Determination of affinity and efficacy of acetylcholinesterase inhibitors using isothermal titration calorimetry

• Published in: Biochimica et biophysica acta Vol. 1860; no. 5; pp. 967 - 974
• Main Authors: Draczkowski, Piotr, Tomaszuk, Anna, Halczuk, Pawel, Strzemski, Maciej, Matosiuk, Dariusz, Jozwiak, Krzysztof
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 01.05.2016
• Subjects: acetylcholine; Acetylcholine - chemistry; Acetylcholinesterase; Acetylcholinesterase - chemistry; Alzheimer disease; Ambenonium Chloride - chemistry; Animals; calorimetry; Calorimetry - methods; Cholinesterase Inhibitors - chemistry; Edrophonium - chemistry; Electrophorus - metabolism; Electrophorus electricus; enthalpy; Enzyme activity assay; Fish Proteins - antagonists & inhibitors; Fish Proteins - chemistry; Galantamine - chemistry; Indans - chemistry; Inhibitor; inhibitory concentration 50; Interactions; Isothermal titration calorimetry; ITC; Kinetics; memory; nerve tissue; neurons; Piperidines - chemistry; synapse; Tacrine - chemistry; Thermodynamics; titration; ITC; Inhibitor; Isothermal titration calorimetry; Interactions; Acetylcholinesterase; Enzyme activity assay

Acetylcholinesterase (AChE), an enzyme rapidly terminating nerve signals at synapses of cholinergic neurons is an important drug target in treatment of Alzheimer's disease and related memory loss conditions. Here we present comprehensive use of isothermal titration calorimetry (ITC) for investi...