Synthesis of new Carnitine Palmitoyltransferase I inhibitors derivatives of C75

Carnitine Palmitoyltransferase (CPT1) is an enzyme that catalyzes the transport of fatty acids from the cytosol into the mitochondria. CPT1 inhibition in the hypothalamus increases fatty acid levels, which produces an increased expression of anorexigenic neuropeptides, a sign of satiety. C75 acts as...

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Autores: Makowski, Kamil, Mera Nanín, Paula, Ariza Piquer, Xavier, Serra i Cucurull, Dolors, García Gómez, Jordi, Herrero Rodríguez, Laura, López, Marta, Venegas, Alicia
Tipo de documento: artigo
Estado:Versão publicada
Data de publicação:2019
País:España
Recursos:Universidad de Barcelona
Repositório:Dipòsit Digital de la UB
OAI Identifier:oai:diposit.ub.edu:2445/165108
Acesso em linha:https://hdl.handle.net/2445/165108
Access Level:Acceso aberto
Palavra-chave:Enzims
Mitocondris
Carnitina palmitoïl-transferasa 1
Enzymes
Mitochondria
Carnitine palmitoyltransferase I
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repository_id_str
spelling Synthesis of new Carnitine Palmitoyltransferase I inhibitors derivatives of C75Makowski, KamilMera Nanín, PaulaAriza Piquer, XavierSerra i Cucurull, DolorsGarcía Gómez, JordiHerrero Rodríguez, LauraLópez, MartaVenegas, AliciaEnzimsMitocondrisCarnitina palmitoïl-transferasa 1EnzymesMitochondriaCarnitine palmitoyltransferase ICarnitine Palmitoyltransferase (CPT1) is an enzyme that catalyzes the transport of fatty acids from the cytosol into the mitochondria. CPT1 inhibition in the hypothalamus increases fatty acid levels, which produces an increased expression of anorexigenic neuropeptides, a sign of satiety. C75 acts as an antiobesity predrug. In vivo C75, is converted into C75-CoA adduct, which is a potent inhibitor of CPT1 and produces a loss of appetite and body weight. In this work, we present three new derivatives of C75, where the carboxylic group is replaced by a carnitine unit, malonic group, and a hydroxyl group with changes from trans to cis relative stereochemistry. Our results suggest that introducing a bigger group than carboxylic in β position or cis relative configuration of the lactone leads to a decrease of CPT1 inhibitory activity.Universidad Católica de Oriente2019info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionapplication/pdfhttps://hdl.handle.net/2445/165108Articles publicats en revistes (Química Inorgànica i Orgànica)reponame:Dipòsit Digital de la UBinstname:Universidad de BarcelonaInglésReproducció del document publicat a: https://doi.org/10.21931/RB/2019.04.03.7Bionatura, 2019, vol. 4, num. 3, p. 917-921https://doi.org/10.21931/RB/2019.04.03.7cc-by-sa (c) Makowski, Kamil et al., 2019http://creativecommons.org/licenses/by-sa/3.0/esinfo:eu-repo/semantics/openAccessoai:diposit.ub.edu:2445/1651082026-05-27T06:46:51Z
dc.title.none.fl_str_mv Synthesis of new Carnitine Palmitoyltransferase I inhibitors derivatives of C75
title Synthesis of new Carnitine Palmitoyltransferase I inhibitors derivatives of C75
spellingShingle Synthesis of new Carnitine Palmitoyltransferase I inhibitors derivatives of C75
Makowski, Kamil
Enzims
Mitocondris
Carnitina palmitoïl-transferasa 1
Enzymes
Mitochondria
Carnitine palmitoyltransferase I
title_short Synthesis of new Carnitine Palmitoyltransferase I inhibitors derivatives of C75
title_full Synthesis of new Carnitine Palmitoyltransferase I inhibitors derivatives of C75
title_fullStr Synthesis of new Carnitine Palmitoyltransferase I inhibitors derivatives of C75
title_full_unstemmed Synthesis of new Carnitine Palmitoyltransferase I inhibitors derivatives of C75
title_sort Synthesis of new Carnitine Palmitoyltransferase I inhibitors derivatives of C75
dc.creator.none.fl_str_mv Makowski, Kamil
Mera Nanín, Paula
Ariza Piquer, Xavier
Serra i Cucurull, Dolors
García Gómez, Jordi
Herrero Rodríguez, Laura
López, Marta
Venegas, Alicia
author Makowski, Kamil
author_facet Makowski, Kamil
Mera Nanín, Paula
Ariza Piquer, Xavier
Serra i Cucurull, Dolors
García Gómez, Jordi
Herrero Rodríguez, Laura
López, Marta
Venegas, Alicia
author_role author
author2 Mera Nanín, Paula
Ariza Piquer, Xavier
Serra i Cucurull, Dolors
García Gómez, Jordi
Herrero Rodríguez, Laura
López, Marta
Venegas, Alicia
author2_role author
author
author
author
author
author
author
dc.subject.none.fl_str_mv Enzims
Mitocondris
Carnitina palmitoïl-transferasa 1
Enzymes
Mitochondria
Carnitine palmitoyltransferase I
topic Enzims
Mitocondris
Carnitina palmitoïl-transferasa 1
Enzymes
Mitochondria
Carnitine palmitoyltransferase I
description Carnitine Palmitoyltransferase (CPT1) is an enzyme that catalyzes the transport of fatty acids from the cytosol into the mitochondria. CPT1 inhibition in the hypothalamus increases fatty acid levels, which produces an increased expression of anorexigenic neuropeptides, a sign of satiety. C75 acts as an antiobesity predrug. In vivo C75, is converted into C75-CoA adduct, which is a potent inhibitor of CPT1 and produces a loss of appetite and body weight. In this work, we present three new derivatives of C75, where the carboxylic group is replaced by a carnitine unit, malonic group, and a hydroxyl group with changes from trans to cis relative stereochemistry. Our results suggest that introducing a bigger group than carboxylic in β position or cis relative configuration of the lactone leads to a decrease of CPT1 inhibitory activity.
publishDate 2019
dc.date.none.fl_str_mv 2019
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv https://hdl.handle.net/2445/165108
url https://hdl.handle.net/2445/165108
dc.language.none.fl_str_mv Inglés
language_invalid_str_mv Inglés
dc.relation.none.fl_str_mv Reproducció del document publicat a: https://doi.org/10.21931/RB/2019.04.03.7
Bionatura, 2019, vol. 4, num. 3, p. 917-921
https://doi.org/10.21931/RB/2019.04.03.7
dc.rights.none.fl_str_mv cc-by-sa (c) Makowski, Kamil et al., 2019
http://creativecommons.org/licenses/by-sa/3.0/es
info:eu-repo/semantics/openAccess
rights_invalid_str_mv cc-by-sa (c) Makowski, Kamil et al., 2019
http://creativecommons.org/licenses/by-sa/3.0/es
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv Universidad Católica de Oriente
publisher.none.fl_str_mv Universidad Católica de Oriente
dc.source.none.fl_str_mv Articles publicats en revistes (Química Inorgànica i Orgànica)
reponame:Dipòsit Digital de la UB
instname:Universidad de Barcelona
instname_str Universidad de Barcelona
reponame_str Dipòsit Digital de la UB
collection Dipòsit Digital de la UB
repository.name.fl_str_mv
repository.mail.fl_str_mv
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score 15,300719

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