Depsipeptides Targeting Tumor Cells: Milestones from In Vitro to Clinical Trials

Cancer is currently considered one of the most threatening diseases worldwide. Diet could be one of the factors that can be enhanced to comprehensively address a cancer patient’s condition. Unfortunately, most molecules capable of targeting cancer cells are found in uncommon food sources. Among them...

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Main Authors: Plinio A. Trinidad-Calderón, Carlos Daniel Varela-Chinchilla, Silverio García-Lara
Format: Article
Language:English
Published: MDPI AG 2023-01-01
Series:Molecules
Subjects:
Online Access:https://www.mdpi.com/1420-3049/28/2/670
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author Plinio A. Trinidad-Calderón
Carlos Daniel Varela-Chinchilla
Silverio García-Lara
author_facet Plinio A. Trinidad-Calderón
Carlos Daniel Varela-Chinchilla
Silverio García-Lara
author_sort Plinio A. Trinidad-Calderón
collection DOAJ
description Cancer is currently considered one of the most threatening diseases worldwide. Diet could be one of the factors that can be enhanced to comprehensively address a cancer patient’s condition. Unfortunately, most molecules capable of targeting cancer cells are found in uncommon food sources. Among them, depsipeptides have emerged as one of the most reliable choices for cancer treatment. These cyclic amino acid oligomers, with one or more subunits replaced by a hydroxylated carboxylic acid resulting in one lactone bond in a core ring, have broadly proven their cancer-targeting efficacy, some even reaching clinical trials and being commercialized as “anticancer” drugs. This review aimed to describe these depsipeptides, their reported amino acid sequences, determined structure, and the specific mechanism by which they target tumor cells including apoptosis, oncosis, and elastase inhibition, among others. Furthermore, we have delved into state-of-the-art in vivo and clinical trials, current methods for purification and synthesis, and the recognized disadvantages of these molecules. The information collated in this review can help researchers decide whether these molecules should be incorporated into functional foods in the near future.
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spelling doaj.art-fe06a1f231c84d6e9f42c5d868c6f0552023-11-30T23:43:07ZengMDPI AGMolecules1420-30492023-01-0128267010.3390/molecules28020670Depsipeptides Targeting Tumor Cells: Milestones from In Vitro to Clinical TrialsPlinio A. Trinidad-Calderón0Carlos Daniel Varela-Chinchilla1Silverio García-Lara2Tecnológico de Monterrey, School of Engineering, and Sciences, Avenida Eugenio Garza Sada 2501, Monterrey 64849, Nuevo León, MexicoTecnológico de Monterrey, School of Engineering, and Sciences, Avenida Eugenio Garza Sada 2501, Monterrey 64849, Nuevo León, MexicoTecnológico de Monterrey, School of Engineering, and Sciences, Avenida Eugenio Garza Sada 2501, Monterrey 64849, Nuevo León, MexicoCancer is currently considered one of the most threatening diseases worldwide. Diet could be one of the factors that can be enhanced to comprehensively address a cancer patient’s condition. Unfortunately, most molecules capable of targeting cancer cells are found in uncommon food sources. Among them, depsipeptides have emerged as one of the most reliable choices for cancer treatment. These cyclic amino acid oligomers, with one or more subunits replaced by a hydroxylated carboxylic acid resulting in one lactone bond in a core ring, have broadly proven their cancer-targeting efficacy, some even reaching clinical trials and being commercialized as “anticancer” drugs. This review aimed to describe these depsipeptides, their reported amino acid sequences, determined structure, and the specific mechanism by which they target tumor cells including apoptosis, oncosis, and elastase inhibition, among others. Furthermore, we have delved into state-of-the-art in vivo and clinical trials, current methods for purification and synthesis, and the recognized disadvantages of these molecules. The information collated in this review can help researchers decide whether these molecules should be incorporated into functional foods in the near future.https://www.mdpi.com/1420-3049/28/2/670depsipeptideanticancercancer-targetingcellfunctional foodenrichment
spellingShingle Plinio A. Trinidad-Calderón
Carlos Daniel Varela-Chinchilla
Silverio García-Lara
Depsipeptides Targeting Tumor Cells: Milestones from In Vitro to Clinical Trials
Molecules
depsipeptide
anticancer
cancer-targeting
cell
functional food
enrichment
title Depsipeptides Targeting Tumor Cells: Milestones from In Vitro to Clinical Trials
title_full Depsipeptides Targeting Tumor Cells: Milestones from In Vitro to Clinical Trials
title_fullStr Depsipeptides Targeting Tumor Cells: Milestones from In Vitro to Clinical Trials
title_full_unstemmed Depsipeptides Targeting Tumor Cells: Milestones from In Vitro to Clinical Trials
title_short Depsipeptides Targeting Tumor Cells: Milestones from In Vitro to Clinical Trials
title_sort depsipeptides targeting tumor cells milestones from in vitro to clinical trials
topic depsipeptide
anticancer
cancer-targeting
cell
functional food
enrichment
url https://www.mdpi.com/1420-3049/28/2/670
work_keys_str_mv AT plinioatrinidadcalderon depsipeptidestargetingtumorcellsmilestonesfrominvitrotoclinicaltrials
AT carlosdanielvarelachinchilla depsipeptidestargetingtumorcellsmilestonesfrominvitrotoclinicaltrials
AT silveriogarcialara depsipeptidestargetingtumorcellsmilestonesfrominvitrotoclinicaltrials