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

(2000) BIOCONJUGATE CHEMISTRY. 11(2). p.131-139
Author
Organization
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.
Keywords
BLOCK-COPOLYMERS, ACID ENANTIOMERS, AMINO-ACID, DERIVATIZATION, POLYMERS

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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.
@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},
}

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