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Discovery of a VHL and HIF1α interaction inhibitor with in vivo angiogenic activity via structure-based virtual screening.
Yang, Chao; Wang, Wanhe; Chen, Linmin; Liang, Jiaxin; Lin, Sheng; Lee, Ming-Yuen; Ma, Dik-Lung; Leung, Chung-Hang.
Afiliación
  • Yang C; State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao, China. duncanleung@umac.mo.
  • Wang W; Department of Chemistry, Hong Kong Baptist University, Kowloon Tong, Hong Kong, China. edmondma@hkbu.edu.hk.
  • Chen L; State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao, China. duncanleung@umac.mo.
  • Liang J; State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao, China. duncanleung@umac.mo.
  • Lin S; Department of Chemistry, Hong Kong Baptist University, Kowloon Tong, Hong Kong, China. edmondma@hkbu.edu.hk.
  • Lee MY; State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao, China. duncanleung@umac.mo.
  • Ma DL; Department of Chemistry, Hong Kong Baptist University, Kowloon Tong, Hong Kong, China. edmondma@hkbu.edu.hk.
  • Leung CH; State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao, China. duncanleung@umac.mo.
Chem Commun (Camb) ; 52(87): 12837-12840, 2016 Oct 25.
Article en En | MEDLINE | ID: mdl-27709157
ABSTRACT
We describe herein compound 1, which is similar to many known natural products, as an inhibitor of the VHL-HIF1α interaction via structure-based virtual screening. Compound 1 disrupts VHL-mediated HIF1α degradation, leading to significantly increased VEGF expression. To our knowledge, compound 1 is a member of only the second class of small molecule inhibitors of the VHL-HIF1α interaction.
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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Conformación Proteica / Neovascularización Fisiológica / Proteína Supresora de Tumores del Síndrome de Von Hippel-Lindau / Subunidad alfa del Factor 1 Inducible por Hipoxia / Bibliotecas de Moléculas Pequeñas / Ensayos Analíticos de Alto Rendimiento / Mapas de Interacción de Proteínas Tipo de estudio: Diagnostic_studies / Screening_studies Límite: Humans Idioma: En Revista: Chem Commun (Camb) Asunto de la revista: QUIMICA Año: 2016 Tipo del documento: Article País de afiliación: China
Buscar en Google
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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Conformación Proteica / Neovascularización Fisiológica / Proteína Supresora de Tumores del Síndrome de Von Hippel-Lindau / Subunidad alfa del Factor 1 Inducible por Hipoxia / Bibliotecas de Moléculas Pequeñas / Ensayos Analíticos de Alto Rendimiento / Mapas de Interacción de Proteínas Tipo de estudio: Diagnostic_studies / Screening_studies Límite: Humans Idioma: En Revista: Chem Commun (Camb) Asunto de la revista: QUIMICA Año: 2016 Tipo del documento: Article País de afiliación: China