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Small structural changes of the imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitors produce an improved safety profile.
Futatsugi, K; Huard, K; Kung, D W; Pettersen, J C; Flynn, D A; Gosset, J R; Aspnes, G E; Barnes, R J; Cabral, S; Dowling, M S; Fernando, D P; Goosen, T C; Gorczyca, W P; Hepworth, D; Herr, M; Lavergne, S; Li, Q; Niosi, M; Orr, S T M; Pardo, I D; Perez, S M; Purkal, J; Schmahai, T J; Shirai, N; Shoieb, A M; Zhou, J; Goodwin, B.
Afiliação
  • Futatsugi K; Pfizer Inc. Medicine Design , 610 Main Street , Cambridge , Massachusetts , 02155 USA . Email: Kim.Huard@Pfizer.com.
  • Huard K; Pfizer Inc. Medicine Design , 610 Main Street , Cambridge , Massachusetts , 02155 USA . Email: Kim.Huard@Pfizer.com.
  • Kung DW; Pfizer Inc. Medicine Design , Eastern Point Road , Groton , Connecticut , 06340 USA . Email: Daniel.W.Kung@pfizer.com.
  • Pettersen JC; Pfizer Inc. Drug Safety Research and Development , Eastern Point Road , Groton , Connecticut , 06340 USA.
  • Flynn DA; Pfizer Inc. Drug Safety Research and Development , Eastern Point Road , Groton , Connecticut , 06340 USA.
  • Gosset JR; Pfizer Inc. Medicine Design , 610 Main Street , Cambridge , Massachusetts , 02155 USA . Email: Kim.Huard@Pfizer.com.
  • Aspnes GE; Pfizer Inc. Medicine Design , 610 Main Street , Cambridge , Massachusetts , 02155 USA . Email: Kim.Huard@Pfizer.com.
  • Barnes RJ; Pfizer Inc. Drug Safety Research and Development , Eastern Point Road , Groton , Connecticut , 06340 USA.
  • Cabral S; Pfizer Inc. Medicine Design , Eastern Point Road , Groton , Connecticut , 06340 USA . Email: Daniel.W.Kung@pfizer.com.
  • Dowling MS; Pfizer Inc. Medicine Design , Eastern Point Road , Groton , Connecticut , 06340 USA . Email: Daniel.W.Kung@pfizer.com.
  • Fernando DP; Pfizer Inc. Medicine Design , Eastern Point Road , Groton , Connecticut , 06340 USA . Email: Daniel.W.Kung@pfizer.com.
  • Goosen TC; Pfizer Inc. Medicine Design , Eastern Point Road , Groton , Connecticut , 06340 USA . Email: Daniel.W.Kung@pfizer.com.
  • Gorczyca WP; Pfizer Inc. Drug Safety Research and Development , Eastern Point Road , Groton , Connecticut , 06340 USA.
  • Hepworth D; Pfizer Inc. Medicine Design , 610 Main Street , Cambridge , Massachusetts , 02155 USA . Email: Kim.Huard@Pfizer.com.
  • Herr M; Pfizer Inc. Medicine Design , Eastern Point Road , Groton , Connecticut , 06340 USA . Email: Daniel.W.Kung@pfizer.com.
  • Lavergne S; Pfizer Inc. Medicine Design , Eastern Point Road , Groton , Connecticut , 06340 USA . Email: Daniel.W.Kung@pfizer.com.
  • Li Q; Pfizer Inc. Medicine Design , Eastern Point Road , Groton , Connecticut , 06340 USA . Email: Daniel.W.Kung@pfizer.com.
  • Niosi M; Pfizer Inc. Medicine Design , Eastern Point Road , Groton , Connecticut , 06340 USA . Email: Daniel.W.Kung@pfizer.com.
  • Orr STM; Pfizer Inc. Medicine Design , Eastern Point Road , Groton , Connecticut , 06340 USA . Email: Daniel.W.Kung@pfizer.com.
  • Pardo ID; Pfizer Inc. Drug Safety Research and Development , Eastern Point Road , Groton , Connecticut , 06340 USA.
  • Perez SM; Pfizer Inc. Cardiovascular and Metabolic Disease Research Unit , 610 Main Street , Cambridge , Massachusetts , 02155 USA.
  • Purkal J; Pfizer Inc. Cardiovascular and Metabolic Disease Research Unit , 610 Main Street , Cambridge , Massachusetts , 02155 USA.
  • Schmahai TJ; Pfizer Inc. Drug Safety Research and Development , Eastern Point Road , Groton , Connecticut , 06340 USA.
  • Shirai N; Pfizer Inc. Drug Safety Research and Development , Eastern Point Road , Groton , Connecticut , 06340 USA.
  • Shoieb AM; Pfizer Inc. Drug Safety Research and Development , Eastern Point Road , Groton , Connecticut , 06340 USA.
  • Zhou J; Pfizer Inc. Drug Safety Research and Development , Eastern Point Road , Groton , Connecticut , 06340 USA.
  • Goodwin B; Pfizer Inc. Cardiovascular and Metabolic Disease Research Unit , 610 Main Street , Cambridge , Massachusetts , 02155 USA.
Medchemcomm ; 8(4): 771-779, 2017 Apr 01.
Article em En | MEDLINE | ID: mdl-30108796
ABSTRACT
Small molecule DGAT2 inhibitors have shown promise for the treatment of metabolic diseases in preclinical models. Herein, we report the first toxicological evaluation of imidazopyridine-based DGAT2 inhibitors and show that the arteriopathy associated with imidazopyridine 1 can be mitigated with small structural modifications, and is thus not mechanism related.
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Texto completo: 1 Base de dados: MEDLINE Idioma: En Revista: Medchemcomm Ano de publicação: 2017 Tipo de documento: Article
Texto completo
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PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Idioma: En Revista: Medchemcomm Ano de publicação: 2017 Tipo de documento: Article