PMID: 9531424Apr 8, 1998Paper

Bufokinin: a substance P-related peptide from the gut of the toad, Bufo marinus with high binding affinity but low selectivity for mammalian tachykinin receptors

The Journal of Peptide Research : Official Journal of the American Peptide Society
J M ConlonE Burcher

Abstract

A tachykinin peptide, termed bufokinin, was isolated in pure form from an extract of the intestine of the toad, Bufo marinus, and its primary structure was established as: Lys-Pro-Arg-Pro-Asp-Gln-Phe-Tyr-Gly-Leu-Met.NH2. This sequence was confirmed by chemical synthesis and shows four amino acid substitutions (Arg1 --> Lys,Lys3 --> Arg,Gln5 --> Asp and Phe8 --> Tyr) compared with substance P. Binding parameters for synthetic bufokinin and mammalian tachykinins were compared using receptor-selective radioligands and crude membranes from rat tissues enriched in the NK-1 (submandibular gland) , NK-2 (stomach fundus) and NK-3 (brain) receptors. In terms of inhibiting the binding of the selective radioligands, bufokinin (Kd = 0.3 nM) was 1.8-fold more potent than substance P at the rat NK-1 site, but it was only 2-fold less potent (Kd = 2.8 nM) than neurokinin A at the NK-2 site and only 2-fold less potent (Kd = 48 nM) than neurokinin B at the NK-3 site. Thus, bufokinin shows relatively high affinity but lack of selectivity for all three tachykinin binding sites in rat tissues.

References

Jun 15, 1992·European Journal of Biochemistry·J Jensen, J M Conlon
May 31, 1991·Biochemical and Biophysical Research Communications·H KozawaH Matsuo
Feb 1, 1988·Regulatory Peptides·J M ConlonL Thim
Sep 1, 1980·Analytical Biochemistry·P J Munson, D Rodbard
Jun 1, 1993·Journal of Neurochemistry·C J MussapE Burcher
Mar 1, 1996·The Journal of Steroid Biochemistry and Molecular Biology·M K KodjoH Vaudry

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Citations

Nov 9, 2000·Clinical and Experimental Pharmacology & Physiology·L LiuE Burcher
Jun 3, 2006·Natural Product Reports·Tara L PukalaMichael J Tyler
Dec 31, 2016·Journal of Ethnopharmacology·Candelario RodríguezMarcelino Gutiérrez
Oct 12, 2001·Brain Research Bulletin·S Holmgren, J Jensen
Jul 27, 2005·Peptides·Lu Liu, Elizabeth Burcher

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