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] |