Cyclic Dipeptides: The Biological and Structural Landscape with Special Focus on the Anti-Cancer Proline-Based Scaffold

Authors

Joanna Bojarska, Technical University of Lodz
Adam Mieczkowski, Polish Academy of Sciences
Zyta M. Ziora, The University of Queensland
Mariusz Skwarczynski, The University of Queensland
Istvan Toth, The University of Queensland
Ahmed O. Shalash, The University of Queensland
Keykavous Parang, Chapman UniversityFollow
Shaima Ahmed El-Mowafi, Chapman UniversityFollow
Eman H. M. Mohammed, Chapman UniversityFollow
Sherif Elnagdy, Cairo University
Maha AlKhazindar, Cairo University
Wojciech M. Wolf, Technical University of Lodz

Document Type

Article

Publication Date

10-14-2021

Abstract

Cyclic dipeptides, also know as diketopiperazines (DKP), the simplest cyclic forms of peptides widespread in nature, are unsurpassed in their structural and bio-functional diversity. DKPs, especially those containing proline, due to their unique features such as, inter alia, extra-rigid conformation, high resistance to enzyme degradation, increased cell permeability, and expandable ability to bind a diverse of targets with better affinity, have emerged in the last years as biologically pre-validated platforms for the drug discovery. Recent advances have revealed their enormous potential in the development of next-generation theranostics, smart delivery systems, and biomaterials. Here, we present an updated review on the biological and structural profile of these appealing biomolecules, with a particular emphasis on those with anticancer properties, since cancers are the main cause of death all over the world. Additionally, we provide a consideration on supramolecular structuring and synthons, based on the proline-based DKP privileged scaffold, for inspiration in the design of compound libraries in search of ideal ligands, innovative self-assembled nanomaterials, and bio-functional architectures.

Comments

This article was originally published in Biomolecules, volume 11, issue 10, in 2021. https://doi.org/10.3390/biom11101515

Recommended Citation

Bojarska, J.; Mieczkowski, A.; Ziora, Z.; Skwarczynski, M.; Toth, I.; Shalash, A.O.; Parang, K.; El-Mowafi, S.A.; Mohammed, E.H.M.; Elnagdy, S.; et al. Cyclic Dipeptides: The Biological and Structural Landscape with Special Focus on the Anti-Cancer Proline-Based Scaffold. Biomolecules 2021, 11, 1515. https://doi.org/10.3390/biom11101515

Copyright

The authors

Creative Commons License

This work is licensed under a Creative Commons Attribution 4.0 License.