Download Chemical Modulators of Protein Misfolding and by Pierfausto Seneci PDF

By Pierfausto Seneci

This publication is a neurochemistry-based spouse for Protein Misfolding and Neurodegenerative illnesses: Molecular Targets, an Elsevier identify through an identical writer publishing in December 2014. whereas the 1st ebook specializes in biology and molecular ambitions, this better half publication describes how those ambitions are regulated by means of small molecules and disease-modifying compounds. The publication starts off with a short creation to how key proteins turn into dysfunctional, and every next bankruptcy describes significant disorder mechanisms in Alzheimer’s and different tauopathies. homes and improvement prestige of those molecular goals and illness mechanisms are completely defined, as are small molecule effectors of autophagy and dis-aggregating brokers.

• Written to supply accomplished insurance of neurodegenerative disease-modifying compounds;
• offers discipline-specific chapters that conceal medicinal chemistry and scientific applications;
• offers an outline of greater than 2 hundred chemical sessions and lead compounds, performing on chosen molecular objectives which are of relevance to any neurodegenerative disorder;
• insurance of misfolding ailments, chaperone proteins, ubiquitination and autophagy/oncology makes this ebook compatible for structural neurochemists, chemists, biologists, non-CNS scientists, and scientists drawn to drug discovery.

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Br. J. Pharmacol. 2009, 156, 982–993. , et al. The gamma-secretase modulator CHF5074 reduces the accumulation of native hyperphosphorylated tau in a transgenic mouse model of Alzheimer’s disease. J. Mol. Neurosci. 2011, 45, 22–31. ; Martino, P. , et al. Therapeutic effect of CHF5074, a new g-secretase modulator, in a mouse model of scrapie. Prion. 2012, 6, 62–72. ; Viscomi, A. , et al. Pharmacological targeting of the b-amyloid precursor protein intracellular domain. Sci. Rep. 2014, 4, 4618. [93] Konietzko, U.

CHF5074, a novel gamma secretase modulator, restores hippocampal neurogenesis potential and reverses contextual memory deficit in a transgenic mouse model of Alzheimer’s disease. J. Alzheimer’s Dis. 2010, 20, 159–173. ; Baldassarro, V. , et al. Multi-target action of the novel anti-Alzheimer compound CHF5074: in vivo study of long term treatment in Tg2576 mice. BMC Neurosci. 2013, 14, 44. [88] Imbimbo, B. , et al. 1-(39,49-Dichloro-2-fluoro[1,19-biphenyl]-4-yl)-cyclopropanecarboxylic acid (CHF5074), a novel gamma-secretase modulator, reduces brain beta-amyloid pathology in a transgenic mouse model of Alzheimer’s disease without causing peripheral toxicity.

The many substrates of presenilin/gamma-secretase. J. Alzheimer’s Dis. 2011, 25, 3–28. ; Funamoto, S. g-Secretase-dependent proteolysis of transmembrane domain of amyloid precursor protein: successive tri- and tetrapeptide release in amyloid b-protein production. Int. J. Alzheimer’s Dis. 2012, 2012 591392. [67] Selkoe, D. J. Alzheimer’s disease: genes, proteins, and therapy. Physiol. Rev. 2001, 81, 741–766. [68] Golde, T. ; Koo, E. ; Felsenstein, K. ; Osborne, B. ; Miele, L. g-Secretase inhibitors and modulators.

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