The interaction between the alpha2beta1
integrin and collagen plays a crucial role in the development of pathological
conditions, such as thrombus formation and cancer cell metastasis. Accordingly,
the alpha2beta1 integrin is a promising target for the development of new drug
molecules to treat these diseases. Here, we have designed, synthesized, and
measured in vitro a set of novel drug-like compounds that block the protein–protein
interactions between alpha2beta1 integrin and collagen. The obtained
structure–activity relationship reveals the key features that are required for
successful inhibition of this integrin–collagen interaction.