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PolExGene meeting February, 8-9 2007 Paris, ENS

PolExGene meeting February, 8-9 2007 Paris, ENS. 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. Cell Penetrating Peptide Synthesis

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PolExGene meeting February, 8-9 2007 Paris, ENS

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  1. PolExGene meeting February, 8-9 2007 Paris, ENS 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

  2. Cell Penetrating Peptide Synthesis (in progress) mixing purpose Polyarginine-based peptides H-(Arg)8-OH H-RRRRRRRR-OH H-(Arg)8-NH2 H-RRRRRRRR-NH2 Ac-(Arg)8-OH Ac-RRRRRRRR-OH Ac-RRRRRRRR-NH2 Ac-(Arg)8-NH2 Idem with poly Arg11

  3. Peptide synthesis and purification

  4. Nter Cys peptides for maleimide ligation or SS bond Cter Cys peptides for maleimide ligation or SS bond H- or Ac-Cys-RQIKIWFQNRRMKWKK-OH H- or Ac-RQIKIWFQNRRMKWKK-Cys-OH H- or Ac-Cys-GRKKRRQRRRPPQ-OH H- or Ac-GRKKRRQRRRPPQ-Cys-OH H- or Ac-Cys-RRRRRRRR-OH H- or Ac-RRRRRRRR-Cys-OH N-hydroxysuccinimide peptide (covalent link) Protected-(RQIKIWFQNRRMKWKK)-NHS Protected-(GRKKRRQRRRPPQ)-NHS Protected-RRRRRRRR-NHS Cell Penetrating Peptide for covalent anchoring on cationic polymers (proposition) Rem: Cys can be repaced by simpler thiol containg group

  5. Other Perspectives • ‘Tagged’ CPP N-ter, C-ter or within chain (FTIC, others?, Qdot?) • Modified CPP Penetratin, Tat or polyarginine Bioavailability beta-peptides Peptoids • Selectionof CIP Specific sequences for specific receptors: RGD? Other specific ligands?

  6. Needs of PolExGene Partners CPP and CIP Type (tat, Arg, penetratin, others?) Quantity? Purity? Number of analogues (only one?) Fonctionnalisation? Protection?

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