Table 1.

Cyclophilin A binding and inhibition of MLR and IL-2 production by CsA analogsa

CSA derivativebMLRIL-2CYP A binding
CsA100100100
(γ-OH) MeLeu4-Cs (211–810)0.80.9100
D-Sar (α-SMe)3 Val2-DH-Cs (209–825)1055200
Allo-Thr-2-Cs91120
Norvaline-2-Cs483720
d-Ala(3-acetylamino)-8-Cs5533125
Thr-2-Cs5910071
d-MeSer-3-Cs7742333
d-Ser(O-CH2CH2-OH)-8-Cs100100200
d-Ser-8-Cs139167167
  • a The ability of a series of CsA analogs to inhibit an MLR assay, IL-2 production, or cyclophilin A (CYP A) binding was compared to that of CsA and is expressed here as percentage of activity relative to CsA activity.

  • b In CsA derivatives, CsA is shown as Cs.