Abstract:With over 60 % of protein-protein interfaces featuring an α-helix, the use of α-helix mimetics as inhibitors of these interactions is a prevalent therapeutic strategy. However, methods to control the conformation of mimetics, thus enabling maximum efficacy, can be restrictive. Alternatively, conformation can be controlled through the introduction of destabilizing synpentane interactions. This tactic, which is often adopted by Nature, is not a common feature of lead optimization owing to the significant synthet… Show more
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