Development of Dual-acting Modulators for Proteolytic Cleavage of Amyloid Precursor Proteins

CNU IR > Pharmacy and Science > 2011 Taiwanese-Russian Organic, Medicinal and Bio Chemistry Interactions & PST Medicinal Chemistry Symposium > Item 310902800/24211

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Title:	Development of Dual-acting Modulators for Proteolytic Cleavage of Amyloid Precursor Proteins
Authors:	Ming-Kuan Hu (胡明寬)
Date:	2011
Issue Date:	2011-06-23 14:57:05 (UTC+8)
Abstract:	One of the pathological hallmarks of Alzheimer's disease (AD) is the cerebral accumulation of amyloid plaques, and the major constituents of these plaques are the 40—42 residue amyloid-β peptides (Aβs), to which the amount of generation was dependent on the proteolytic processing of amyloid precursor proteins (APPs) sequentially by the β- and γ-secretases. An alternative processing of APP by α-secretase could be regulated via activation of mitogen-activated protein kinase (MAPK) pathway and considered to be beneficial, because this process generates neuroprotective secretory amyloid precursor protein (sAPP) and thus precludes the production of amyloidogenic Aβs and reduces the risk of AD. On the basis of these investigations, strategies to the development of single chemical entities to modulate multiple targets were suitably applied to the therapeutic approaches for AD. Here, efforts to identify dual-acting molecules and the screeniig for selectivity against γ-secretase and simultaneously modulation of MAPK pathway of these compounds are presented.
Relation:	2011年台俄有機、藥物與生物化學交流暨藥物化學研討會，起迄日：2011/04/06~2011/04/05，地點：溪頭台大實驗林
Appears in Collections:	[Pharmacy and Science] 2011 Taiwanese-Russian Organic, Medicinal and Bio Chemistry Interactions & PST Medicinal Chemistry Symposium

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