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  • Title: Synthesis of oligotuftsin-based branched oligopeptide conjugates for chemotactic drug targeting.
    Author: Mezö G, Láng O, Jakab A, Bai KB, Szabó I, Schlosser G, Láng J, Köhidai L, Hudecz F.
    Journal: J Pept Sci; 2006 May; 12(5):328-36. PubMed ID: 16245264.
    Abstract:
    The synthesis and chemotactic properties of a new class of branched oligopeptide-based conjugates are described. Tetratuftsin derivatives containing chemotactic formyl tripeptides (For-MLF, For-NleLF or For-MMM) in branches were prepared by stepwise solid-phase peptide synthesis. The influence of the composition and ionic charge of the carrier-branched oligopeptide on the chemotactic behaviour of the conjugate was studied in Tetrahymena pyriformis. Conjugates with methotrexate (Mtx) as a drug component was also prepared. For this, a GFLGC spacer, cleavable by cathepsin B, was used. The spacer with N-terminal methotrexate was coupled to the chloroacetylated chemotactic carrier molecule by thioether bond formation. The chemotactic activity and cytotoxity of Mtx conjugates were also studied.
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