Heparan Sulfate (HS), a member of the Glycosaminoglycan family, is a linear and sulfated polysaccharide displaying a high level of molecular diversity. HS chains interact and modulate the activity of numerous HS binding proteins (HSBP), amongst which validated therapeutic targets . The selective inhibition of a given protein/HS interaction has been attracting increasing interest as an original therapeutic mode of action, especially since the commercialization of Arixtra® , the synthetic version of a pentasaccharide sequence specifically recognizing and activating antithrombin-III. To date, it has not been possible to generalize to other HSBP the strategy used to identify this sequence. In Orsay, we aim at overcoming such a bottleneck by conceiving and synthesizing tailored probes to address different aspects of HS biology and devise therapeutic innovation based on the modulation of HS-HSBP interactions . To reach these aims, we developed new methodologies in organic synthesis and optimized each step by determining their critic parameters , thus illustrating that glycochemistry represent an ideal playground to revise central concepts in organic chemistry, as well as to initiate original developments and methodologies.
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