Peptidomimetics are ideal components in cancer therapy because of their advantages in production, such as the possibility of automated chemical synthesis, and ease of modification. The unique advantage of peptidomimetics lies in biological interactions: they provide many possible interaction targets from cancer diagnosis to treatment.
The most influential applications of peptidomimetics in cancer therapy are in three fields: (1) simulating natural interactions between natural proteins or molecules to affect the viability of cancer, (2) targeted therapy or cancer diagnosis, and (3) delivering drugs across biological barriers. We will hopefully see the preclinical research and development of new candidate peptidomimetic drugs.