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

Bojarska, Joanna and Mieczkowski, Adam and Ziora, Zyta M. and Skwarczyński, Mariusz and Toth, Istvan and Shalash, Ahmed O. and Parang, Keykavous and El-Mowafi, Shaima A. and Eman, H. M. Mohammed and Elnagdy, Sherif and AlKhazindar, Maha and Wolf, Wojciech M. (2021) Cyclic Dipeptides: The Biological and Structural Landscape with Special Focus on the Anti-Cancer Proline-Based Scaffold. Biomolecules, 11 (10). p. 1515. ISSN 2218-273X

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Official URL: https://www.mdpi.com/2218-273X/11/10/1515

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.

Item Type:Article
Subjects:Q Science > QD Chemistry
R Medicine > RM Therapeutics. Pharmacology
Divisions:Department of Biophysics
ID Code:2252
Deposited By: Dr Adam Mieczkowski
Deposited On:20 Feb 2023 12:49
Last Modified:20 Feb 2023 12:49

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