Characterization, Dynamics, and Mechanism of CXCR4 Antagonists on a Constitutively Active Mutant (Cell Chemical Biology)

In this work, Rosenberg and co-authors characterize several potent small-molecule CXCR4 antagonists. The authors discuss two different possible mechanisms for why the N1193.35A CXCR4 mutant exhibits constitutive signaling, providing biochemical evidence supporting the role of a `hydrophobic triad` observed only in the mutant.