Pharmacological Characterization of Ligand-receptor Interactions at the Zebrafish Bradykinin Receptor

Overview

Journal Br J Pharmacol

Publisher Wiley

Specialty Pharmacology

Date 2005 Jan 13

PMID 15644864

Citations 3

Authors

Torun Bromee

Jyrki P Kukkonen

Per Andersson

J Michael Conlon

Dan Larhammar

Affiliations

Soon will be listed here.

Abstract

Ligand interactions of a piscine bradykinin (BK) receptor expressed in vitro have been characterized for the first time by measuring inositol phosphate accumulation. The ligands were analogues of zebrafish BK with serial substitutions by D-amino acids or alanine. Substitutions at residues Arg(1), Gly(4), Ser(6), Pro(7), Leu(8) and Arg(9) caused greatly reduced potency and maximum response. The Pro(3) --> Ala analogue had higher potency but lower maximum response. The peptide HOE140 was a weak partial agonist although it is an antagonist at the human B2 receptor and a potent agonist at chicken B2.Thus, cloned zebrafish BK receptor reveals a ligand-interaction profile that is distinct from mammalian B1 and B2 receptors and from the previously characterized BK receptor in trout stomach, but similar to the receptor in cod intestine. These results increase our understanding of the evolution of BK receptors and the functions of the kallikrein-kinin system.

Citing Articles

Fishing for Contact: Modeling Perivascular Glioma Invasion in the Zebrafish Brain.

Umans R, Ten Kate M, Pollock C, Sontheimer H ACS Pharmacol Transl Sci. 2021; 4(4):1295-1305.

PMID: 34423267 PMC: 8369679. DOI: 10.1021/acsptsci.0c00129.

A novel transgenic zebrafish model for blood-brain and blood-retinal barrier development.

Xie J, Farage E, Sugimoto M, Anand-Apte B BMC Dev Biol. 2010; 10:76.

PMID: 20653957 PMC: 2914679. DOI: 10.1186/1471-213X-10-76.

Critical role of tissue kallikrein in vessel formation and maturation: implications for therapeutic revascularization.

Stone O, Richer C, Emanueli C, van Weel V, Quax P, Katare R Arterioscler Thromb Vasc Biol. 2009; 29(5):657-64.

PMID: 19164804 PMC: 2827862. DOI: 10.1161/ATVBAHA.108.182139.

References

Regoli D, Pheng L, Allogho S, Gobeil F . Receptors for kinins: from classical pharmacology to molecular biology. Immunopharmacology. 1996; 33(1-3):24-31. DOI: 10.1016/0162-3109(96)00077-x. View

Conlon J, Le Mevel J, Conklin D, Weaver L, Duff D, Olson K . Isolation and cardiovascular activity of a second bradykinin-related peptide ([Arg0, Trp5, Leu8]bradykinin) from trout. Peptides. 1996; 17(3):531-7. DOI: 10.1016/0196-9781(96)00024-1. View

Leeb T, Mathis S . The sixth transmembrane domains of the human B1 and B2 bradykinin receptors are structurally compatible and involved in discriminating between subtype-selective agonists. J Biol Chem. 1997; 272(1):311-7. DOI: 10.1074/jbc.272.1.311. View

Platzack B, Conlon J . Purification, structural characterization, and cardiovascular activity of cod bradykinins. Am J Physiol. 1997; 272(2 Pt 2):R710-7. DOI: 10.1152/ajpregu.1997.272.2.R710. View

Hall J . Bradykinin receptors. Gen Pharmacol. 1997; 28(1):1-6. DOI: 10.1016/s0306-3623(96)00174-7. View

Austin C, Faussner A, Robinson H, Chakravarty S, Kyle D, Bathon J . Stable expression of the human kinin B1 receptor in Chinese hamster ovary cells. Characterization of ligand binding and effector pathways. J Biol Chem. 1997; 272(17):11420-5. DOI: 10.1074/jbc.272.17.11420. View

