Discovery of the first selective C5A receptor 2 (C5L2/C5AR2) ligands

US10280197B2 · kind B2 · utility

Assignees

• The Regents of the University of California · US
• THE TEXAS A&M UNIVERSITY SYSTEM · US
• The University Of Queensland · AU
• The University of Sheffield · GB

Inventors

• Dimitrios Monikis · Riverside, US
• Christodoulos A. Floudas
• Trent Martin Woodruff · Brisbane, AU
• Matthew Cooper · Cambridge, GB
• Daniel E. Croker · Tarago, AU
• Peter N. Monk · Sheffield, GB

Key dates

• Filing date: Oct 17, 2016
• Grant date: May 7, 2019
• Expiry date: Oct 17, 2036

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K38/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

A method of selectively modulating the activity of C5a receptor 2 (C5aR2). The method includes exposing the receptor to a compound that selectively modulates C5aR2 compared to C5a receptor 1 (C5aR1). In some cases, the compound is peptide P32 or P59. Methods of recruiting β-arrestin 2 in a cell, modulating C5a-induced ERK1/2 activation in a macrophage, selectively inhibiting the release of IL-6 from a macrophage, are also provided.