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. Author manuscript; available in PMC: 2018 Oct 1.
Published in final edited form as: Biochim Biophys Acta. 2017 Mar 29;1863(10 Pt A):2414–2435. doi: 10.1016/j.bbadis.2017.03.020

Figure 5.

Figure 5

Bivalent and multivalent ligand binding modes. (A) The bivalent ligand first binds a receptor with one pharmacophore in a monovalent fashion. (B) The second pharmacophore is tethered in close proximity to the second binding site. (C) The second pharmacophore can bind the second receptor with reduced entropic cost. Similar binding mode may exist for multivalent ligands with more than two pharmacophores. (D) Monovalent ligands bind monomers, dimers, and higher-order oligomers equally. (E) Bivalent ligands bind dimers and higher-order oligomers in a cooperative synergistic fashion. (F) Multivalent ligands bind GPCR clusters in a cooperative synergistic fashion. Image modified from Lensing, et. al. [134].