RT info:eu-repo/semantics/article
T1 Small molecule anion carriers facilitate lactate transport in model liposomes and cells
A1 Alonso Carrillo, Daniel
A1 Arias Betancur, Alain
A1 Carreira Barral, Israel
A1 Fontova Pale, Pere
A1 Soto Cerrato, Vanessa
A1 García Valverde, María
A1 Pérez Tomás, Ricardo
A1 Quesada Pato, Roberto
K1 Biología molecular
K1 Molecular biology
K1 Química orgánica
K1 Chemistry, Organic
K1 Bioquímica
K1 Biochemistry
AB An excessive production of lactate by cancer cells fosters tumor growth and metastasis. Therefore, targeting lactate metabolism and transport offers a new therapeutic strategy against cancer, based on dependency of some cancer cells for lactate as energy fuel or as oncogenic signal. Herein we present a family ofanionophores based on the structure of click-tambjamines that have proved to be extremely active lactatecarriers across phospholipid membranes. Compound 1, the most potent lactate transmembrane carrier,was studied in HeLa cells. The use of a monocarboxylate transporters (MCTs) inhibitor proved that 1 isan active lactate transporter in living cells, confirming the results obtained in phospholipid vesicles. Moreover, an additive effect of compound 1 with cisplatin was observed in HeLa cells. Identification of activelactate anionophores working in living cells opens up ways to exploit this class of compounds as moleculartools and drugs addressing dysregulated lactate metabolism.
PB Elsevier
SN 2589-0042
YR 2023
FD 2023-09
LK http://hdl.handle.net/10259/8608
UL http://hdl.handle.net/10259/8608
LA eng
NO This research has been financially supported by Consejería de Educación de la Junta de Castilla y León (project BU067P20) and Ministerio de Ciencia e Innovación (project PID2020-117610RB-I00). D.A.-C., I.C.-B. and P.F. thank Consejería de Educación de la Junta de Castilla y León, European Regional Development Fund (ERDF) and European Social Fund (ESF) for their pre-doctoral (D.A.-C.) and post-doctoral (I.C.-B. and P.F.) contracts. A.A.-B. thanks to PFCHA/Becas Chile (Folio#72200156). The authors gratefully acknowledge Andrea Sancho-Medina for her contributions to transmembrane anion transport experiments.
DS Repositorio Institucional de la Universidad de Burgos
RD 09-may-2024