@article { WOS:000320347100035, title = {Backbone cyclic helix mimetic of chemokine (C-C motif) receptor 2: A rational approach for inhibiting dimerization of G protein-coupled receptors}, journal = {BIOORGANIC \& MEDICINAL CHEMISTRY}, volume = {21}, year = {2013}, note = {[[{"fid":"263833","view_mode":"default","type":"media","attributes":{"style":"width: 450px; height: 113px;","alt":"back","class":"img-responsive media-element file-default "}}]] }, month = {JUL 1}, pages = {3958-3966}, abstract = {

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.


}, issn = {0968-0896}, doi = {10.1016/j.bmc.2013.03.019}, author = {Mattan Hurevich and Ratner-Hurevich, Maya and Tal-Gan, Yftah and Deborah E. Shalev and Ben-Sasson, Shlomo Z. and Gilon, Chaim} }