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Titolo:
OPTIMIZATION OF THE REACTION CONDITIONS FOR THE SYNTHESIS OF NEOGLYCOPROTEIN-AZT-MONOPHOSPHATE CONJUGATES
Autore:
KUIPERS ME; SWART PJ; HENDRIKS MMWB; MEIJER DKF;
Indirizzi:
GIDS,PHARMACOKINET & DRUG DELIVERY SECT,ANTONIUS DEUSINGLAAN 2 9713 AW GRONINGEN NETHERLANDS UNIV GRONINGEN,CTR PHARM,PHARMACOKINET & DRUG DELIVERY SECT 9713 AW GRONINGEN NETHERLANDS RES GRP CHEMOMETR 9713 AW GRONINGEN NETHERLANDS
Titolo Testata:
Journal of medicinal chemistry
fascicolo: 6, volume: 38, anno: 1995,
pagine: 883 - 889
SICI:
0022-2623(1995)38:6<883:OOTRCF>2.0.ZU;2-X
Fonte:
ISI
Lingua:
ENG
Soggetto:
LACTOSAMINATED ALBUMIN; ANTIVIRAL DRUGS; ZIDOVUDINE AZT; ARA-AMP; PROTEIN; AIDS; ERYTHROCYTES; THERAPY; CELLS; HIV;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
31
Recensione:
Indirizzi per estratti:
Citazione:
M.E. Kuipers et al., "OPTIMIZATION OF THE REACTION CONDITIONS FOR THE SYNTHESIS OF NEOGLYCOPROTEIN-AZT-MONOPHOSPHATE CONJUGATES", Journal of medicinal chemistry, 38(6), 1995, pp. 883-889

Abstract

The coupling of the monophosphate derivative of 3-azido-2,3-dideoxythymidine (AZTMP) to glycoproteins by water soluble carbodiimide l-3-[3-(dimethylamino)propyl]-3-ethylcarbodiimide) was greatly improved, relative to a recently reported method, by using also N-hydroxysulfosuccinimide (NHS) in the conjugation reaction. The hydrolysis of the activated AZTMP intermediate, responsible for the low degree of conjugation in the earlier method, could be delayed considerably if the activated phosphate group was converted into an activated ester by addition of NHS. In order to minimize the use of compounds needed for the preparation of AZTMP-protein conjugates, the present study was undertaken to determine if the reaction conditions could be optimized such that a conjugate with 2 AZTMP molecules/mol of neoglycoprotein would result. In addition a low proportion of cross-linked conjugates was desired. Optimization was achieved studying the shape of three-dimensional response surfaces, in which the degree of AZTMP coupling and the percentage of monomeric conjugates were regarded as the relevant responses. It appeared that the optimal conditions for coupling 1-2 mol of AZTMP to 1 mol of glycoprotein were an incubation time of 30 h, an AZTMP amount of 4 mg, an NHS amount between 8 and 15 mg, and a glycoprotein amount of 50mg.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/07/20 alle ore 15:07:26