Cholinesterase as a target for drug development in alzheimer’s disease

  • Piyoosh Sharma
  • , Manish Kumar Tripathi
  • , Sushant Kumar Shrivastava

Research output: Chapter in Book/Report/Conference proceedingChapterpeer-review

Abstract

Alzheimer’s disease (AD) is an enormous healthcare challenge, and 50 million people are currently suffering from it. There are several pathophysiological mechanisms involved, but cholinesterase inhibitors remained the major target from the last 2–3 decades. Among four available therapeutics (donepezil, rivastigmine, galantamine, and memantine), three of them are cholinesterase inhibitors. Herein, we describe the role of acetylcholine sterase (AChE) and related hypothesis in AD along with the pharmacological and chemical aspects of the available cholinesterase inhibitors. This chapter discusses the development of several congeners and hybrids of available cholinesterase inhibitors along with their binding patterns in enzyme active sites.

Original languageEnglish
Title of host publicationMethods in Molecular Biology
PublisherHumana Press Inc.
Pages257-286
Number of pages30
DOIs
StatePublished - 2020

Publication series

NameMethods in Molecular Biology
Volume2089
ISSN (Print)1064-3745
ISSN (Electronic)1940-6029

Keywords

  • Acetylcholine
  • Acetylcholinesterase
  • Acyl binding pocket
  • Amyloid beta
  • Anionic subsite
  • Butyrylcholine
  • Butyrylcholinesterase
  • Catalytic active site
  • Choline acetyltransferase
  • Donepezil
  • Galantamine
  • N-Benzylpiperidine
  • Oxyanion hole
  • Peripheral anionic site
  • Rivastigmine
  • Tacrine

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