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

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.