Site-specific PEGylation endows a mammalian ribonuclease with antitumor activity
نویسندگان
چکیده
منابع مشابه
Site-specific PEGylation endows a mammalian ribonuclease with antitumor activity.
Mammalian ribonucleases are emerging as cancer chemotherapeutic agents. Their cationicity engenders cell permeability, and their enzymatic activity destroys the biochemical information encoded by RNA. The pharmacologic potential of ribonucleases is, however, obviated by their high sensitivity to a cytosolic inhibitor protein (RI) and their small size, which limits their residence in serum. We r...
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In this study, N-terminal site-specific mono-PEGylation of the recombinant lidamycin apoprotein (rLDP) of lidamycin (LDM) was prepared using a polyethyleneglycol (PEG) derivative (M w 20 kDa) through a reactive terminal aldehyde group under weak acidic conditions (pH 5.5). The biochemical properties of mPEG-rLDP-AE, an enediyne-integrated conjugate, were analyzed by SDS-PAGE, RP-HPLC, SEC-HPLC ...
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Angiogenin (ANG) promotes the formation of blood vessels in animals. This hormone is a small, monomeric protein that is homologous to bovine pancreatic ribonuclease A (RNase). ANG is a poor ribonuclease but its ribonucleolytic activity is essential for its angiogenic activity. RNase is not angiogenic. A hybrid protein was produced in which 13 residues of a divergent surface loop of ANG were sub...
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Despite the critical role of erythropoietin (EPO) as therapeutic agent in treatment of anemia, its consumption is limited due to several disadvantages including the product short half-life, immunogenicity and susceptibility to proteolytic degradation. To overcome these drawbacks efficient methods such as site-specific PEGylation have been developed among witch N-terminal PEGylation has found mo...
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Site-specific cross-linking can generate homogeneous multimeric proteins of defined valency. Pancreatic-type ribonucleases are an especially attractive target, as their natural dimers can enter mammalian cells, evade the cytosolic ribonuclease inhibitor (RI), and exert their toxic ribonucleolytic activity. Here, we report on the use of eight distinct thiol-reactive cross-linking reagents to pro...
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ژورنال
عنوان ژورنال: Cancer Biology & Therapy
سال: 2011
ISSN: 1538-4047,1555-8576
DOI: 10.4161/cbt.12.3.15959