Title : Highlights of ASS234: a novel and promising therapeutic agent for Alzheimer's disease therapy - Romero_2020_Neural.Regen.Res_15_30
Author(s) : Romero A , Marco-Contelles J , Ramos E
Ref : Neural Regen Res , 15 :30 , 2020
Abstract :

There is no effective treatment to face Alzheimer's disease complexity. Multitarget molecules are a good approach against the multiple physiopathological events associated with its development and progression. In this context, N-((5-(3-(1-benzylpiperidin-4-yl) propoxy)-1- methyl-1H-indol-2-yl)methyl)-N-methylprop-2-yn-1-amine (ASS234) has been tested achieving promising results. ASS234 has demonstrated to cross the blood-brain barrier in vivo, and a good in silico safety profile being less toxic than donepezil. Besides, ASS234 reversibly inhibits human acetyl- and butyryl-cholinesterase, and irreversibly inhibits human monoamine oxidase A and B. Moreover, this multitarget molecule has antioxidant and neuroprotective properties, and inhibits Alphabeta1-42 and Alphabeta1-40 self-aggregation. Inquiring about the mechanism of action, several signaling pathways related to Alzheimer's disease had been explored showing that ASS234 induces the wingless-type MMTV integration site (Wnt) family and several members of the heat shock proteins family and moreover counteracts neuroinflammatory and oxidative stress-related genes promoting the induction of several key antioxidant genes. Finally, in vivo experiments with ASS234 in C57BL/6J mice displayed its ability to reduce amyloid plaque burden and gliosis in the cortex and hippocampus, ameliorating scopolamine-induced learning deficits. Here we gather the information regarding ASS234 evaluated so far, showing its ability to face different targets, necessary to counteract a neurodegenerative disease as complex as the Alzheimer's disease.

PubMedSearch : Romero_2020_Neural.Regen.Res_15_30
PubMedID: 31535639

Related information

Inhibitor ASS234

Citations formats

Romero A, Marco-Contelles J, Ramos E (2020)
Highlights of ASS234: a novel and promising therapeutic agent for Alzheimer's disease therapy
Neural Regen Res 15 :30

Romero A, Marco-Contelles J, Ramos E (2020)
Neural Regen Res 15 :30