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Current Topics in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

γ-Secretase Modulation and its Promise for Alzheimers Disease: a Medicinal Chemistry Perspective

Author(s): Ilaria Peretto and Elena La Porta

Volume 8, Issue 1, 2008

Page: [38 - 46] Pages: 9

DOI: 10.2174/156802608783334097

Price: $65

Abstract

γ-Secretase modulation holds the promise for the development of a disease-modifying therapy for Alzheimers disease (AD). This novel concept of manipulating the cleavage specificity of the γ-secretase enzyme by pharmacological means implies that steady state levels of the potentially disease-causing amyloid-β(1-42) peptide can be lowered without the undesired side effects associated with full inhibition of this aspartyl-type protease. Following on from the initial discovery that certain non-steroidal anti-inflammatory drugs (NSAIDs) exhibit properties characteristic of γ-secretase modulators, this class of compounds has been extensively studied and exploited, leading to the discovery of NSAIDs derivatives endowed with improved potency for the reduction of amyloid-β(1-42) peptide production. In addition, a very limited number of non-NSAID derived γ-secretase modulators has also been recently claimed in the patent literature, suggesting that only a restricted number of pharmacophores might be involved in the modulation of γ-secretase.


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