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Heterologous Expression of Excitability Proteins: Route to More Specific Drugs?

Lester, Henry A. (1988) Heterologous Expression of Excitability Proteins: Route to More Specific Drugs? Science, 241 (4869). pp. 1057-1063. ISSN 0036-8075. doi:10.1126/science.2457947.

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Many clinically important drugs act on the intrinsic membrane proteins (ion channels, receptors, and ion pumps) that control cell excitability. A major goal of pharmacology has been to develop drugs that are more specific for a particular subtype of excitability molecule. DNA cloning has revealed that many excitability proteins are encoded by multigene families and that the diversity of previously recognized pharmacological subtypes is matched, and probably surpassed, by the diversity of messenger RNAs that encode excitability molecules. In general, the diverse subtypes retain their properties when the excitability proteins are expressed in foreign cells such as oocytes and mammalian cell lines. Such heterologous expression may therefore become a tool for testing drugs against specific subtypes. In a systematic research program to exploit this possibility, major considerations include alternative processing of messenger RNA for excitability proteins, coupling to second-messenger systems, and expression of enough protein to provide material for structural studies.

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Lester, Henry A.0000-0002-5470-5255
Additional Information:© 1988 American Association for the Advancement of Science. I thank N. Davidson, T. M. Fong, H. Graves, D. S. Krafte, L. A. Jaffe, D. Julius, D. Kline, W. Koch, C. Labarca, R. J. Leonard, J. Lindstrom, E. McKenna, R. W. Olsen, J. H. Sabry, A. Schwartz, M. Tanouye, and L. Yu for comments on this article and M. A. Buckles for assistance with the manuscript. Supported by grants from NIH, the Klingenstein Fund, and the Drown Foundation.
Funding AgencyGrant Number
Esther A. and Joseph Klingenstein FundUNSPECIFIED
Drown FoundationUNSPECIFIED
Issue or Number:4869
Record Number:CaltechAUTHORS:20141222-150346710
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Official Citation:Heterologous expression of excitability proteins: route to more specific drugs? HA Lester Science 26 August 1988: 241 (4869), 1057-1063. [DOI:10.1126/science.2457947]
Usage Policy:No commercial reproduction, distribution, display or performance rights in this work are provided.
ID Code:53115
Deposited By: Tony Diaz
Deposited On:23 Dec 2014 17:10
Last Modified:10 Nov 2021 19:48

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