Role of Lys215 located in the fifth transmembrane domain of the AT2 receptor in ligand-receptor interaction

Regulatory Peptides
L PulakatNara Gavini

Abstract

Studies on ligand-receptor interaction of Angiotensin II (Ang II) receptor type 1 have shown that for peptidic ligands to bind this receptor they must interact via their C-terminal carboxylate group to the positively charged side chain of the Lysine residue 199 located in the fifth transmembrane domain of this receptor. In the Ang II receptor type AT2, this Lysine residue is conserved at position 215 in the fifth transmembrane domain. To determine the specific mechanism of ligand binding to the Angiotensin II receptor type AT2, mutated AT2 receptors were generated in which the Lys215 was replaced with glutamic acid, glutamine, alanine and arginine. The ability of these mutated receptors to bind peptidic ligands 125I-[Sar1-Ile8]Ang II (non-specific for AT2 receptor type), 125I-CGP42112A (AT2 receptor specific) and the non-peptidic ligand PD123319 (AT2 receptor specific) was evaluated by expressing these receptors in Xenopus oocytes and performing binding assays. The Lys215Glu and Lys215Gln mutants of AT2 receptor lost their affinity to 125I-[Sar1-Ile8]Ang II, but retained their affinity to 125I-CGP42112A and PD123319. In contrast, Lys215Arg mutant retained its affinity to 125I-[Sar1-Ile8]Ang II, but exhibited lower affinity to 1...Continue Reading

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Citations

Dec 14, 1999·Protein Science : a Publication of the Protein Society·J SunT E Hugli
Oct 16, 2007·Journal of Molecular Graphics & Modelling·Christian SköldAnders Karlén
Jun 6, 2003·Bioorganic & Medicinal Chemistry·Susanna LindmanAnders Hallberg
Nov 13, 2004·Arteriosclerosis, Thrombosis, and Vascular Biology·Christoph J WruckThomas Unger
Feb 6, 2008·Chemical Biology & Drug Design·Swati Jain, Arpita Yadav
Nov 15, 2003·American Journal of Physiology. Regulatory, Integrative and Comparative Physiology·Kwang-Lae HoeJuan M Saavedra
Mar 11, 2000·American Journal of Physiology. Endocrinology and Metabolism·S GallinatC Sumners
Oct 8, 1999·Biochemical and Biophysical Research Communications·J KurfisL Pulakat
Jun 15, 2004·Biochemical and Biophysical Research Communications·Lakshmi PulakatNara Gavini

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