Cell-penetrating peptides: classes, origin, and current landscape.

Francesca Milletti

Hoffmann-La Roche Inc., pRED Informatics, 340 Kingsland Street, Nutley, NJ, USA. francesca.milletti@roche.com

Drug discovery today 2012 Aug

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With more than ten new FDA approvals since 2001, peptides are emerging as an important therapeutic alternative to small molecules. However, unlike small molecules, peptides on the market today are limited to extracellular targets. By contrast, cell-penetrating peptides (CPPs) can target intracellular proteins and also carry other cargoes (e.g. other peptides, small molecules or proteins) into the cell, thus offering great potential as future therapeutics. In this review I present a classification scheme for CPPs based on their physical-chemical properties and origin, and I provide a general framework for understanding and discovering new CPPs. Copyright © 2012 Elsevier Ltd. All rights reserved.