Bioactive cell penetrating peptides and proteins in cancer: a bright future ahead

•Many key engines of cancer remain undruggable by conventional approaches.•Therapeutic peptides and proteins promise to drug challenging cancer targets.•Internalization sequences can be identified or engineered in bioactive molecules.•Chemistry and drug humanization can overcome some challenges to c...

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Bibliographic Details
Published in:Current opinion in pharmacology 2019-08, Vol.47, p.133-140
Main Authors: Jauset, Toni, Beaulieu, Marie-Eve
Format: Article
Language:English
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Summary:•Many key engines of cancer remain undruggable by conventional approaches.•Therapeutic peptides and proteins promise to drug challenging cancer targets.•Internalization sequences can be identified or engineered in bioactive molecules.•Chemistry and drug humanization can overcome some challenges to clinical viability. Peptides and proteins bear an extraordinary therapeutic potential to effectively and selectively target many components of cells currently considered undruggable. However, their intracellular delivery remains a critical challenge. Cell penetrating peptides and protein domains (CPPs) can be employed to translocate therapeutic polypeptides through the cellular membrane. Here, we describe examples of linear peptides and proteins, byciclic macropeptides and nanobodies that target key players in cancer development, with intrinsic and engineered cell penetrating ability. We also describe current solutions to the main challenges to their clinical viability.
ISSN:1471-4892
1471-4973
DOI:10.1016/j.coph.2019.03.014