Schroeder C, Beug H, Muller-Esterl W . Cloning and functional characterization of the ornithokinin receptor. Recognition of the major kinin receptor antagonist, HOE140, as a full agonist. J Biol Chem. 1997; 272(19):12475-81. DOI: 10.1074/jbc.272.19.12475. View

Jensen J, Conlon J . Effects of trout bradykinin on the motility of the trout stomach and intestine: evidence for a receptor distinct from mammalian B1 and B2 subtypes. Br J Pharmacol. 1997; 121(3):526-30. PMC: 1564722. DOI: 10.1038/sj.bjp.0701175. View

Takano M, Kondo J, Yayama K, Otani M, Sano K, Okamoto H . Molecular cloning of cDNAs for mouse low-molecular-weight and high-molecular-weight prekininogens. Biochim Biophys Acta. 1997; 1352(2):222-30. DOI: 10.1016/s0167-4781(97)00018-3. View

10.

De Weerd W . Bradykinin sequesters B2 bradykinin receptors and the receptor-coupled Galpha subunits Galphaq and Galphai in caveolae in DDT1 MF-2 smooth muscle cells. J Biol Chem. 1997; 272(28):17858-66. DOI: 10.1074/jbc.272.28.17858. View

11.

Ricupero D, Polgar P, Taylor L, Sowell M, Gao Y, Bradwin G . Enhanced bradykinin-stimulated phospholipase C activity in murine embryonic stem cells lacking the G-protein alphaq-subunit. Biochem J. 1998; 327 ( Pt 3):803-9. PMC: 1218860. DOI: 10.1042/bj3270803. View

12.

Guex N, Peitsch M . SWISS-MODEL and the Swiss-PdbViewer: an environment for comparative protein modeling. Electrophoresis. 1998; 18(15):2714-23. DOI: 10.1002/elps.1150181505. View

13.

Regoli D, Nsa Allogho S, Rizzi A, Gobeil F . Bradykinin receptors and their antagonists. Eur J Pharmacol. 1998; 348(1):1-10. DOI: 10.1016/s0014-2999(98)00165-4. View

14.

MARCEAU F, Hess J, Bachvarov D . The B1 receptors for kinins. Pharmacol Rev. 1998; 50(3):357-86. View

15.

Fathy D, Kyle D . High-affinity binding of peptide agonists to the human B1 bradykinin receptor depends on interaction between the peptide N-terminal L-lysine and the fourth extracellular domain of the receptor. Mol Pharmacol. 2000; 57(1):171-9. View

16.

Yang X, Taylor L, Polgar P . Effect of the G-protein, G alpha(i2), and G alpha(i3) subunit knockdown on bradykinin-induced signal transduction in rat-1 cells. Mol Cell Biol Res Commun. 1999; 1(3):227-36. DOI: 10.1006/mcbr.1999.0136. View

17.

Mahabeer R, Bhoola K . Kallikrein and kinin receptor genes. Pharmacol Ther. 2000; 88(1):77-89. DOI: 10.1016/s0163-7258(00)00080-2. View

18.

Jensen J, Soto A, Conlon J . Structure-activity relationships of trout bradykinin ([Arg(0),Trp(5),Leu(8)]-bradykinin). Peptides. 2001; 21(12):1793-8. DOI: 10.1016/s0196-9781(00)00336-3. View

19.

Kang D, Lamb M, Fathy D . The human B1 bradykinin receptor exhibits high ligand-independent, constitutive activity. Roles of residues in the fourth intracellular and third transmembrane domains. J Biol Chem. 2001; 276(12):8785-92. DOI: 10.1074/jbc.M007396200. View

20.

Shahbazi F, Conlon J, Holmgren S, Jensen J . Effects of cod bradykinin and its analogs on vascular and intestinal smooth muscle of the Atlantic cod, Gadus morhua. Peptides. 2001; 22(7):1023-9. DOI: 10.1016/s0196-9781(01)00420-x. View