TABLE 1

Pepducins described for CXCR4a

All C-terminal ends are modified to an amide; N-terminal end Pal is Palmitic acid; all listed pepducins for CXCR4 are derived from ICL1 except PZ-210. R1 = R2 = L-Photo-Leucine.

Embedded Image

CXCR4Sequence
 ICL163-MGYQKKLRSMTDKYRLHL-80
 ICL3224-SKLSHSKGHQKRKALK-239
PepducinSequenceFunctionRef.
 ATI-2341Pal –MGYQKKLRSMTDKYRLBiased agonistTchernychev et al., 2010, Janz et al., 2011, Quoyer et al., 2013
 ATI-2346Pal -KKLRSMTDKYRLHPAMQuoyer et al., 2013, Tchernychev et al., 2010
 ATI-2756Pal -GGYQKKLRpHTDKYRLSAR analog of ATI-2341 with improved plasma stabilityQuoyer et al., 2013, Carlson et al., 2012
 ATI-2766R1-GGYQKK-R2-SATDKYRLFluorescent pepducinJanz et al., 2011
 PZ-218 (x4pal-i1)Pal -MGYQKKLRSMTDAntagonistKaneider et al., 2005, O’Callaghan et al., 2012a,b
 Intracellular loops   (ICL PZ-210 (x4pal-i3)Pal -SKLSHSKGHQKRKALKAntagonistKaneider et al., 2005, O’Callaghan et al., 2012a-b
  • ICL, intracellular loops.

  • a Tchernychev et al. (2010) and its supporting information mentions further screening of more intracellular loop 1 pepducins in a chemotaxis assay. All show lower potencies than ATI-2341, and sequences were partly not mentioned; the patent US 9,096,646 (McMurry et al., 2015) of CXCR4 pepducins mentions further pepducins from all three intracellular loops that were partially screened.