Citation:
Hurevich, M. ; Ratner-Hurevich, M. ; Tal-Gan, Y. ; Shalev, D. E. ; Ben-Sasson, S. Z. ; Gilon, C. . Backbone Cyclic Helix Mimetic Of Chemokine (C-C Motif) Receptor 2: A Rational Approach For Inhibiting Dimerization Of G Protein-Coupled Receptors. BIOORGANIC & MEDICINAL CHEMISTRY 2013, 21, 3958-3966.
Date Published:
JUL 1Abstract:
The transmembrane helical bundle of G protein-coupled receptors (GPCRs) dimerize through helix-helix interactions in response to inflammatory stimulation. A strategy was developed to target the helical dimerization site of GPCRs by peptidomimetics with drug like properties. The concept was demonstrated by selecting a potent backbone cyclic helix mimetic from a library that derived from the dimerization region of chemokine (C-C motif) receptor 2 (CCR2) that is a key player in Multiple Sclerosis. We showed that CCR2 based backbone cyclic peptide having a stable helix structure inhibits specific CCR2-mediated chemotactic migration (C) 2013 Elsevier Ltd. All rights reserved.
Notes:
