Iz. Siemion et al., ON THE IMMUNOSTIMULATIVE AND IMMUNOSUPPRESSIVE CONFORMATION OF THYMOPENTIN ANALOGS, Polish Journal of Chemistry, 69(12), 1995, pp. 1669-1678
A series of structural analogues of lactoferrin immunosuppressive pent
apeptide I (Arg-Lys-Pro-Val-Asp) were investigated for their immunomod
ulatory activity. The series consisted of the following compounds: Arg
-Lys-Pro-Val-D-Asp (II), Arg-Lys-D-Pro-Val-Asp (III), Cys(Acm)-Arg-Lys
-Pro-Val-Asp-Cys(Acm) (IV), Cys(Acm)-Arg-Lys-D-Pro-Val-Asp-Cys(Acm) (V
) and two cyclic peptides VI and VII: H-Cys-Arg-Lys-Pro-Val-Asp-Cys-OI
I (VI) II-Cys-Arg-Lys-D-Pro-Val-Asp-Cys-OH (VII) We found that all the
se compounds demonstrate the immunosuppressive activity of diverse ran
ge regarding the both: humoral and cellular immune response. Using the
conformation of I resulted from X-ray data as tile model ''immunosupp
ressive'' conformation we compared it with the ''immunostimulative'' c
onformation proposed for thymopentin (TPS) [1]. The tolerance of the b
ioactive conformation of I to the configurational change on tile centr
al Pro residue was also investigated.