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Literature DB >> 25699147

Interconversion of Functional Activity by Minor Structural Alterations in Nonpeptide AT2 Receptor Ligands.

Charlotta Wallinder¹, Christian Sköld¹, Milad Botros², Marie-Odile Guimond³, Mathias Hallberg², Nicole Gallo-Payet³, Anders Karlén¹, Mathias Alterman¹.

Abstract

Migration of the methylene imidazole side chain in the first reported selective drug-like AT2 receptor agonist C21/M024 (1) delivered the AT2 receptor antagonist C38/M132 (2). We now report that the AT2 receptor antagonist compound 4, a biphenyl derivative that is structurally related to 2, is transformed to the agonist 6 by migration of the isobutyl group. The importance of the relative position of the methylene imidazole and the isobutyl substituent is highlighted herein.

Entities: Chemical Gene

Keywords: AT2 receptor; C21/M024; C38/M132; agonist; antagonist; nonpeptide ligands

Year: 2014 PMID： 25699147 PMCID： PMC4329586 DOI： 10.1021/ml500427r

Source DB: PubMed Journal: ACS Med Chem Lett ISSN： 1948-5875 Impact factor: 4.345

26 in total

1. Nitric oxide and cyclic GMP are involved in angiotensin II AT(2) receptor effects on neurite outgrowth in NG108-15 cells.

Authors: Louis Gendron; Frédéric Côté; Marcel D Payet; Nicole Gallo-Payet
Journal: Neuroendocrinology Date: 2002-01 Impact factor: 4.914

2. Stimulation of AT2 receptor exerts beneficial effects in stroke-prone rats: focus on renal damage.

Authors: Paolo Gelosa; Alice Pignieri; Lars Fändriks; Marc de Gasparo; Anders Hallberg; Cristina Banfi; Laura Castiglioni; Lucia Turolo; Uliano Guerrini; Elena Tremoli; Luigi Sironi
Journal: J Hypertens Date: 2009-12 Impact factor: 4.844

Review 3. Novel therapeutic targets for the treatment of heart failure.

Authors: Juan Tamargo; José López-Sendón
Journal: Nat Rev Drug Discov Date: 2011-06-24 Impact factor: 84.694

Review 4. Update on the angiotensin AT(2) receptor.

Authors: Claudia A McCarthy; Robert E Widdop; Kate M Denton; Emma S Jones
Journal: Curr Hypertens Rep Date: 2013-02 Impact factor: 5.369

5. EMA401, an orally administered highly selective angiotensin II type 2 receptor antagonist, as a novel treatment for postherpetic neuralgia: a randomised, double-blind, placebo-controlled phase 2 clinical trial.

Authors: Andrew S C Rice; Robert H Dworkin; Tom D McCarthy; Praveen Anand; Chas Bountra; Philip I McCloud; Julie Hill; Gary Cutter; Geoff Kitson; Nuket Desem; Milton Raff
Journal: Lancet Date: 2014-02-05 Impact factor: 79.321

6. Angiotensin II receptors and renin in the porcine uterus: myometrial AT2 and endometrial AT1 receptors are down-regulated during gestation.

Authors: A H Nielsen; K Schauser; H Winther; V Dantzer; K Poulsen
Journal: Clin Exp Pharmacol Physiol Date: 1997-05 Impact factor: 2.557

7. Design, synthesis, and biological evaluation of the first selective nonpeptide AT2 receptor agonist.

Authors: Yiqian Wan; Charlotta Wallinder; Bianca Plouffe; Hélène Beaudry; A K Mahalingam; Xiongyu Wu; Berndt Johansson; Mathias Holm; Milad Botoros; Anders Karlén; Anders Pettersson; Fred Nyberg; Lars Fändriks; Nicole Gallo-Payet; Anders Hallberg; Mathias Alterman
Journal: J Med Chem Date: 2004-11-18 Impact factor: 7.446

8. Expression and role of the angiotensin II AT2 receptor in human prostate tissue: in search of a new therapeutic option for prostate cancer.

Authors: Marie-Odile Guimond; Marie-Claude Battista; Fatemeh Nikjouitavabi; Maude Carmel; Véronique Barres; Alexandre A Doueik; Ladan Fazli; Martin Gleave; Robert Sabbagh; Nicole Gallo-Payet
Journal: Prostate Date: 2013-02-06 Impact factor: 4.104

Interconversion of Functional Activity by Minor Structural Alterations in Nonpeptide AT2 Receptor Ligands.

1. Nitric oxide and cyclic GMP are involved in angiotensin II AT(2) receptor effects on neurite outgrowth in NG108-15 cells.

2. Stimulation of AT2 receptor exerts beneficial effects in stroke-prone rats: focus on renal damage.

Review 3. Novel therapeutic targets for the treatment of heart failure.

Review 4. Update on the angiotensin AT(2) receptor.

5. EMA401, an orally administered highly selective angiotensin II type 2 receptor antagonist, as a novel treatment for postherpetic neuralgia: a randomised, double-blind, placebo-controlled phase 2 clinical trial.

6. Angiotensin II receptors and renin in the porcine uterus: myometrial AT2 and endometrial AT1 receptors are down-regulated during gestation.

7. Design, synthesis, and biological evaluation of the first selective nonpeptide AT2 receptor agonist.

8. Expression and role of the angiotensin II AT2 receptor in human prostate tissue: in search of a new therapeutic option for prostate cancer.

9. The angiotensin AT2 receptor modulates T-type calcium current in non-differentiated NG108-15 cells.

10. Selective angiotensin II AT2 receptor agonists: Benzamide structure-activity relationships.

Review 1. The Angiotensin AT₂ Receptor: From a Binding Site to a Novel Therapeutic Target.

Review 2. Small-molecule inhibitors of Slack potassium channels as potential therapeutics for childhood epilepsies.

3. Evolution of Angiotensin Peptides and Peptidomimetics as Angiotensin II Receptor Type 2 (AT2) Receptor Agonists.

Review 3. Novel therapeutic targets for the treatment of heart failure.

Review 4. Update on the angiotensin AT(2) receptor.

Review 1. The Angiotensin AT2 Receptor: From a Binding Site to a Novel Therapeutic Target.

Review 2. Small-molecule inhibitors of Slack potassium channels as potential therapeutics for childhood epilepsies.

Review 1. The Angiotensin AT₂ Receptor: From a Binding Site to a Novel Therapeutic Target.