Journal
MOLECULES
Volume 28, Issue 2, Pages -Publisher
MDPI
DOI: 10.3390/molecules28020679
Keywords
symmetry; C3; homo-trimeric; drug design
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A number of proteins can adopt a homotrimeric spatial conformation, which is crucial for biologic targets in designing C3-symmetric ligands for optimized ligand-target interactions and therapeutic benefits. Both proteins and DNA can benefit from these ligands, even if their conformation does not correspond to a C3-symmetry. The discovery of new homotrimeric targets, such as the SARS-CoV2 spike protein, is expected to increase the use of these ligands in the future. The synthesis of C3-symmetric ligands presents chemical challenges but can result in aesthetically appealing drug candidates.
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.
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