Abstract |
Nigrin b and ebulin l are type 2 ribosome-inactivating proteins (RIPs) with 10(4) times less cellular and in vivo toxicity than ricin that are currently being considered for the construction of anti- cancer conjugates. Here we provide evidence that both RIPs can be used for the construction of conjugates directed to a target such as the transferrin receptor (TfR), which is over-expressed in cancer cells. Nigrin b- and ebulin l- transferrin conjugates were constructed with no substantial reduction in the translational inhibitory molecular activity of either RIPs. Conjugation with transferrin decreased the IC(50) of the proteins from 3 x 10(-7)M ( nigrin b) and 1.5 x 10(-8)M (ebulin l) to 3.5 x 10(-10)M in HeLa cells. Thus, both conjugates could be considered as useful tools for targeting TfR-over-expressing cancer cells.
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Authors | Lucía Citores, J Miguel Ferreras, Raquel Muñoz, Jorge Benítez, Pilar Jiménez, Tomás Girbés |
Journal | Cancer letters
(Cancer Lett)
Vol. 184
Issue 1
Pg. 29-35
(Oct 08 2002)
ISSN: 0304-3835 [Print] Ireland |
PMID | 12104045
(Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Plant Proteins
- Protein Synthesis Inhibitors
- Receptors, Transferrin
- Ribosome Inactivating Proteins, Type 2
- Transferrin
- ebulin r protein, Sambucus ebulus
- N-Glycosyl Hydrolases
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Topics |
- Animals
- Drug Delivery Systems
- HeLa Cells
(drug effects, metabolism)
- Humans
- N-Glycosyl Hydrolases
(pharmacology)
- Plant Proteins
(pharmacology)
- Protein Synthesis Inhibitors
(pharmacology)
- Rabbits
- Receptors, Transferrin
(metabolism)
- Ribosome Inactivating Proteins, Type 2
- Transferrin
(pharmacology)
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