Article
Modulation of ligand selectivity by mutation of the first extracellular loop of the human C5a receptor.
Biochemical pharmacology - 15 Jun 2001
Cain S A, Woodruff T M, Taylor S M, Fairlie D P, Sanderson S D, Monk P N
Abstract excerpt
The cyclic C5a receptor antagonist, phenylalanine [L-ornithine-proline-D-cyclohexylalanine-tryptophan-arginine] (F-[OPchaWR]), has approximately 1000-fold less affinity for the C5a receptor (C5aR) on murine polymorphonuclear leukocytes than on human. Analysis of C5aR from different species shows that a possible cause of this difference is the variation in the sequence of the first extracellular loop of the...
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