• Publications
  • Influence
An inhibitor of casein kinase I epsilon induces phase delays in circadian rhythms under free-running and entrained conditions.
Casein kinase Iepsilon (CKIepsilon) is an essential component of the biological clock, phosphorylating PER proteins, and in doing so regulating their turnover and nuclear entry in oscillator cells ofExpand
  • 76
  • 18
An Inhibitor of Casein Kinase Iϵ Induces Phase Delays in Circadian Rhythms under Free-Running and Entrained Conditions
Casein kinase Iϵ (CKIϵ) is an essential component of the biological clock, phosphorylating PER proteins, and in doing so regulating their turnover and nuclear entry in oscillator cells of theExpand
  • 99
  • 12
Concentration-Dependent Modulation of Amyloid-β in Vivo and in Vitro Using the γ-Secretase Inhibitor, LY-450139
LY-450139 is a γ-secretase inhibitor shown to have efficacy in multiple cellular and animal models. Paradoxically, robust elevations of plasma amyloid-β (Aβ) have been reported in dogs and humansExpand
  • 124
  • 5
Concentration-dependent modulation of amyloid-beta in vivo and in vitro using the gamma-secretase inhibitor, LY-450139.
LY-450139 is a gamma-secretase inhibitor shown to have efficacy in multiple cellular and animal models. Paradoxically, robust elevations of plasma amyloid-beta (Abeta) have been reported in dogs andExpand
  • 57
  • 5
Pharmacodynamics and Pharmacokinetics of the γ-Secretase Inhibitor PF-3084014
  • T. Lanz, K. Wood, +16 authors B. Tate
  • Chemistry, Medicine
  • Journal of Pharmacology and Experimental…
  • 1 July 2010
PF-3084014 [(S)-2-((S)-5,7-difluoro-1,2,3,4-tetrahydronaphthalen-3-ylamino)-N-(1-(2-methyl-1-(neopentylamino)propan-2-yl)-1H-imidazol-4-yl)pentanamide] is a novel γ-secretase inhibitor that reducesExpand
  • 49
  • 2
Optimization of a natural product-based class of γ-secretase modulators.
A series of triterpene-based γ-secretase modulators is optimized. An acetate present at the C24 position of the natural product was replaced with either carbamates or ethers to provide compounds withExpand
  • 40
  • 2
Efficacy of SPI-1865, a novel gamma-secretase modulator, in multiple rodent models
IntroductionModulation of the gamma-secretase enzyme, which reduces the production of the amyloidogenic Aβ42 peptide while sparing the production of other Aβ species, is a promising therapeuticExpand
  • 25
  • 1
Modulation of Gamma-Secretase for the Treatment of Alzheimer's Disease
The Amyloid Hypothesis states that the cascade of events associated with Alzheimer's disease (AD)—formation of amyloid plaques, neurofibrillary tangles, synaptic loss, neurodegeneration, andExpand
  • 22
  • 1
  • PDF
Chronic treatment with a selective inhibitor of casein kinase I δ/ε yields cumulative phase delays in circadian rhythms
IntroductionCasein kinase I ε/δ phosphorylates certain clock-related proteins as part of a complex arrangement of transcriptional/translational feedback loops that comprise the circadian oscillatorExpand
  • 23
  • 1
Initial Optimization of a New Series of γ-Secretase Modulators Derived from a Triterpene Glycoside.
The discovery of a new series of γ-secretase modulators is disclosed. Starting from a triterpene glycoside γ-secretase modulator that gave a very low brain-to-plasma ratio, initial SAR andExpand
  • 21
  • 1