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Molecular Pharmacology

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Research ArticleArticle

Identification of Two Prokineticin cDNAs: Recombinant Proteins Potently Contract Gastrointestinal Smooth Muscle

M. Li, C. M. Bullock, D. J. Knauer, F. J. Ehlert and Q. Y. Zhou
Molecular Pharmacology April 2001, 59 (4) 692-698; DOI: https://doi.org/10.1124/mol.59.4.692
M. Li
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C. M. Bullock
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D. J. Knauer
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F. J. Ehlert
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Q. Y. Zhou
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Abstract

The motility of gastrointestinal tract is regulated by classical neurotransmitters, neuropeptides, and humoral agents. Two novel human cDNAs have been cloned based on their sequence similarity to a frog skin secretion protein, Bv8, and a nontoxic protein of mamba snake venom. These human cDNAs encode two secreted proteins of 86 and 81 amino acids. Northern blot hybridization has revealed that these cDNAs are expressed in gastrointestinal tract, particularly the stomach. Recombinant proteins with authentic N-terminal sequences have been produced in Escherichia coli and refolded into functional proteins by careful control of protein aggregation. Mass spectrometry has confirmed the formation of five pairs of disulfide bonds. The refolded recombinant proteins potently contract gastrointestinal smooth muscle with EC50 values in the subnanomolar range. The contractile effects of the recombinant proteins are specific for gastrointestinal smooth muscle, because they have no effect on vascular or respiratory smooth muscle. To reflect their potent and specific effects on gastrointestinal smooth muscle cells, we have named these recombinant proteins prokineticins. Ligand binding studies with iodinated prokineticin revealed the presence of a high-affinity site in ileal smooth muscle. The displacement of specific binding by GTPγS suggests that the prokineticin receptor may belong to the family of G protein-coupled receptors. Experiments with verapamil and nifedipine revealed that calcium influx is essential for the contractile activity of prokineticins on gastrointestinal smooth muscle. In summary, we have identified two novel endogenous regulators of gastrointestinal motility. The availability of recombinant prokineticins should provide novel therapeutic agents for disorders involving impaired gastrointestinal motility.

Footnotes

    • Received October 23, 2000.
    • Accepted December 26, 2000.
  • Send reprint requests to: Qun-Yong Zhou, Ph.D., Pharm.D., Department of Pharmacology, University of California, Irvine, CA 92697. E-mail: qzhou{at}uci.edu

  • The American Society for Pharmacology and Experimental Therapeutics
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Molecular Pharmacology: 59 (4)
Molecular Pharmacology
Vol. 59, Issue 4
1 Apr 2001
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Research ArticleArticle

Identification of Two Prokineticin cDNAs: Recombinant Proteins Potently Contract Gastrointestinal Smooth Muscle

M. Li, C. M. Bullock, D. J. Knauer, F. J. Ehlert and Q. Y. Zhou
Molecular Pharmacology April 1, 2001, 59 (4) 692-698; DOI: https://doi.org/10.1124/mol.59.4.692

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Research ArticleArticle

Identification of Two Prokineticin cDNAs: Recombinant Proteins Potently Contract Gastrointestinal Smooth Muscle

M. Li, C. M. Bullock, D. J. Knauer, F. J. Ehlert and Q. Y. Zhou
Molecular Pharmacology April 1, 2001, 59 (4) 692-698; DOI: https://doi.org/10.1124/mol.59.4.692
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