UE Bio-targeted chemistry 1

Course outline:

This course describes synthetic approaches and methods for: the synthesis of library of small[1]molecules, the assembly of peptide and analogs, the engineering of molecular conjugates of biomolecules, and the applications of that family of molecules in therapeutics, diagnostics and nanotechnologies (i.e. biosensors).

Details:

1/ Peptides and protein engineering

I.Structural aspects

II.Synthetic strategies (SPPS, fragment synthesis, native ligation)

III.Applications in vectorization (Monoclonal antibodies, cell-penetrating peptides, peptide ligands, nanoparticles)

IV.Antimicrobial peptides, toxins

V.Pseudopeptides

2/ Chemical ligation

I. The different reactions

II.Multiple chemoselective ligations

III.Installing bioorthogonal functionality into target biomolecules

IV.In vivo click chemistry

3/ Combinatorial chemistry

I. Drug Discovery

II.Synthetic strategies (combinatorial vs parallel synthesis; solid vs supported synthesis)

III.Dynamic Combinatorial Chemistry / Target guided synthesis

4/ Biosensors

I. Medicinal, environment and food safety applications

II.Biomolecules for molecular recognition

III.Chemical modifications for immobilization and transduction

Prerequisites: Organic chemistry, Peptide synthesis (M1 Master Program CHI703, CHI832).

Skills:

Chemical methods for ligations of complex biomolecules (peptides, oligonucleotides and carbohydrates), applications in biosensor. Combinatorial chemistry: principles / techniques/ applications. Reactivity, synthetic methods and applications of peptides.