Synthesis of poly(ethylene glycol)-based saquinavir prodrug conjugates and assessment of release and anti-HIV-1 bioactivity using a novel protease inhibition assay.

Abstract

Various poly(ethylene glycol)(PEG)-based prodrug conjugates of the HIV-1 protease inhibitor (PI) saquinavir (SQV) were prepared using several types of chemical groups potentially capable of modifying its pharmacokinetic properties. These prodrug conjugates included SQV-cysteine-PEG3400, SQV-cysteine-PEG3400-biotin, SQV-cysteine(R.I.CK-Tat9) [a cationic… (More)

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@article{Gunaseelan2004SynthesisOP, title={Synthesis of poly(ethylene glycol)-based saquinavir prodrug conjugates and assessment of release and anti-HIV-1 bioactivity using a novel protease inhibition assay.}, author={Simi Gunaseelan and Olivia Debrah and Li Wan and Michael J. Leibowitz and Arnold B. Rabson and Stanley M. Stein and Patrick J. Sinko}, journal={Bioconjugate chemistry}, year={2004}, volume={15 6}, pages={1322-33} }