Thymosin-like peptides as potential immunostimulants. Synthesis via the polymeric-reagent method.
This paper reports our attempt at designing new immunostimulating peptides which are chemically related to the bioactive peptides thymosin alpha 1 and thymopentin. Three peptides were synthesized, Asp-Leu-Lys-Glu-Arg-Lys-Asp-Val-Tyr (3), Arg-Lys-Asp-Val-Tyr-Glu-Glu-Ala-Glu-Asn (2), and Asp-Leu-Lys-Glu-Arg-Lys-Asp-Val-Tyr-Glu-Glu-Ala-Glu-Asn (1), each of which contains the thymopentin sequence and portions of the bioactive sequence of thymosin alpha 1. Peptides 1-3 were assembled from selected blocked fragments that were synthesized by the polymeric-reagent method, using PHBT (polystyrene-bound 1-hydroxybenzotriazole) as the activating polymer. The ability of peptides 1-3 to enhance the activation (RNA synthesis) and proliferation (DNA synthesis) of human T lymphocytes was determined. In comparison to thymosin alpha 1, thymosin alpha 1 (15-28), and thymopentin, peptides 1-3 did not show significant enhancement of these processes.
Mokotoff
M
M
Department of Pharmaceutical Sciences, School of Pharmacy, University of Pittsburgh, Pennsylvania 15261.
Zhao
M
M
Roth
S M
SM
Shelley
J A
JA
Slavoski
J N
JN
Kouttab
N M
NM
D000595:Amino Acid Sequence; D055598:Chemical Phenomena; D002621:Chemistry; D004247:DNA / Q000096:biosynthesis; D006801:Humans; D007202:Indicators and Reagents; D008969:Molecular Sequence Data; D010446:Peptide Fragments / Q000494:pharmacology; D010455:Peptides / Q000138:chemical synthesis / Q000494:pharmacology*; D011137:Polystyrenes; D012313:RNA / Q000096:biosynthesis; D013601:T-Lymphocytes / Q000187:drug effects* / Q000378:metabolism; D000077596:Thymalfasin; D016305:Thymopentin; D013946:Thymopoietins / Q000494:pharmacology; D013947:Thymosin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D014230:Triazoles
D007202:Indicators and Reagents; D010446:Peptide Fragments; D010455:Peptides; D011137:Polystyrenes; D013946:Thymopoietins; D014230:Triazoles; D013947:Thymosin; D012313:RNA; D004247:DNA; C011852:1-hydroxybenzotriazole; D016305:Thymopentin; D000077596:Thymalfasin