TABLE 6

List of conserved residues in four chemokine receptors that have been mutated to alanine in this and other published studies (Dragic et al., 2000; Mirzadegan et al., 2000; Berkhout et al., 2003; de Mendonça et al., 2005; Maeda et al., 2006; Seibert et al., 2006; Wise et al., 2007)

Mutation of the underlined and bold residues has been reported to display a loss of antagonist activity. Residues in parentheses have no significant effect on either agonist or antagonist activity; italic residues indicate mutants with poor cell surface expression and/or reduced chemotactic activity compared with wild-type receptor; residues in normal type and not in parentheses have not been mutated; and underlined and italic residues have significant effect on small molecule agonist activity. Glu7.39 mutation results are for E7.39Q mutation and not the alanine mutation.


CCR1

CCR2

CCR3

CCR5
Tyr411.39 Tyr49 1.39 Tyr41 1.39 Tyr371.39
(Trp902.60) Trp982.60 Trp862.60 Trp862.60
Tyr1133.32 Tyr1203.32 Tyr1133.32 Tyr1083.32
Tyr1143.33 His1213.33 His1143.33 (Phe1093.33)
Leu1173.36 Tyr124 3.36 Leu1173.36 Tyr1123.36
(Trp2526.48) Trp256 6.48 Trp2526.48 Trp2486.48
Ile2596.55 Ile2636.55 Ile2596.55 (Leu2556.55)
Glu2877.39 Glu2917.39 Glu2877.39 Glu2837.39
Val2887.40
Thr2927.40
Val2887.40
Thr2847.40