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Poly(ethylene glycol) multiblock copolymer as a carrier of anti-cancer drug doxorubicin

Michal Pechar, Karel Ulbrich, Vladimír Šubr, Leonard W Seymour and Etienne Schacht (2000) BIOCONJUGATE CHEMISTRY. 11(2). p.131-139
abstract
The synthesis of a novel water-soluble polymer drug carrier system based on biodegradable poly(ethylene glycol) block copolymer is described in this paper. The copolymer consisting of PEG blocks of molecular weight 2000 Linked by means of an oligopeptide with amino end groups was prepared by interfacial polycondensation of the diamine and PEG bis(succinimidyl carbonate). The structure of the oligopeptide diamine consisting of glutamic acid and lysine residues was designed as a substrate for cathepsin B, a lysosomal enzyme, which was assumed to be one of the enzymes responsible for the degradation of the polymer carrier in vivo. Each of the oligopeptide blocks incorporated in the carrier contained three carboxylic groups of which some were used for attachment of an anti-cancer drug, doxorubicin (Dox), via a tetrapeptide spacer Gly-Phe-Leu-Gly. This tetrapeptide spacer is susceptible to enzymatic hydrolysis. In vitro release of Dox and the degradation of the polymer chain by cathepsin B as well as preliminary evaluation of in vivo anti-cancer activity of the conjugate are also demonstrated.
Please use this url to cite or link to this publication:
author
organization
year
type
journalArticle (original)
publication status
published
subject
keyword
BLOCK-COPOLYMERS, ACID ENANTIOMERS, AMINO-ACID, DERIVATIZATION, POLYMERS
journal title
BIOCONJUGATE CHEMISTRY
Bioconjugate Chem.
volume
11
issue
2
pages
131 - 139
Web of Science type
Article
Web of Science id
000086023400001
ISSN
1043-1802
DOI
10.1021/bc990092l
language
English
UGent publication?
yes
classification
A1
id
124583
handle
http://hdl.handle.net/1854/LU-124583
date created
2004-01-14 13:36:00
date last changed
2016-12-19 15:37:49
@article{124583,
  abstract     = {The synthesis of a novel water-soluble polymer drug carrier system based on biodegradable poly(ethylene glycol) block copolymer is described in this paper. The copolymer consisting of PEG blocks of molecular weight 2000 Linked by means of an oligopeptide with amino end groups was prepared by interfacial polycondensation of the diamine and PEG bis(succinimidyl carbonate). The structure of the oligopeptide diamine consisting of glutamic acid and lysine residues was designed as a substrate for cathepsin B, a lysosomal enzyme, which was assumed to be one of the enzymes responsible for the degradation of the polymer carrier in vivo. Each of the oligopeptide blocks incorporated in the carrier contained three carboxylic groups of which some were used for attachment of an anti-cancer drug, doxorubicin (Dox), via a tetrapeptide spacer Gly-Phe-Leu-Gly. This tetrapeptide spacer is susceptible to enzymatic hydrolysis. In vitro release of Dox and the degradation of the polymer chain by cathepsin B as well as preliminary evaluation of in vivo anti-cancer activity of the conjugate are also demonstrated.},
  author       = {Pechar, Michal and Ulbrich, Karel and \v{S}ubr, Vladim{\'i}r and Seymour, Leonard W and Schacht, Etienne},
  issn         = {1043-1802},
  journal      = {BIOCONJUGATE CHEMISTRY},
  keyword      = {BLOCK-COPOLYMERS,ACID ENANTIOMERS,AMINO-ACID,DERIVATIZATION,POLYMERS},
  language     = {eng},
  number       = {2},
  pages        = {131--139},
  title        = {Poly(ethylene glycol) multiblock copolymer as a carrier of anti-cancer drug doxorubicin},
  url          = {http://dx.doi.org/10.1021/bc990092l},
  volume       = {11},
  year         = {2000},
}

Chicago
Pechar, Michal, Karel Ulbrich, Vladimír Šubr, Leonard W Seymour, and Etienne Schacht. 2000. “Poly(ethylene Glycol) Multiblock Copolymer as a Carrier of Anti-cancer Drug Doxorubicin.” Bioconjugate Chemistry 11 (2): 131–139.
APA
Pechar, M., Ulbrich, K., Šubr, V., Seymour, L. W., & Schacht, E. (2000). Poly(ethylene glycol) multiblock copolymer as a carrier of anti-cancer drug doxorubicin. BIOCONJUGATE CHEMISTRY, 11(2), 131–139.
Vancouver
1.
Pechar M, Ulbrich K, Šubr V, Seymour LW, Schacht E. Poly(ethylene glycol) multiblock copolymer as a carrier of anti-cancer drug doxorubicin. BIOCONJUGATE CHEMISTRY. 2000;11(2):131–9.
MLA
Pechar, Michal, Karel Ulbrich, Vladimír Šubr, et al. “Poly(ethylene Glycol) Multiblock Copolymer as a Carrier of Anti-cancer Drug Doxorubicin.” BIOCONJUGATE CHEMISTRY 11.2 (2000): 131–139. Print.