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Practical synthesis of the therapeutic leads tigilanol tiglate and its analogues
Tigilanol tiglate is a therapeutic lead for the treatment of a broad range of cancers. Now, it has been shown that tigilanol tiglate can be synthesized in a time and step economical fashion from phorbol—its naturally abundant biosynthetic precursor. This synthesis provides rapid access to analogues with unprecedented protein kinase C binding activity.
- Paul A. Wender
- , Zachary O. Gentry
- & Edward Njoo
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Article
| Open AccessControlled masking and targeted release of redox-cycling ortho-quinones via a C–C bond-cleaving 1,6-elimination
A strategy for protecting redox-active ortho-quinones, which show promise as anticancer agents but suffer from redox-cycling behaviour and systemic toxicity, has been developed. The ortho-quinones are derivatized to redox-inactive para-aminobenzyl ketols. Upon amine deprotection, an acid-promoted, self-immolative C–C bond-cleaving 1,6-elimination releases the redox-active hydroquinone. The strategy also enables conjugation to a carrier for targeted delivery of ortho-quinone species.
- Lavinia Dunsmore
- , Claudio D. Navo
- & Gonçalo J. L. Bernardes
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Tricyclic cell-penetrating peptides for efficient delivery of functional antibodies into cancer cells
Reliable intracellular delivery of antibodies is one of the grand challenges in biomedical research, with the potential to address unmet clinical needs or to enable basic research. Now, it has been shown that tricyclic peptide complexes can transport functional antibodies into the cytoplasm and nucleus of cells to specifically target intracellular proteins.
- Ole Tietz
- , Fernando Cortezon-Tamarit
- & Katherine A. Vallis
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Switching on prodrugs using radiotherapy
Prodrugs offer one route to treat cancer, but they require activation once they have been delivered to the tumour. Now, a simultaneous chemo-radiotherapy strategy has been demonstrated in mice that uses gamma or X-ray irradiation to locally activate an anticancer prodrug.
- Jin Geng
- , Yichuan Zhang
- & Mark Bradley
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News & Views |
Expanding the effectiveness of screening
DNA-encoded libraries are a powerful tool to identify hit compounds for drug discovery. Now, two papers have reported new advances in this technology. One paper reports a method to screen for binders inside a living cell, and the other investigates the effects of stereo- and regiochemistry on ligand discovery.
- Minsoo Song
- & Gil Tae Hwang
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News & Views |
Plastic antibodies for cancer therapy?
Monoclonal antibodies have shown tremendous success in cancer treatment; however, humanization for clinical applications is expensive and not straightforward. Now, molecularly imprinted polymer nanogels have been developed that can block cell-surface proteins and disrupt tumour spheroids.
- Alessandra Maria Bossi