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. Author manuscript; available in PMC: 2014 Jan 15.
Published in final edited form as: Biochem Pharmacol. 2012 Sep 10;85(2):147–152. doi: 10.1016/j.bcp.2012.08.021

Table 2.

mAb that recognize specific conformations of GPCRs

Receptor mAb-Source/composition Epitope Recognized Receptor State Detected Pharmacology Ref
CCR5 MC-4, MC-5, MC-7 N-terminal domain Agonist conformation with multiple ligands bound Agonist Inhibition [19]
CCR5 MC-1 ICL-2 Agonist conformation Multiple agonist inhibition [19]
CCR5 MC-6 ECL- conformation determinant Active conformation Stabilizes active conformation [19]
CXCR4 12G5 ECL-1,2 conformational Cell type and donor specific conformations Inhibition of chemotaxis [55]
CXCR4 44717.111 (12G5 also examine in this paper) Proteoliposome (PMPLs) containing CXCR4 Binds to SDF-1 bound or unbound R Abolished binding of GP120 [56]
CXCR4 Llama immunization with CXCR4- expressing HEK293; followed by phage library selection Antagonist and inverse agonist, binds to ECL2 and ECL3 [57]
CCR5 3A9 Phage Displayed CCR5 epitopes inferred by alanine mapping to extracellular loops and computer modeling Not indicated Not Indicated [58]
β2AR Camelid Nanobody Nb80 Cytoplasmic end of receptor projecting into the lattice By modeling and Crystallography -the agonist active state Intracellular loop binding no pharmacological activity noted [59]
Rhodopsi n K42–41L antibody selected by reactivity with a peptide in a phage display library Epitope found in dark-adapted rhodopsin and metarhodopsin I not in metarhodopsin II and is a sequence in C3 loop Inhibits for formation of metarhodpsin II while stabilizing metarhodpsin I- locks C3 loop into an extended conformation Not studied [60]