SAR insights into TET2 catalytic domain inhibition: Synthesis of 2-Hydroxy-4-Methylene-pentanedicarboxylates.

Tiwari, Anand D; Guan, Yihong; Grabowski, Dale R; Maciejewski, Jaroslaw P; Jha, Babal K; Phillips, James G

Tiwari, Anand D; Guan, Yihong; Grabowski, Dale R; Maciejewski, Jaroslaw P; Jha, Babal K; Phillips, James G.

Afiliación

Tiwari AD; Department of Translational Hematology and Oncology Research, Taussig Cancer Institute, Cleveland, OH 44195, USA. Electronic address: tiwaria@ccf.org.
Guan Y; Department of Translational Hematology and Oncology Research, Taussig Cancer Institute, Cleveland, OH 44195, USA.
Grabowski DR; Department of Translational Hematology and Oncology Research, Taussig Cancer Institute, Cleveland, OH 44195, USA.
Maciejewski JP; Department of Translational Hematology and Oncology Research, Taussig Cancer Institute, Cleveland, OH 44195, USA; Cleveland Clinic Lerner College of Medicine, Cleveland, OH 44195, USA; Case Comprehensive Cancer Center, Case Western Reserve University, Cleveland, OH 44106, USA.
Jha BK; Department of Translational Hematology and Oncology Research, Taussig Cancer Institute, Cleveland, OH 44195, USA; Cleveland Clinic Lerner College of Medicine, Cleveland, OH 44195, USA; Case Comprehensive Cancer Center, Case Western Reserve University, Cleveland, OH 44106, USA.
Phillips JG; Department of Translational Hematology and Oncology Research, Taussig Cancer Institute, Cleveland, OH 44195, USA; Case Comprehensive Cancer Center, Case Western Reserve University, Cleveland, OH 44106, USA. Electronic address: phillij5@ccf.org.

Bioorg Med Chem ; 39: 116141, 2021 06 01.

Article en En | MEDLINE | ID: mdl-33894507

Asunto(s)

Dominio Catalítico/efectos de los fármacos; Proteínas de Unión al ADN/metabolismo; Ácidos Dicarboxílicos/síntesis química; Ácidos Dicarboxílicos/farmacología; Dioxigenasas/metabolismo; Sistema Libre de Células; Metilación de ADN; Ácidos Dicarboxílicos/química; Humanos; Simulación del Acoplamiento Molecular; Análisis Espectral/métodos; Relación Estructura-Actividad; Células THP-1

Palabras clave

2-Hydroxyglutarate; Dioxygenase; Enzyme inhibition; Epigenetic; TET; α-KG

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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Dominio Catalítico / Dioxigenasas / Ácidos Dicarboxílicos / Proteínas de Unión al ADN Límite: Humans Idioma: En Revista: Bioorg Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2021 Tipo del documento: Article

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