Peptidomimetics: A Synthetic Tool for Inhibiting Protein–Protein Interactions in Cancer

Lloyd Mabonga, Abidemi Paul Kappo

Research output: Contribution to journalReview articlepeer-review

60 Citations (Scopus)


Protein–protein interactions (PPI) are vital in modulating biochemical pathways in many biological processes. Inhibiting PPI is a tremendously important diagnostic and therapeutic strategy in averting pathophysiological cues and disease progression. Targeting PPI as a smart drug discovery tool has been largely overlooked over the years due to their highly dynamic and expansive interfacial areas. However in recent years, researchers have developed new technologies that have the potential to move this approach up the technology development curve and enable the regular discovery of PPI-focused smart drugs. Few drugs are already on the market and some potential drug-like candidates are in clinical trials. In this study we review the application of peptidomimetics as a valuable tool in PPI inhibition in cancer. First, we describe PPI and the general properties of the PPI interface. Next, we discuss the classification of peptidomimetics. Lastly, we focus on the application of peptidomimetics on targeted PPI in cancer pathways.

Original languageEnglish
Pages (from-to)225-241
Number of pages17
JournalInternational Journal of Peptide Research and Therapeutics
Issue number1
Publication statusPublished - 1 Mar 2020
Externally publishedYes


  • Cancer
  • Mimicries
  • Peptidomimetics
  • Protein–protein interactions
  • Proteomimetics

ASJC Scopus subject areas

  • Analytical Chemistry
  • Bioengineering
  • Biochemistry
  • Molecular Medicine
  • Drug Discovery


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