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001-es BibID:	BIBFORM078151
035-os BibID:	(PMID)1527783
Első szerző:	Balajthy Zoltán (biokémikus, sejtbiológus)
Cím:	Synthesis and functional evaluation of a peptide derivative of 1-beta-D-arabinofuranosylcytosine / Zoltán Balajthy, János Aradi, Ildikó T. Kiss, Pál Elődi
Dátum:	1992
Megjegyzések:	We have synthesized a peptidyl prodrug derivative of 1-beta-D-arabinofuranosylcytosine (1) designed to be a selective substrate of plasmin. D-Val-Leu-Lys-ara-C (2) was obtained by coupling the protected peptide Cbz-D-Val-Leu-(N6-Cbz)Lys-OH and ara-C (1) by a water-soluble carbodiimide (EDCI), followed by the removal of the Cbz groups by using catalytic hydrogenolysis over Pd/C. The kinetic constant of hydrolysis of 2 in the presence of plasmin demonstrated effective release of 1. The amino group of 1, which is sensitive to the removal by cytidine deaminase, is protected in 2 by the formation of the amide bond resulting in a prolonged half-life of 2 in biological milieu. The antiproliferative efficiency of 2 against L1210 leukemic cells was significantly higher than that of 1. The activity of 2 was abolished in the presence of serine proteinase inhibitor, (4-amidinopheny)methanesulfonyl fluoride. These data indicate that 2 is a prodrug form of 1 in systems generating plasmin.
Tárgyszavak:	Orvostudományok Elméleti orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban
Megjelenés:	Journal of Medicinal Chemistry. - 35 : 18 (1992), p. 3344-3349. -
További szerzők:	Aradi János (1942-) (biokémikus, vegyész) Kiss Ildikó (biokémikus) Elődi Pál (1927-2002) (biokémikus)
Internet cím:	Intézményi repozitóriumban (DEA) tárolt változat DOI
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