Conformational dynamics underlying Atypical Chemokine Receptor 3 activation

ABSTRACT: Here we used Hydrogen/Deuterium exchange mass spectrometry (HDX-MS) to examine the binding mode and mechanism of action of various small-molecule ACKR3 ligands of different efficacy for β-arrestin recruitment. Our results show that activation or inhibition of ACKR3 is largely governed by intracellular conformational changes of helix 6, intracellular loop 2 and helix 7, while the DRY motif becomes protected during both processes. Moreover, HDX-MS identifies the binding sites and the allosteric modulation of ACKR3 upon β-arrestin 1 binding.

INSTRUMENT(S):

ORGANISM(S): Homo Sapiens (human)

SUBMITTER: Functional Proteomics Platform FPP  

LAB HEAD: Cherine Bechara

PROVIDER: PXD044103 | Pride | 2024-07-16

REPOSITORIES: Pride