![[Feedback]](/icons/banner/feedbackACT.gif){kind=icon}
![[For Subscribers]](/icons/banner/subscriberACT.gif){kind=icon}
![[Archive]](/icons/banner/archiveACT.gif){kind=icon}
![[Search]](/icons/banner/searchACT.gif){kind=icon}
![[Contents]](/icons/banner/tocACT.gif){kind=icon}
|
|
|
|
|
||
JF Hess, JA Borkowski, T Macneil, GY Stonesifer, J Fraher, CD Strader and RW Ransom
Department of Molecular Pharmacology and Biochemistry, Merck Research Laboratories, Rahway, NJ 07065.
The pharmacology of cloned B2 bradykinin receptors heterologously expressed in cell lines lacking any endogenous bradykinin receptors was analyzed. The possibility of B2 bradykinin receptor heterogeneity had been proposed on the basis of numerous studies in various tissue preparations. The results reported here permit a direct evaluation of some of these hypotheses by examining the pharmacological properties of cloned bradykinin receptors. A cloned human B2 bradykinin receptor was stably transfected into Chinese hamster ovary cells. The data suggest that in response to bradykinin (BK), the cloned receptor activates both phosphatidylinositol hydrolysis and arachidonic acid release by independent pathways. Thus, the activation of these two second messenger pathways does not require the existence of two B2 bradykinin receptor subtypes. A mouse gene encoding the B2 bradykinin receptor was isolated, and the coding region was expressed in COS-7 cells. This murine receptor exhibited the pharmacological properties of a "classical" B2 bradykinin receptor. A comparison of the pharmacological profiles of cloned human and murine homologs of the B2 bradykinin receptor indicates that both receptors bind agonists with similar properties. However, the two receptors differ dramatically in their affinity for some peptide antagonists. The mouse receptor has a 60- to 80-fold higher affinity for [D-Arg0Hyp3, Thi5,8,D-Phe7]BK and [D- Arg0,Hyp3,D-Phe7]BK than its human homolog. Thus, the species of a bradykinin receptor can have a significant effect on its pharmacology. The cloning, expression, and pharmacological comparison of human and mouse B2 bradykinin receptor genes indicate that some of the previous reports of B2 receptor subtypes can be explained by species differences in a single B2 bradykinin receptor gene.
This article has been cited by other articles:
|
|
 |
|
  S. Wang, Y. Dai, T. Fukuoka, H. Yamanaka, K. Kobayashi, K. Obata, X. Cui, M. Tominaga, and K. Noguchi Phospholipase C and protein kinase A mediate bradykinin sensitization of TRPA1: a molecular mechanism of inflammatory pain Brain, May 1, 2008; 131(5): 1241 - 1251. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 M. Chachisvilis, Y.-L. Zhang, and J. A. Frangos G protein-coupled receptors sense fluid shear stress in endothelial cells PNAS, October 17, 2006; 103(42): 15463 - 15468. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 D. Biyashev, F. Tan, Z. Chen, K. Zhang, P. A. Deddish, E. G. Erdos, and C. Hecquet Kallikrein activates bradykinin B2 receptors in absence of kininogen Am J Physiol Heart Circ Physiol, March 1, 2006; 290(3): H1244 - H1250. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 J. H. Kim, D. Jain, O. Tliba, B. Yang, W. F. Jester Jr., R. A. Panettieri Jr., Y. Amrani, and E. Pure TGF-{beta} potentiates airway smooth muscle responsiveness to bradykinin Am J Physiol Lung Cell Mol Physiol, October 1, 2005; 289(4): L511 - L520. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 D. A. Davis, K. E. Singer, M. De La Luz Sierra, M. Narazaki, F. Yang, H. M. Fales, R. Yarchoan, and G. Tosato Identification of carboxypeptidase N as an enzyme responsible for C-terminal cleavage of stromal cell-derived factor-1{alpha} in the circulation Blood, June 15, 2005; 105(12): 4561 - 4568. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 L. M. F. Leeb-Lundberg, F. Marceau, W. Muller-Esterl, D. J. Pettibone, and B. L. Zuraw International Union of Pharmacology. XLV. Classification of the Kinin Receptor Family: from Molecular Mechanisms to Pathophysiological Consequences Pharmacol. Rev., March 1, 2005; 57(1): 27 - 77. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 E. G Erdos Kinins, the long march--A personal view Cardiovasc Res, June 1, 2002; 54(3): 485 - 491. [Full Text] [PDF]
