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Toward the Selective Inhibition of G Proteins: Total Synthesis of a Simplified YM-254890 Analog.
Rensing, Derek T; Uppal, Sakshi; Blumer, Kendall J; Moeller, Kevin D.
Afiliação
  • Rensing DT; †Department of Chemistry, Washington University, St. Louis, Missouri 63130, United States.
  • Uppal S; †Department of Chemistry, Washington University, St. Louis, Missouri 63130, United States.
  • Blumer KJ; ‡Department of Cell Biology and Physiology, Washington University School of Medicine, St. Louis, Missouri 63110, United States.
  • Moeller KD; †Department of Chemistry, Washington University, St. Louis, Missouri 63130, United States.
Org Lett ; 17(9): 2270-3, 2015 May 01.
Article em En | MEDLINE | ID: mdl-25875152
ABSTRACT
A simplified analog (WU-07047) of the selective Gαq/11 inhibitor YM-254890 has been synthesized, and an initial probe of its activity conducted. In the analog, the two peptide-based linkers in the cyclic YM-254890 have been replaced with hydrocarbon chains. This enables a convergent approach to the synthesis of the analog. Biochemical assays showed that while the simplified analog is not as potent as YM-254890, it does still inhibit Gq.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Peptídeos Cíclicos / Proteínas de Ligação ao GTP Idioma: En Ano de publicação: 2015 Tipo de documento: Article
Texto completo
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XML
PubMed Links
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Peptídeos Cíclicos / Proteínas de Ligação ao GTP Idioma: En Ano de publicação: 2015 Tipo de documento: Article