Not only is the stapling moiety fundamental to mimicking biological activity but also the bridge size and its location and orientation within the bridge.
TORONTO, Ontario (PRWEB)
October 12, 2022
An increasing number of peptides are used in active pharmaceutical ingredients, cosmetics, diagnostics, and vaccines. Several are based on long sequences, cyclic structures, and multi-branched systems that require complex synthetic strategies to incorporate homodetic and heterodetic bridges, post-translational modifications, or constrained unnatural amino acids.
Therefore, peptide organic synthetic chemists have to overcome a variety of difficulties not only on a small scale but also during the scale-up. For example, side chain-to-side chain cyclizations represent a strategy for the enrichment of bioactive conformational ensembles. Structural rigidification reduces entropy and may lock molecules into receptor-binding conformations. Structural manipulations, therefore, contribute to the enhancement of target specificity, induce higher binding affinity and biological potency and often lead to lower metabolic susceptibility and more favorable pharmacokinetics.
In this webinar, the featured speaker will discuss the syntheses of biologically relevant cyclopeptides containing not only 1,4-disubstituted-[1,2,3]-triazolyl bridges but also interlocked dicarba bridges and 1,3-butadiyne constraints. This offers a powerful approach for generating stable helix mimetic structures or β-turn conformations. Not only is the stapling moiety fundamental to mimicking biological activity but also the bridge size and its location and orientation within the bridge.
Join this webinar to hear the speaker explore multiple parameters in technologies that improve the efficacy of solid-phase syntheses in complex peptides. The role of temperature, solvent volumes, coupling systems, and mixing modes (N2 bubbling and/or oscillation mixing) will be discussed, in addition, and how they can optimize protocols to develop the best conditions for the small-scale and mainly further upscaling of solid-phase synthesis.
Join Prof. Anna Maria Papini, University of Florence, Department of Chemistry “Ugo Schiff”, Interdepartmental Research Unit of Peptide and Protein Chemistry and Biology, for the live webinar on Friday, October 28, 2022, at 10 am EDT (3 pm BST/UK).
For more information, or to register for this event, visit Obtaining Complex Peptides Thanks to Efficient Technologies is No Longer a Dream: Successful Stories of Difficult Syntheses.
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