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PolExGene meeting August, 23-24 2007 Helsinki. CNRS Montpellier (France) Max Mousseron Institute of Biomolecules Pr. Jean Martinez, Dr. Muriel Amblard Dr. Gilles Subra. WP 2 : Synthesis of Selected CPP. WP 3 : Synthesis of Selected CIP. Ac-Tat(Arg 3,4 ). Tat(48-60). Tat(Arg 3,4 ).
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PolExGene meeting August, 23-24 2007 Helsinki CNRS Montpellier (France) Max Mousseron Institute of Biomolecules Pr. Jean Martinez, Dr. Muriel Amblard Dr. Gilles Subra WP 2 : Synthesis of Selected CPP WP 3 : Synthesis of Selected CIP
Ac-Tat(Arg3,4) Tat(48-60) Tat(Arg3,4) H-GRKKRRQRRRPPQ-OH H-GRRRRRQRRRPPQ-OH Ac-GRRRRRQRRRPPQ-OH Acetyl-Tat Ac-GRKKRRQRRRPPQ-OH Cell Penetrating Peptide Synthesis Peptides deriving from protein transduction domain Tat Tat-NH2 H-GRKKRRQRRRPPQ-NH2 JMV3535 (Alain) Acetyl-Tat-NH2 Ac-GRKKRRQRRRPPQ-NH2 JMV3536 (Alain) Acetyl-Tat(48-57)-NH2 Ac-GRKKRRQRRR-NH2 JMV3484 (Alain) Tat(48-57) H-GRKKRRQRRR-OH JMV3481 (Alain) JMV3508 (Alain) JMV3509 (Alain)
Cell Penetrating Peptide Synthesis Polyarginine-based peptides H-(Arg)8-NH2 H-RRRRRRRR-NH2 JMV3506 (Alain) Ac-(Arg)8-NH2 Ac-RRRRRRRR-NH2 JMV3507 (Alain) Ac-Cys-(Arg)8-NH2 Ac-Cys-RRRRRRRR-NH2 (Peter) Ac-(Arg)8-OH Ac-RRRRRRRR-OH JMV3482 (Alain) Ac-(Arg)11-OH Ac-RRRRRRRRRRR-OH JMV3483 (Alain)
Cell Interacting Peptide Synthesis RGD-based peptides H-Cys-Gly-Gly-Arg-Gly-Asp-Ser-OH JMV3622 (Peter) JMV3619 cyclo[Arg-Gly-Asp-(D)Phe-Lys(H-Cys-Gly-Gly-) (Peter)
Polyplexes assembly strategies (I) Unprotected Peptide (CIP, CPP…) Polymer Chemoselective reation Example:
Polyplexes assembly strategies (II) Protected Peptide (CIP, CPP…) Polymer P P P P Coupling reaction P P P P deprotection P Example: P
Needs of PolExGene Partners CPP and CIP Type (tat, Arg, penetratin, others?) Other specific CIPs ? Fonctionnalisation? Protection?