Curcumin Derivatives Inhibit or Modulate Beta-Amyloid Precursor Protein Metabolism

Publisher： Karger

E-ISSN： 1660-2862|4|2-3|88-93

ISSN： 1660-2854

Source： Neurodegenerative Diseases, Vol.4, Iss.2-3, 2007-06, pp. : 88-93

Disclaimer: Any content in publications that violate the sovereignty, the constitution or regulations of the PRC is not accepted or approved by CNPIEC.

Previous Menu Next

Abstract

Curcumin-derived oxazoles and pyrazoles were synthesized in order to minimize the metal chelation properties of curcumin. The reduced rotational freedom and the absence of stereoisomers was anticipated to enhance the inhibition of γ-secretase. Accordingly, the replacement of the 1,3-dicarbonyl moiety by isosteric heterocycles turned curcumin analogue oxazoles and pyrazoles into potent γ-secretase inhibitors. Compounds 4a-i were found to be potent inhibitors of γ-secretase and displayed activity in the low micromolar range.

Related content

Destruxin E Decreases Beta-Amyloid Generation by Reducing Colocalization of Beta-Amyloid-Cleaving Enzyme 1 and Beta-Amyloid Protein Precursor

By  

Neurodegenerative Diseases, Vol. 6, Iss. 5-6, 2009-09 ,pp. : 230-239 (10)

Karger

Access to resources Recommend Favorite

Soluble Beta-Amyloid Leads to Mitochondrial Defects in Amyloid Precursor Protein and Tau Transgenic Mice

By  

Neurodegenerative Diseases, Vol. 5, Iss. 3-4, 2008-03 ,pp. : 157-159 (3)

Karger

Access to resources Recommend Favorite

Influence of Lentiviral β-Synuclein Overexpression in the Hippocampus of a Transgenic Mouse Model of Alzheimer's Disease on Amyloid Precursor Protein Metabolism and Pathology

By  

Neurodegenerative Diseases, Vol. 15, Iss. 4, 2015-06 ,pp. : 243-257 (15)

Karger

Access to resources Recommend Favorite

The Functions of Mammalian Amyloid Precursor Protein and Related Amyloid Precursor-Like Proteins

By  

Neurodegenerative Diseases, Vol. 3, Iss. 4-5, 2006-10 ,pp. : 239-246 (8)

Karger

Access to resources Recommend Favorite

Beta-amyloid peptides induces neuronal apoptosis via a mechanism independent of unfolded protein responses

By Yu Man-Shan   Suen Ka-Chun   Kwok Nga-Sze   So Kwok-Fai   Hugon Jacques   Chang Raymond  

Apoptosis, Vol. 11, Iss. 5, 2006-05 ,pp. : 687-700 (14)

Springer Publishing Company

Access to resources Recommend Favorite