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Review

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

1
Faculty of Chemistry, Institute of General & Inorganic Chemistry, Technical University of Lodz, 90-924 Lodz, Poland
2
Institute of Biochemistry and Biophysics, Polish Academy of Sciences, Pawinskiego 5a, 02-106 Warsaw, Poland
3
Institute for Molecular Bioscience, The University of Queensland, St. Lucia, QLD 4072, Australia
4
School of Chemistry and Molecular Biosciences, The University of Queensland, St. Lucia, QLD 4072, Australia
5
School of Pharmacy, The University of Queensland, Woolloongabba, QLD 4102, Australia
6
Center for Targeted Drug Delivery, Department of Biomedical and Pharmaceutical Sciences, Harry and Diane Rinker Health Science Campus, School of Pharmacy, Chapman University, Irvine, CA 92618, USA
7
Botany Department, Faculty of Science, Cairo University, Giza 12613, Egypt
*
Author to whom correspondence should be addressed.
Academic Editors: Marc Maresca, Vladimir N. Uversky and Prakash Kulkarni
Biomolecules 2021, 11(10), 1515; https://doi.org/10.3390/biom11101515
Received: 18 September 2021 / Revised: 11 October 2021 / Accepted: 12 October 2021 / Published: 14 October 2021
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. View Full-Text
Keywords: cyclic dipeptides; diketopiperazines; proline-based DKPs; drug discovery; privileged scaffold; supramolecular structuring cyclic dipeptides; diketopiperazines; proline-based DKPs; drug discovery; privileged scaffold; supramolecular structuring
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MDPI and ACS Style

Bojarska, J.; Mieczkowski, A.; Ziora, Z.M.; Skwarczynski, M.; Toth, I.; Shalash, A.O.; Parang, K.; El-Mowafi, S.A.; Mohammed, E.H.M.; Elnagdy, S.; AlKhazindar, M.; Wolf, W.M. 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

AMA Style

Bojarska J, Mieczkowski A, Ziora ZM, Skwarczynski M, Toth I, Shalash AO, Parang K, El-Mowafi SA, Mohammed EHM, Elnagdy S, AlKhazindar M, Wolf WM. Cyclic Dipeptides: The Biological and Structural Landscape with Special Focus on the Anti-Cancer Proline-Based Scaffold. Biomolecules. 2021; 11(10):1515. https://doi.org/10.3390/biom11101515

Chicago/Turabian Style

Bojarska, Joanna, Adam Mieczkowski, Zyta M. Ziora, Mariusz Skwarczynski, Istvan Toth, Ahmed O. Shalash, Keykavous Parang, Shaima A. El-Mowafi, Eman H.M. Mohammed, Sherif Elnagdy, Maha AlKhazindar, and Wojciech M. Wolf 2021. "Cyclic Dipeptides: The Biological and Structural Landscape with Special Focus on the Anti-Cancer Proline-Based Scaffold" Biomolecules 11, no. 10: 1515. https://doi.org/10.3390/biom11101515

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