Cell Penetrating Peptides (CPPs)

Dear Colleagues,

In less than 25 years, Cell Penetrating Peptides (CPPs) have progressed from challenging a paradigm to entering clinical trials, with at least two candidates reaching Phase III. Counterintuitively, though charged molecules and hydrophilic biopolymers are inherently prevented from crossing phospholipid bilayers, CPPs, peptide sequences 5- to 30-amino acid long generally displaying high net charges, possess the ability to efficiently translocate cell membranes and deliver a broad range of cargoes intracellularly.

The capacity of CPPs to reach intracellular targets significantly expand the pharmacological target space: 60% of current drug targets, addressed essentially by low molecular weight agents, are extracellular, but cell surface proteins represent only 22% of the proteins encoded by the human genome and a 2 to 30 fold increase in the number of drug targets could arise from the sequencing of the human genome. Also, biologics, macromolecular agents with limited membrane translocation abilities, are becoming one of the fastest growing classes of new therapeutics, accounting already for 20–25% of all new drug approvals.

CPPs can transport low molecular weight agents, proteins, nucleic acids, polymers, nanoparticles and liposomes through cell membranes and also through the blood–brain barrier. Furthermore, their interest is not limited to a wealth of potential therapeutic and/or imaging applications, they are also fundamental tools to study cell membrane dynamics and structure, including curvature, and cell entry mechanisms. CPPs have been instrumental in the implementation and development of biochemical, biophysical and functional assays and of molecular dynamic simulations, in experiments delineating the structural requirements for cell internalisation. Potentially permeating cells indiscriminately, CPPs can also achieve three levels of targeting selectivities, tissue, cell and organelle.

Prof. Dr. Marc Devocelle
Gest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

• intracellular delivery
• membrane dynamics
• endocytosis, direct translocation
• cationic, amphipathic, hydrophobic properties
• molecular, biological, supramolecular cargoes

• Cell Penetrating Peptides (CPPs) in Molecules (5 articles)