Part I
Classes and Prediction of Cell-Penetrating
Peptides ...................................................... 1
Ülo Langel
Chapter 1
Penetratins ..................................................... 5
Edmond Dupont, Alain Prochiantz, and Alain Joliot
Chapter 2
Tat-Derived Cell-Penetrating Peptides: Discovery, Mechanism
of Cell Uptake, and Applications to the Delivery of
Oligonucleotides ............................................... 29
Said Abes, Jean-Philippe Richard, Alain Thierry,
Philippe Clair, and Bernard Lebleu
Chapter 3
Model Amphipathic Peptides ..................................... 43
Johannes Oehlke, Burkhard Wiesner, and Michael Bienert
Chapter 4
Cell-Penetrating cis-γ-Amino-L-Proline-Derived Peptides ........ 61
Josep Farrera-Sinfreu, Ernest Giralt, Miriam Royo, and
Fernando Albericio
Chapter 5
Prediction of Cell-Penetrating Peptides ........................ 77
Mattias Hällbrink and Ülo Langel
Part II
Mechanisms of Cell-Penetrating Peptides .............. 87
Astrid Gräslund
Chapter 6
Inverted Lipid Models: A Pathway for Peptide
Internalization? ............................................... 89
Gérard Chassaing, Sandrine Sagan, Olivier Lequin,
Antonin Lamaziere, Jesus Ayala-Sanmartin, Germain Trugnan,
Gérard Bolbach, and Fabienne Burlina
Chapter 7
Membrane Interactions of Cell-Penetrating Peptides ............ 109
Elin K. Esbjörner, Astrid Gräslund, and Bengt Nordén
Chapter 8
Interactions of Cell-Penetrating Peptides with Model
Membranes ..................................................... 139
Sebastien Deshayes, May C. Morris, Gilles Divita, and
Frédéric Heitz
Chapter 9
The Import Mechanism of Cationic Cell-Penetrating Peptides
and Its Implications for the Delivery of Peptide Inhibitors
of Signal Transduction ........................................ 161
Mariola Fotin-Mleczek, Söhnke Voss, and Roland Brock
Chapter 10
Mechanisms of Cargo Delivery by Transportans .................. 183
Margus Pooga, Kärt Padari, and Ülo Langel
Chapter 11
Tat-Mediated Peptide/Protein Transduction In Vivo ............. 201
Wenge Shi and Steven F. Dowdy
Chapter 12
Proteoglycans as Endocytosis Receptors for CPPs ............... 219
Mattias Belting, Anders Wittrup, and Staffan Sandgren
Part III
Functionality of Shuttling Proteins and
Protein-Derived Peptides ................................ 235
Alain Prochiantz
Chapter 13
Cell Permeable Peptides and Messenger Proteins, from
a Serendipitous Observation to a New Signaling Mechanism ...... 239
Alain Prochiantz
Chapter 14
Pharmacology and In Vivo Efficacy of Pepducins in Hemostasis
and Arterial Thrombosis ....................................... 245
Lidija Covic, Boris Tchernychev, Suzanne Jacques, and Athan
Kuliopulos
Chapter 15
H0XB4 Homeoprotein Transfer Promotes the Expansion of
Hematopoietic Stem Cells ...................................... 259
Sophie Amsellem and Serge Fichelson
Chapter 16
Applications of Cell-Penetrating Peptides as Signal
Transduction Modulators ....................................... 273
Sarah Jones and John Howl
Chapter 17
SynB Vectors as Drug Carriers ................................. 293
Jamal Temsamani
Part IV
Applications of Cell-Penetrating Peptides in
Gene Modulation and Protein Transport ................ 309
Steven F. Dowdy
Chapter 18
Peptide Conjugates of Oligonucleotide Analogs and siRNA for
Gene Expression Modulation .................................... 313
John J. Turner, Andrey A. Arzumanov, Gabriela Ivanova,
Martin Fabani, and Michael J. Gait
Chapter 19
Lego-Like Strategy for Assembling Multivalent Peptide-Based
Vehicles Able to Deliver Molecular Cargoes into Cells ......... 329
Stephen A. Waschuk, Gregory M.K. Poon, and Jean Gariepy
Chapter 20
Mechanistic Insights into Guanidinium-Rich Transporters
Entering Cells ................................................ 353
Jonathan B. Rothbard, Theodore C. Jessop, Lisa Jones, Elena
Goun, Rajesh Shinde, Christopher H. Contag, and Paul A. Wender
Chapter 21
Cell-Penetrating Short Interfering RNAs and Decoy
Oligonucleotides .............................................. 375
Samir El-Andaloussi, Henrik Johansson, Pontus Lundberg, and
Ülo Langel
Chapter 22
A Noncovalent Peptide-Based Strategy for Peptide and
Short Interfering RNA Delivery ................................ 387
May C. Morris, Sébastien Deshayes, Federica Simeoni,
Gudrun Aldrian-Herrada, Frédéric Heitz, and Gilles Divita
Part V
Selective Targeting to Tumors and Other Tissues
with Cell-Penetrating Peptides: In Vivo
Applications ............................................... 409
Ernst Wagner
Chapter 23
Selective Delivery to Vascular Addresses: In Vivo Applications
of Cell-Type-Specific Cell-Penetrating Peptides ............... 413
Pirjo Laakkonen and Erkki Ruoslahti
Chapter 24
In Vivo Applications of Cell-Penetrating Peptides ............. 423
Sterghios Moschos, Andrew Williams, and Mark A. Lindsay
Chapter 25
Intracellular Delivery of Nanoparticles with CPPs ............. 439
Bhawna Gupta and Vladimir P. Torchilin
Chapter 26
Strategies to Incorporate CPPs into Synthetic Viruses for
Tumor-Targeted Gene Therapy ................................... 455
Ernst Wagner and Manfred Ogris
Chapter 27
Cell-Permeable Penta-Peptides Derived from Bax-Inhibiting
Peptide ....................................................... 469
Jose A. Gomez, Vivian Gama, and Shigemi Matsuyama
Chapter 28
Cellular Uptake of Liposomal and Micellar Carriers Mediated
by ApoE-Derived Peptides ...................................... 483
Margitta Dathe, Sandro Keller, Ines Sauer, and Michael
Bienert
Chapter 29
Imaging the Influx of Cell-Penetrating Peptides into
the Cytosol of Individual Live Cells .......................... 505
Stephen R. Adams and Roger Y. Tsien
Chapter 30
Microbial Membrane-Penetrating Peptides and Their
Applications .................................................. 515
Anita Ganyu, Ülo Langel, and Liam Good
Part VI
CPP Methods ................................................ 535
Chapter 31
Design and Synthesis of Cell-Penetrating Peptides ............. 537
Yang Jiang, Ursel Soomets, and Ülo Langel
Chapter 32
Toxicity Methods for Cell-Penetrating Peptides ................ 553
Külliki Saar and Ülo Langel
Chapter 33
Methods to Study the Translocation of Cell-Penetrating
Peptides ...................................................... 567
Maria Lindgren, Margus Pooga, and Ülo Langel
Index ......................................................... 589
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