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Myeloperoxidase inhibition in mice alters atherosclerotic lesion composition.
Roth Flach, Rachel J; Su, Chunyan; Bollinger, Eliza; Cortes, Christian; Robertson, Andrew W; Opsahl, Alan C; Coskran, Timothy M; Maresca, Kevin P; Keliher, Edmund J; Yates, Phillip D; Kim, Albert M; Kalgutkar, Amit S; Buckbinder, Leonard.
Afiliación
  • Roth Flach RJ; Internal Medicine Research Unit, Pfizer Inc., Cambridge, Massachusetts, United States of America.
  • Su C; Internal Medicine Research Unit, Pfizer Inc., Cambridge, Massachusetts, United States of America.
  • Bollinger E; Internal Medicine Research Unit, Pfizer Inc., Cambridge, Massachusetts, United States of America.
  • Cortes C; Internal Medicine Research Unit, Pfizer Inc., Cambridge, Massachusetts, United States of America.
  • Robertson AW; Drug Safety Research and Development Global Pathology, Pfizer Inc., Groton, Connecticut, United States of America.
  • Opsahl AC; Drug Safety Research and Development Global Pathology, Pfizer Inc., Groton, Connecticut, United States of America.
  • Coskran TM; Drug Safety Research and Development Global Pathology, Pfizer Inc., Groton, Connecticut, United States of America.
  • Maresca KP; Early Clinical Development, Pfizer Inc., Cambridge, Massachusetts, United States of America.
  • Keliher EJ; Early Clinical Development, Pfizer Inc., Cambridge, Massachusetts, United States of America.
  • Yates PD; Early Clinical Development, Pfizer Inc., Cambridge, Massachusetts, United States of America.
  • Kim AM; Internal Medicine Research Unit, Pfizer Inc., Cambridge, Massachusetts, United States of America.
  • Kalgutkar AS; Medicine Design, Pfizer Inc., Cambridge, Massachusetts, United States of America.
  • Buckbinder L; Internal Medicine Research Unit, Pfizer Inc., Cambridge, Massachusetts, United States of America.
PLoS One ; 14(3): e0214150, 2019.
Article en En | MEDLINE | ID: mdl-30889221
Myeloperoxidase (MPO) is a highly abundant protein within the neutrophil that is associated with lipoprotein oxidation, and increased plasma MPO levels are correlated with poor prognosis after myocardial infarct. Thus, MPO inhibitors have been developed for the treatment of heart failure and acute coronary syndrome in humans. 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide PF-06282999 is a recently described selective small molecule mechanism-based inactivator of MPO. Here, utilizing PF-06282999, we investigated the role of MPO to regulate atherosclerotic lesion formation and composition in the Ldlr-/- mouse model of atherosclerosis. Though MPO inhibition did not affect lesion area in Ldlr-/- mice fed a Western diet, reduced necrotic core area was observed in aortic root sections after MPO inhibitor treatment. MPO inhibition did not alter macrophage content in and leukocyte homing to atherosclerotic plaques. To assess non-invasive monitoring of plaque inflammation, [18F]-Fluoro-deoxy-glucose (FDG) was administered to Ldlr-/- mice with established atherosclerosis that had been treated with clinically relevant doses of PF-06282999, and reduced FDG signal was observed in animals treated with a dose of PF-06282999 that corresponded with reduced necrotic core area. These data suggest that MPO inhibition does not alter atherosclerotic plaque area or leukocyte homing, but rather alters the inflammatory tone of atherosclerotic lesions; thus, MPO inhibition could have utility to promote atherosclerotic lesion stabilization and prevent atherosclerotic plaque rupture.
Asunto(s)

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirimidinonas / Peroxidasa / Aterosclerosis / Placa Aterosclerótica / Macrófagos / Acetamidas Límite: Animals Idioma: En Revista: PLoS One Asunto de la revista: CIENCIA / MEDICINA Año: 2019 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Estados Unidos

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirimidinonas / Peroxidasa / Aterosclerosis / Placa Aterosclerótica / Macrófagos / Acetamidas Límite: Animals Idioma: En Revista: PLoS One Asunto de la revista: CIENCIA / MEDICINA Año: 2019 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Estados Unidos