chemical Research, Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA
Curr Opin Drug Discov Devel 7:536-56. 2004..This review provides a perspective on the recent developments in the design of BACE-1 inhibitors. An overview of early research is also included, with particular emphasis on a comprehensive survey of the patent literature...
- Discovery of cyclic acylguanidines as highly potent and selective beta-site amyloid cleaving enzyme (BACE) inhibitors: Part I--inhibitor design and validationZhaoning Zhu
Department of Medicinal Chemistry, Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, USA
J Med Chem 53:951-65. 2010....