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Article

Chimeric Drug Design with a Noncharged Carrier for Mitochondrial Delivery

1
Departamento de Fisicoquimica, Unidad de Excelencia de Química Aplicada a Biomedicina y Medioambiente, Facultad de Farmacia, Universidad de Granada, Campus Cartuja, 18071 Granada, Spain
2
Departamento de Quimica Organica, Unidad de Excelencia de Química Aplicada a Biomedicina y Medioambiente, Facultad de Ciencias, Universidad de Granada, Campus Fuentenueva, 18071 Granada, Spain
3
GENYO, Pfizer-University of Granada-Junta de Andalucía Centre for Genomics and Oncological Research. Avda. Ilustracion 114. PTS, 18016 Granada, Spain
4
Department of Chemistry, K. U. Leuven, Celestijnenlaan 200F, B-3001 Heverlee, Belgium
*
Author to whom correspondence should be addressed.
Current address: Interdisciplinary Institute for Neuroscience, UMR 5297, Centre National de la Recherche Scientifique, F-33076 Bordeaux, France; and Interdisciplinary Institute for Neuroscience, University of Bordeaux, F-33076 Bordeaux, France.
Current address: Departamento de Bioquimica y Biologia Molecular I, Facultad de Ciencias, Universidad de Granada, Campus Fuentenueva, 18071 Granada, Spain.
Academic Editor: Joanna Kopecka
Pharmaceutics 2021, 13(2), 254; https://doi.org/10.3390/pharmaceutics13020254
Received: 13 December 2020 / Revised: 25 January 2021 / Accepted: 3 February 2021 / Published: 12 February 2021
(This article belongs to the Special Issue Mitochondria-targeted drug delivery)
Recently, it was proposed that the thiophene ring is capable of promoting mitochondrial accumulation when linked to fluorescent markers. As a noncharged group, thiophene presents several advantages from a synthetic point of view, making it easier to incorporate such a side moiety into different molecules. Herein, we confirm the general applicability of the thiophene group as a mitochondrial carrier for drugs and fluorescent markers based on a new concept of nonprotonable, noncharged transporter. We implemented this concept in a medicinal chemistry application by developing an antitumor, metabolic chimeric drug based on the pyruvate dehydrogenase kinase (PDHK) inhibitor dichloroacetate (DCA). The promising features of the thiophene moiety as a noncharged carrier for targeting mitochondria may represent a starting point for the design of new metabolism-targeting drugs. View Full-Text
Keywords: antitumor agents; fluorescence lifetime imaging; medicinal chemistry; metabolic drug; mitochondrial carrier antitumor agents; fluorescence lifetime imaging; medicinal chemistry; metabolic drug; mitochondrial carrier
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MDPI and ACS Style

Ripoll, C.; Herrero-Foncubierta, P.; Puente-Muñoz, V.; Gonzalez-Garcia, M.C.; Miguel, D.; Resa, S.; Paredes, J.M.; Ruedas-Rama, M.J.; Garcia-Fernandez, E.; Roldan, M.; Rocha, S.; De Keersmaecker, H.; Hofkens, J.; Martin, M.; Cuerva, J.M.; Orte, A. Chimeric Drug Design with a Noncharged Carrier for Mitochondrial Delivery. Pharmaceutics 2021, 13, 254. https://doi.org/10.3390/pharmaceutics13020254

AMA Style

Ripoll C, Herrero-Foncubierta P, Puente-Muñoz V, Gonzalez-Garcia MC, Miguel D, Resa S, Paredes JM, Ruedas-Rama MJ, Garcia-Fernandez E, Roldan M, Rocha S, De Keersmaecker H, Hofkens J, Martin M, Cuerva JM, Orte A. Chimeric Drug Design with a Noncharged Carrier for Mitochondrial Delivery. Pharmaceutics. 2021; 13(2):254. https://doi.org/10.3390/pharmaceutics13020254

Chicago/Turabian Style

Ripoll, Consuelo, Pilar Herrero-Foncubierta, Virginia Puente-Muñoz, M. C. Gonzalez-Garcia, Delia Miguel, Sandra Resa, Jose M. Paredes, Maria J. Ruedas-Rama, Emilio Garcia-Fernandez, Mar Roldan, Susana Rocha, Herlinde De Keersmaecker, Johan Hofkens, Miguel Martin, Juan M. Cuerva, and Angel Orte. 2021. "Chimeric Drug Design with a Noncharged Carrier for Mitochondrial Delivery" Pharmaceutics 13, no. 2: 254. https://doi.org/10.3390/pharmaceutics13020254

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