SSAO substrates exhibiting insulin-like effects in adipocytes as a promising treatment option for metabolic disorders

Josep Mercader, Zsuzsa Iffiú-Soltesz, Xavier Brenachot, Ágota Földi, Petra Dunkel, Balázs Balogh, Camille Attané, Philippe Valet, P. Mátyus, Christian Carpéné

Research output: Contribution to journalArticle

14 Citations (Scopus)

Abstract

Background: Benzylamine exerts insulin-like effects in adipocytes (e.g., glucose uptake and antilipolysis) and improves glucose handling in rodents. Results: In murine adipocytes, benzylamine mimics another insulin action: it enhances apelin expression in a manner that is blocked by the semicarbazide-sensitive amine oxidase/vascular adhesion protein-1 (SSAO/VAP-1) inhibitor semicarbazide. It is shown that in human adipocytes, benzylamine activates glucose transport, but its effects are not additive to maximal insulin stimulation. Benzylamine effects are hydrogen peroxide dependent. They can be reproduced by novel substrates, but not by benzaldehyde. Conclusion: Owing to the parallelism between the in vitro insulin mimicry and the in vivo improvement of glucose handling elicited by benzylamine in rodents, the SSAO/VAP-1 substrates, with stronger effects on human adipocytes than benzylamine, show promising applications for the treatment of insulin resistance.

Original languageEnglish
Pages (from-to)1735-1749
Number of pages15
JournalFuture Medicinal Chemistry
Volume2
Issue number12
DOIs
Publication statusPublished - Dec 2010

Fingerprint

Adipocytes
Insulin
Amine Oxidase (Copper-Containing)
Glucose
Blood Vessels
Rodentia
Hydrogen Peroxide
Insulin Resistance
benzylamine
Proteins

ASJC Scopus subject areas

  • Drug Discovery
  • Pharmacology
  • Molecular Medicine

Cite this

Mercader, J., Iffiú-Soltesz, Z., Brenachot, X., Földi, Á., Dunkel, P., Balogh, B., ... Carpéné, C. (2010). SSAO substrates exhibiting insulin-like effects in adipocytes as a promising treatment option for metabolic disorders. Future Medicinal Chemistry, 2(12), 1735-1749. https://doi.org/10.4155/fmc.10.260

SSAO substrates exhibiting insulin-like effects in adipocytes as a promising treatment option for metabolic disorders. / Mercader, Josep; Iffiú-Soltesz, Zsuzsa; Brenachot, Xavier; Földi, Ágota; Dunkel, Petra; Balogh, Balázs; Attané, Camille; Valet, Philippe; Mátyus, P.; Carpéné, Christian.

In: Future Medicinal Chemistry, Vol. 2, No. 12, 12.2010, p. 1735-1749.

