On the active site for hydrolysis of aryl amides and choline esters by human cholinesterases

Bioorganic & Medicinal Chemistry
Sultan DarveshEarl Martin

Abstract

Cholinesterases, in addition to their well-known esterase action, also show an aryl acylamidase (AAA) activity whereby they catalyze the hydrolysis of amides of certain aromatic amines. The biological function of this catalysis is not known. Furthermore, it is not known whether the esterase catalytic site is involved in the AAA activity of cholinesterases. It has been speculated that the AAA activity, especially that of butyrylcholinesterase (BuChE), may be important in the development of the nervous system and in pathological processes such as formation of neuritic plaques in Alzheimer's disease (AD). The substrate generally used to study the AAA activity of cholinesterases is N-(2-nitrophenyl)acetamide. However, use of this substrate requires high concentrations of enzyme and substrate, and prolonged periods of incubation at elevated temperature. As a consequence, difficulties in performing kinetic analysis of AAA activity associated with cholinesterases have hampered understanding this activity. Because of its potential biological importance, we sought to develop a more efficient and specific substrate for use in studying the AAA activity associated with BuChE, and for exploring the catalytic site for this hydrolysis. Here, ...Continue Reading

References

Jun 10, 2003·Alzheimer Disease and Associated Disorders·Sultan DarveshEarl Martin
Jul 19, 2003·The Journal of Biological Chemistry·Yvain NicoletFlorian Nachon
Jul 17, 2004·Endocrinology·Carine De VrieseChristine Delporte

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Citations

Jan 23, 2008·Biological Chemistry·María F MontenegroCecilio J Vidal
Apr 29, 2014·European Journal of Medicinal Chemistry·Xiao LiXinyong Liu
Oct 24, 2009·Journal of Pharmaceutical and Biomedical Analysis·Matthias KoitkaHans-Hubert Borchert
Aug 11, 2007·Biochimica Et Biophysica Acta·Patrick MassonLawrence M Schopfer
May 8, 2007·International Journal of Developmental Neuroscience : the Official Journal of the International Society for Developmental Neuroscience·Emilene B S SchererAngela T S Wyse
Feb 4, 2010·Chemico-biological Interactions·Sultan DarveshJohn D Fisk
Jan 12, 2012·Journal of Enzyme Inhibition and Medicinal Chemistry·Ian R MacdonaldSultan Darvesh
Dec 1, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Sizhe LiLaurent Soulère
Dec 1, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Terrone L RosenberryFlorian Nachon
Sep 19, 2015·Journal of Labelled Compounds & Radiopharmaceuticals·Scott R Pollack, David J Schenk
Sep 13, 2007·Journal of Enzyme Inhibition and Medicinal Chemistry·Patrick MassonOksana Lockridge
Jun 28, 2019·Chemico-biological Interactions·Aliya R MukhametgalievaPatrick Masson
Aug 21, 2012·Biochemistry·Ian R MacdonaldSultan Darvesh

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