Drug targeting by macromolecules without recognition unit?

Abstract

his review will summarize available information on the ability of macromolecular conjugates containing no specific recognition motifs to deliver anthracyclines (daunomycin, adriamycin) or methotrexate to target cells such as tumour cells or macrophages. Conjugates with natural (proteins, DNA, carbohydrates) and synthetic macromolecules (linear and branched chain poly-alpha-amino acids, non-biodegradable DIVEMA, HPMA etc.) will be reviewed. Experimental data from several laboratories indicate that these conjugates are taken up by cells mainly by fluid-phase or adsorptive endocytosis. It is believed that these processes do not involve 'specific receptors'. Two examples of methotrexate and daunomycin conjugates will be discussed to show the effect of the chemical structure of branched chain polypeptides on the uptake and antitumour or antiparasitic (Leishmania donovani infection) efficacy of conjugates.

Biokonjugátumok – összefogni érdemes

“…34,35,36,37 Új kísérleteinkben, az ErbB2 receptor ligandumát az LTVSPWY oligopeptidet és Dau-t tartalmazó konjugátum állítottunk elõ. 38 Az ErbB2 receptor fokozott expresszióját figyelték meg bizonyos (pl.…”

Synthesis of daunomycin-oligoarginine conjugates and their effect on human leukemia cells (HL-60)

“…6 Conjugation with oligopeptides (e.g. cell-penetrating peptides) 7 or macromolecules 8,9 can be considered as a novel, alternative approach.…”

Ketotifen controlled release from cellulose acetate propionate and cellulose acetate butyrate membranes

“…The application of controlled release systems, in which biologically active substances are released to their environment with controllable rates, has recently grown enormously. The controlled administration of chemicals or drugs is widely publicised in the field of medicine and pharmacy, agriculture, food industry and biotechnology [1][2][3][4][5].…”