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Molecular Pharmacology

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Research ArticleArticle

Synthesis of Selective Agonists for the α7 Nicotinic Acetylcholine Receptor with In Situ Click-Chemistry on Acetylcholine-Binding Protein Templates

John G. Yamauchi, Kimberly Gomez, Neil Grimster, Mikael Dufouil, Ákos Nemecz, Joseph R. Fotsing, Kwok-Yiu Ho, Todd T. Talley, K. Barry Sharpless, Valery V. Fokin and Palmer Taylor
Molecular Pharmacology October 2012, 82 (4) 687-699; DOI: https://doi.org/10.1124/mol.112.080291
John G. Yamauchi
Department of Pharmacology, Skaggs School of Pharmacy and Pharmaceutical Sciences (J.G.Y., K.G., M.D., Á.N., K.H., T.T.T., P.T.), and Department of Chemistry and Biochemistry, Division of Physical Sciences (Á.N.), University of California, San Diego, La Jolla, California; and Skaggs Institute for Chemical Biology, Scripps Research Institute, La Jolla, California (N.G., M.D., J.R.F., K.B.S., V.V.F.)
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Kimberly Gomez
Department of Pharmacology, Skaggs School of Pharmacy and Pharmaceutical Sciences (J.G.Y., K.G., M.D., Á.N., K.H., T.T.T., P.T.), and Department of Chemistry and Biochemistry, Division of Physical Sciences (Á.N.), University of California, San Diego, La Jolla, California; and Skaggs Institute for Chemical Biology, Scripps Research Institute, La Jolla, California (N.G., M.D., J.R.F., K.B.S., V.V.F.)
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Neil Grimster
Department of Pharmacology, Skaggs School of Pharmacy and Pharmaceutical Sciences (J.G.Y., K.G., M.D., Á.N., K.H., T.T.T., P.T.), and Department of Chemistry and Biochemistry, Division of Physical Sciences (Á.N.), University of California, San Diego, La Jolla, California; and Skaggs Institute for Chemical Biology, Scripps Research Institute, La Jolla, California (N.G., M.D., J.R.F., K.B.S., V.V.F.)
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Mikael Dufouil
Department of Pharmacology, Skaggs School of Pharmacy and Pharmaceutical Sciences (J.G.Y., K.G., M.D., Á.N., K.H., T.T.T., P.T.), and Department of Chemistry and Biochemistry, Division of Physical Sciences (Á.N.), University of California, San Diego, La Jolla, California; and Skaggs Institute for Chemical Biology, Scripps Research Institute, La Jolla, California (N.G., M.D., J.R.F., K.B.S., V.V.F.)
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Ákos Nemecz
Department of Pharmacology, Skaggs School of Pharmacy and Pharmaceutical Sciences (J.G.Y., K.G., M.D., Á.N., K.H., T.T.T., P.T.), and Department of Chemistry and Biochemistry, Division of Physical Sciences (Á.N.), University of California, San Diego, La Jolla, California; and Skaggs Institute for Chemical Biology, Scripps Research Institute, La Jolla, California (N.G., M.D., J.R.F., K.B.S., V.V.F.)
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Joseph R. Fotsing
Department of Pharmacology, Skaggs School of Pharmacy and Pharmaceutical Sciences (J.G.Y., K.G., M.D., Á.N., K.H., T.T.T., P.T.), and Department of Chemistry and Biochemistry, Division of Physical Sciences (Á.N.), University of California, San Diego, La Jolla, California; and Skaggs Institute for Chemical Biology, Scripps Research Institute, La Jolla, California (N.G., M.D., J.R.F., K.B.S., V.V.F.)
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Kwok-Yiu Ho
Department of Pharmacology, Skaggs School of Pharmacy and Pharmaceutical Sciences (J.G.Y., K.G., M.D., Á.N., K.H., T.T.T., P.T.), and Department of Chemistry and Biochemistry, Division of Physical Sciences (Á.N.), University of California, San Diego, La Jolla, California; and Skaggs Institute for Chemical Biology, Scripps Research Institute, La Jolla, California (N.G., M.D., J.R.F., K.B.S., V.V.F.)
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Todd T. Talley
Department of Pharmacology, Skaggs School of Pharmacy and Pharmaceutical Sciences (J.G.Y., K.G., M.D., Á.N., K.H., T.T.T., P.T.), and Department of Chemistry and Biochemistry, Division of Physical Sciences (Á.N.), University of California, San Diego, La Jolla, California; and Skaggs Institute for Chemical Biology, Scripps Research Institute, La Jolla, California (N.G., M.D., J.R.F., K.B.S., V.V.F.)
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K. Barry Sharpless
Department of Pharmacology, Skaggs School of Pharmacy and Pharmaceutical Sciences (J.G.Y., K.G., M.D., Á.N., K.H., T.T.T., P.T.), and Department of Chemistry and Biochemistry, Division of Physical Sciences (Á.N.), University of California, San Diego, La Jolla, California; and Skaggs Institute for Chemical Biology, Scripps Research Institute, La Jolla, California (N.G., M.D., J.R.F., K.B.S., V.V.F.)
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Valery V. Fokin
Department of Pharmacology, Skaggs School of Pharmacy and Pharmaceutical Sciences (J.G.Y., K.G., M.D., Á.N., K.H., T.T.T., P.T.), and Department of Chemistry and Biochemistry, Division of Physical Sciences (Á.N.), University of California, San Diego, La Jolla, California; and Skaggs Institute for Chemical Biology, Scripps Research Institute, La Jolla, California (N.G., M.D., J.R.F., K.B.S., V.V.F.)
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Palmer Taylor
Department of Pharmacology, Skaggs School of Pharmacy and Pharmaceutical Sciences (J.G.Y., K.G., M.D., Á.N., K.H., T.T.T., P.T.), and Department of Chemistry and Biochemistry, Division of Physical Sciences (Á.N.), University of California, San Diego, La Jolla, California; and Skaggs Institute for Chemical Biology, Scripps Research Institute, La Jolla, California (N.G., M.D., J.R.F., K.B.S., V.V.F.)
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Article Information