|
|
|
|
 |
|
 G. Griffin, Q. Tao, and M. E. Abood Cloning and Pharmacological Characterization of the Rat CB2 Cannabinoid Receptor J. Pharmacol. Exp. Ther., March 1, 2000; 292(3): 886 - 894. [Abstract] [Full Text]
|
|
|
|
 |
|
 A. Pizard, A. Blaukat, W. Muller-Esterl, F. Alhenc-Gelas, and R. M. Rajerison Bradykinin-induced Internalization of the Human B2 Receptor Requires Phosphorylation of Three Serine and Two Threonine Residues at Its Carboxyl Tail J. Biol. Chem., April 30, 1999; 274(18): 12738 - 12747. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
F. Marceau, J. F. Hess, and D. R. Bachvarov The B1 Receptors for Kinins Pharmacol. Rev., September 1, 1998; 50(3): 357 - 386. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
A. Ni, L. Chao, and J. Chao Transcription Factor Nuclear Factor kappa B Regulates the Inducible Expression of the Human B1 Receptor Gene in Inflammation J. Biol. Chem., January 30, 1998; 273(5): 2784 - 2791. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
A. Pizard, J. Marchetti, J. Allegrini, F. Alhenc-Gelas, and R. M. Rajerison Negative Cooperativity in the Human Bradykinin B2 Receptor J. Biol. Chem., January 16, 1998; 273(3): 1309 - 1315. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 R. G. Miller and R. Sufit New approaches to the treatment of ALS Neurology, April 1, 1997; 48(4_Suppl_4): 28S - 32S. [Full Text] [PDF]
|
|
|
|
|
|
P. Wohlfart, J. Dedio, K. Wirth, B. A. Schölkens, and G. Wiemer Different B1 Kinin Receptor Expression and Pharmacology in Endothelial Cells of Different Origins and Species J. Pharmacol. Exp. Ther., February 1, 1997; 280(2): 1109 - 1116. [Abstract] [Full Text]
|
|
|
|
|
|
T. Leeb, S. A. Mathis, and L. M.F. Leeb-Lundberg 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., January 3, 1997; 272(1): 311 - 317. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
A. Doble The pharmacology and mechanism of action of riluzole Neurology, December 1, 1996; 47(6_Suppl_4): 233S - 241S. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
L. Lacomblez, G. Bensimon, P. N. Leigh, P. Guillet, L. Powe, S. Durrleman, J. C. Delumeau, and V. Meininger A confirmatory dose-ranging study of riluzole in ALS Neurology, December 1, 1996; 47(6_Suppl_4): 242S - 250S. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
M. C.S. Herzig, N. R. Nash, M. Connolly, D. J. Kyle, and L. M.F. Leeb-Lundberg The N Terminus of Bradykinin When Bound to the Human Bradykinin B2 Receptor Is Adjacent to Extracellular Cys20 and Cys277 in the Receptor J. Biol. Chem., November 22, 1996; 271(47): 29746 - 29751. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
R. G. Miller, J. P. Bouchard, P. Duquette, A. Eisen, D. Gelinas, Y. Harati, T. L. Munsat, L. Powe, J. Rothstein, P. Salzman, et al. Clinical trials of riluzole in patients with ALS Neurology, October 1, 1996; 47(4_Suppl_2): 86S - 92S. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
J. M. Wilson, A. I. Levey, A. Rajput, L. Ang, M. Guttman, K. Shannak, H. B. Niznik, O. Hornykiewicz, C. Pifl, and S. J. Kish Differential changes in neurochemical markers of striatal dopamine nerve terminals in idiopathic Parkinson's disease Neurology, September 1, 1996; 47(3): 718 - 726. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
J. A. Borkowski, R. W. Ransom, G. R. Seabrook, M. Trumbauer, H. Chen, R. G. Hill, C. D. Strader, and J. F. Hess Targeted Disruption of a B[IMAGE] Bradykinin Receptor Gene in Mice Eliminates Bradykinin Action in Smooth Muscle and Neurons J. Biol. Chem., June 9, 1995; 270(23): 13706 - 13710. [Abstract] [Full Text] [PDF]
|
|
 |
 |
 |
|
 |
 |
 |
