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Acetylcholinesterase: A Versatile Template to Coin Potent Modulators of Multiple Therapeutic Targets.


ABSTRACT: ConspectusThe enzyme acetylcholinesterase (AChE) hydrolyzes the neurotransmitter acetylcholine (ACh) at cholinergic synapses of the peripheral and central nervous system. Thus, it is a prime therapeutic target for diseases that occur with a cholinergic deficit, prominently Alzheimer's disease (AD). Working at a rate near the diffusion limit, it is considered one of nature's most efficient enzymes. This is particularly meritorious considering that its catalytic site is buried at the bottom of a 20-Å-deep cavity, which is preceded by a bottleneck with a diameter shorter than that of the trimethylammonium group of ACh, which has to transit through it. Not only the particular architecture and amino acid composition of its active site gorge enable AChE to largely overcome this potential drawbac

SUBMITTER: Luque FJ 

PROVIDER: S-EPMC10882973 | biostudies-literature | 2024 Feb

REPOSITORIES: biostudies-literature