vol. 82 no. 4 687-699
DOI 
https://doi.org/10.1124/mol.112.080291
PubMed 
22784805

Published By 
American Society for Pharmacology and Experimental Therapeutics
Print ISSN 
0026-895X
Online ISSN 
1521-0111
History 
  • Received May 28, 2012
  • Accepted July 11, 2012
  • Published online September 26, 2012.

Article Versions

  • Earlier version (July 11, 2012 - 10:45).
  • You are viewing the most recent version of this article.
Copyright & Usage 
Copyright © 2012 The American Society for Pharmacology and Experimental Therapeutics

Author Information

  1. John G. Yamauchi,
  2. Kimberly Gomez,
  3. Neil Grimster,
  4. Mikael Dufouil1,
  5. Ákos Nemecz,
  6. Joseph R. Fotsing2,
  7. Kwok-Yiu Ho,
  8. Todd T. Talley3,
  9. K. Barry Sharpless,
  10. Valery V. Fokin, and
  11. Palmer Taylor
  1. Department of Pharmacology, Skaggs School of Pharmacy and Pharmaceutical Sciences (J.G.Y., K.G., M.D., Á.N., K.H., T.T.T., P.T.), and Department of Chemistry and Biochemistry, Division of Physical Sciences (Á.N.), University of California, San Diego, La Jolla, California; and Skaggs Institute for Chemical Biology, Scripps Research Institute, La Jolla, California (N.G., M.D., J.R.F., K.B.S., V.V.F.)
  1. Address correspondence to:
    Palmer Taylor, Department of Pharmacology, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, Pharmaceutical Sciences Building, 9500 Gilman Dr., La Jolla, CA 92093-0657. E-mail: pwtaylor{at}ucsd.edu
  • ↵1 Current affiliation: University Claude Bernard Lyon 1, Villeurbanne, France.

  • ↵2 Current affiliation: Senomyx, San Diego, California.

  • ↵3 Current affiliation: Department of Biomedical and Pharmaceutical Sciences, College of Pharmacy, Idaho State University, Pocatello, Idaho.

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Molecular Pharmacology: 82 (4)
Molecular Pharmacology
Vol. 82, Issue 4
1 Oct 2012
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Research ArticleArticle

nAChR Click-Chemistry Synthesis and Pharmacological Features

John G. Yamauchi, Kimberly Gomez, Neil Grimster, Mikael Dufouil, Ákos Nemecz, Joseph R. Fotsing, Kwok-Yiu Ho, Todd T. Talley, K. Barry Sharpless, Valery V. Fokin and Palmer Taylor
Molecular Pharmacology October 1, 2012, 82 (4) 687-699; DOI: https://doi.org/10.1124/mol.112.080291

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Research ArticleArticle

nAChR Click-Chemistry Synthesis and Pharmacological Features

John G. Yamauchi, Kimberly Gomez, Neil Grimster, Mikael Dufouil, Ákos Nemecz, Joseph R. Fotsing, Kwok-Yiu Ho, Todd T. Talley, K. Barry Sharpless, Valery V. Fokin and Palmer Taylor
Molecular Pharmacology October 1, 2012, 82 (4) 687-699; DOI: https://doi.org/10.1124/mol.112.080291
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