Research output: Contribution to journalArticle

Mercader, J, Iffiú-Soltesz, Z, Brenachot, X, Földi, Á, Dunkel, P, Balogh, B, Attané, C, Valet, P, Mátyus, P & Carpéné, C 2010, 'SSAO substrates exhibiting insulin-like effects in adipocytes as a promising treatment option for metabolic disorders', Future Medicinal Chemistry, vol. 2, no. 12, pp. 1735-1749. https://doi.org/10.4155/fmc.10.260
Mercader, Josep ; Iffiú-Soltesz, Zsuzsa ; Brenachot, Xavier ; Földi, Ágota ; Dunkel, Petra ; Balogh, Balázs ; Attané, Camille ; Valet, Philippe ; Mátyus, P. ; Carpéné, Christian. / SSAO substrates exhibiting insulin-like effects in adipocytes as a promising treatment option for metabolic disorders. In: Future Medicinal Chemistry. 2010 ; Vol. 2, No. 12. pp. 1735-1749.
@article{fa1e54bc591542eaaba58bead4f165d5,
title = "SSAO substrates exhibiting insulin-like effects in adipocytes as a promising treatment option for metabolic disorders",
abstract = "Background: Benzylamine exerts insulin-like effects in adipocytes (e.g., glucose uptake and antilipolysis) and improves glucose handling in rodents. Results: In murine adipocytes, benzylamine mimics another insulin action: it enhances apelin expression in a manner that is blocked by the semicarbazide-sensitive amine oxidase/vascular adhesion protein-1 (SSAO/VAP-1) inhibitor semicarbazide. It is shown that in human adipocytes, benzylamine activates glucose transport, but its effects are not additive to maximal insulin stimulation. Benzylamine effects are hydrogen peroxide dependent. They can be reproduced by novel substrates, but not by benzaldehyde. Conclusion: Owing to the parallelism between the in vitro insulin mimicry and the in vivo improvement of glucose handling elicited by benzylamine in rodents, the SSAO/VAP-1 substrates, with stronger effects on human adipocytes than benzylamine, show promising applications for the treatment of insulin resistance.",
author = "Josep Mercader and Zsuzsa Iffi{\'u}-Soltesz and Xavier Brenachot and {\'A}gota F{\"o}ldi and Petra Dunkel and Bal{\'a}zs Balogh and Camille Attan{\'e} and Philippe Valet and P. M{\'a}tyus and Christian Carp{\'e}n{\'e}",
year = "2010",
month = "12",
doi = "10.4155/fmc.10.260",
language = "English",
volume = "2",
pages = "1735--1749",
journal = "Future Medicinal Chemistry",
issn = "1756-8919",
publisher = "Future Science",
number = "12",

}

TY - JOUR

T1 - SSAO substrates exhibiting insulin-like effects in adipocytes as a promising treatment option for metabolic disorders

AU - Mercader, Josep

AU - Iffiú-Soltesz, Zsuzsa

AU - Brenachot, Xavier

AU - Földi, Ágota

AU - Dunkel, Petra

AU - Balogh, Balázs

AU - Attané, Camille

AU - Valet, Philippe

AU - Mátyus, P.

AU - Carpéné, Christian

PY - 2010/12

Y1 - 2010/12

N2 - Background: Benzylamine exerts insulin-like effects in adipocytes (e.g., glucose uptake and antilipolysis) and improves glucose handling in rodents. Results: In murine adipocytes, benzylamine mimics another insulin action: it enhances apelin expression in a manner that is blocked by the semicarbazide-sensitive amine oxidase/vascular adhesion protein-1 (SSAO/VAP-1) inhibitor semicarbazide. It is shown that in human adipocytes, benzylamine activates glucose transport, but its effects are not additive to maximal insulin stimulation. Benzylamine effects are hydrogen peroxide dependent. They can be reproduced by novel substrates, but not by benzaldehyde. Conclusion: Owing to the parallelism between the in vitro insulin mimicry and the in vivo improvement of glucose handling elicited by benzylamine in rodents, the SSAO/VAP-1 substrates, with stronger effects on human adipocytes than benzylamine, show promising applications for the treatment of insulin resistance.

AB - Background: Benzylamine exerts insulin-like effects in adipocytes (e.g., glucose uptake and antilipolysis) and improves glucose handling in rodents. Results: In murine adipocytes, benzylamine mimics another insulin action: it enhances apelin expression in a manner that is blocked by the semicarbazide-sensitive amine oxidase/vascular adhesion protein-1 (SSAO/VAP-1) inhibitor semicarbazide. It is shown that in human adipocytes, benzylamine activates glucose transport, but its effects are not additive to maximal insulin stimulation. Benzylamine effects are hydrogen peroxide dependent. They can be reproduced by novel substrates, but not by benzaldehyde. Conclusion: Owing to the parallelism between the in vitro insulin mimicry and the in vivo improvement of glucose handling elicited by benzylamine in rodents, the SSAO/VAP-1 substrates, with stronger effects on human adipocytes than benzylamine, show promising applications for the treatment of insulin resistance.

UR - http://www.scopus.com/inward/record.url?scp=78650182603&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=78650182603&partnerID=8YFLogxK

U2 - 10.4155/fmc.10.260

DO - 10.4155/fmc.10.260

M3 - Article

VL - 2

SP - 1735

EP - 1749

JO - Future Medicinal Chemistry

JF - Future Medicinal Chemistry

SN - 1756-8919

IS - 12

ER -