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Article Dans Une Revue Molecules Année : 2023

C3-Symmetric Ligands in Drug Design: When the Target Controls the Aesthetics of the Drug

Mirjana Antonijevic
Patrick Dallemagne

Résumé

A number of proteins are able to adopt a homotrimeric spatial conformation. Among these structures, this feature appears as crucial for biologic targets, since it facilitates the design of C3-symmetric ligands that are especially suitable for displaying optimized ligand–target interactions and therapeutic benefits. Additionally, DNA as a therapeutic target, even if its conformation into a superhelix does not correspond to a C3-symmetry, can also take advantage of these C3-symmetric ligands for better interactions and therapeutic effects. For the moment, this opportunity appears to be under-exploited, but should become more frequent with the discovery of new homotrimeric targets such as the SARS-CoV2 spike protein. Besides their potential therapeutic interest, the synthetic access to these C3-symmetric ligands often leads to chemical challenges, although drug candidates with an aesthetic structure are generally obtained.

Domaines

Chimie
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Dates et versions

hal-03969919 , version 1 (24-01-2024)

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Mirjana Antonijevic, Christophe Rochais, Patrick Dallemagne. C3-Symmetric Ligands in Drug Design: When the Target Controls the Aesthetics of the Drug. Molecules, 2023, 28 (2), pp.679. ⟨10.3390/molecules28020679⟩. ⟨hal-03969919⟩
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