Display options
Cite
Tong F, Islam RM, Carlier PR, et al. Effects of Anticholinesterases on Catalysis and Induced Conformational Change of the Peripheral Anionic Site of Murine Acetylcholinesterase. Pestic Biochem Physiol. 2013;106(3):79-84doi: 10.1016/j.pestbp.2013.04.001.
Tong, F., Islam, R. M., Carlier, P. R., Ma, M., Ekström, F., & Bloomquist, J. R. (2013). Effects of Anticholinesterases on Catalysis and Induced Conformational Change of the Peripheral Anionic Site of Murine Acetylcholinesterase. Pesticide biochemistry and physiology, 106(3), 79-84. https://doi.org/10.1016/j.pestbp.2013.04.001
Tong, Fan, et al. "Effects of Anticholinesterases on Catalysis and Induced Conformational Change of the Peripheral Anionic Site of Murine Acetylcholinesterase." Pesticide biochemistry and physiology vol. 106,3 (2013): 79-84. doi: https://doi.org/10.1016/j.pestbp.2013.04.001
Tong F, Islam RM, Carlier PR, Ma M, Ekström F, Bloomquist JR. Effects of Anticholinesterases on Catalysis and Induced Conformational Change of the Peripheral Anionic Site of Murine Acetylcholinesterase. Pestic Biochem Physiol. 2013 Jul 01;106(3):79-84. doi: 10.1016/j.pestbp.2013.04.001. PMID: 24003261; PMCID: PMC3758491.
Copy Download .nbib Format: NLM
Share it on

Pestic Biochem Physiol. 2013 Jul 01;106(3):79-84. doi: 10.1016/j.pestbp.2013.04.001.

Effects of Anticholinesterases on Catalysis and Induced Conformational Change of the Peripheral Anionic Site of Murine Acetylcholinesterase.

Pesticide biochemistry and physiology

Fan Tong, Rafique M Islam, Paul R Carlier, Ming Ma, Fredrik Ekström, Jeffrey R Bloomquist

Affiliations

  1. Department of Entomology and Nematology, Emerging Pathogens Institute, University of Florida, Gainesville, FL 32611.

PMID: 24003261 PMCID: PMC3758491 DOI: 10.1016/j.pestbp.2013.04.001

Abstract

Conventional insecticides targeting acetylcholinesterase (AChE) typically show high mammalian toxicities and because there is resistance to these compounds in many insect species, alternatives to established AChE inhibitors used for pest control are needed. Here we used a fluorescence method to monitor interactions between various AChE inhibitors and the AChE peripheral anionic site, which is a novel target for new insecticides acting on this enzyme. The assay uses thioflavin-T as a probe, which binds to the peripheral anionic site of AChE and yields an increase in fluorescent signal. Three types of AChE inhibitors were studied: catalytic site inhibitors (carbamate insecticides, edrophonium, and benzylpiperidine), peripheral site inhibitors (tubocurarine, ethidium bromide, and propidium iodide), and bivalent inhibitors (donepezil, BW284C51, and a series of

Keywords: carbamate; catalytic site; donepezil; edrophonium; ethidium; fluorescence; propidium; tacrine; tacrine dimer; thioflavin-T

References

  1. J Med Chem. 2006 Sep 7;49(18):5491-500 - PubMed
  2. Trans R Soc Trop Med Hyg. 2008 Jun;102(6):591-8 - PubMed
  3. Am J Med. 1971 Apr;50(4):475-92 - PubMed
  4. Adv Enzymol Relat Areas Mol Biol. 1975;43:103-218 - PubMed
  5. Pediatrics. 1988 Jan;81(1):121-6 - PubMed
  6. EMBO J. 2003 Jan 2;22(1):1-12 - PubMed
  7. J Biol Chem. 1999 Jan 29;274(5):2963-70 - PubMed
  8. Environ Health Perspect. 1987 Jun;72:267-81 - PubMed
  9. Environ Health Perspect. 1990 Jul;87:245-54 - PubMed
  10. J Histochem Cytochem. 1981 Apr;29(4):572-6 - PubMed
  11. Bioorg Med Chem Lett. 2012 Jul 15;22(14):4593-8 - PubMed
  12. Bioorg Med Chem. 1999 Feb;7(2):351-7 - PubMed
  13. Biochemistry. 1981 Aug 4;20(16):4803-10 - PubMed
  14. Proc Natl Acad Sci U S A. 1993 Oct 1;90(19):9031-5 - PubMed
  15. Science. 1991 Aug 23;253(5022):872-9 - PubMed
  16. Biochem Pharmacol. 1961 Jul;7:88-95 - PubMed
  17. Biochemistry. 1998 Mar 24;37(12):4206-16 - PubMed
  18. Biochemistry. 2006 Jan 10;45(1):74-81 - PubMed
  19. Structure. 1999 Mar 15;7(3):297-307 - PubMed
  20. J Phys Chem A. 2007 Jun 7;111(22):4829-35 - PubMed
  21. Mol Biol Rep. 1979 Dec 31;5(4):209-14 - PubMed
  22. J Am Chem Soc. 2008 Jun 25;130(25):7856-61 - PubMed
  23. Biochemistry. 1975 May 6;14(9):1989-97 - PubMed
  24. Toxicol Appl Pharmacol. 2008 Aug 1;230(3):390-6 - PubMed
  25. J Biol Chem. 2001 Jun 29;276(26):23282-7 - PubMed
  26. Mol Pharmacol. 1994 Feb;45(2):335-40 - PubMed

Publication Types

Grant support