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Identification of 4-Anilinoquin(az)oline as a Cell-Active Protein Kinase Novel 3 (PKN3) Inhibitor Chemotype.
Asquith, Christopher R M; Temme, Louisa; East, Michael P; Laitinen, Tuomo; Pickett, Julie; Kwarcinski, Frank E; Sinha, Parvathi; Wells, Carrow I; Johnson, Gary L; Zutshi, Reena; Drewry, David H.
Afiliação
  • Asquith CRM; Structural Genomics Consortium UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
  • Temme L; Department of Pharmacology School of Medicine, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
  • East MP; Structural Genomics Consortium UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
  • Laitinen T; Department of Pharmacology School of Medicine, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
  • Pickett J; School of Pharmacy Faculty of Health Sciences, University of Eastern Finland, 70211, Kuopio, Finland.
  • Kwarcinski FE; Structural Genomics Consortium UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
  • Sinha P; Luceome Biotechnologies, LLC, Tucson, AZ 85719, USA.
  • Wells CI; Luceome Biotechnologies, LLC, Tucson, AZ 85719, USA.
  • Johnson GL; Structural Genomics Consortium UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
  • Zutshi R; Department of Pharmacology School of Medicine, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
  • Drewry DH; Lineberger Comprehensive Cancer Center School of Medicine, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
ChemMedChem ; 17(12): e202200161, 2022 06 20.
Article em En | MEDLINE | ID: mdl-35403825
Deep annotation of a library of 4-anilinoquin(az)olines led to the identification of 7-iodo-N-(3,4,5-trimethoxyphenyl)quinolin-4-amine 16 as a potent inhibitor (IC50 =14 nM) of Protein Kinase Novel 3 (PKN3) with micromolar activity in cells. Compound 16 is a potential tool compound to study the cell biology of PKN3 and its role in pancreatic and prostate cancer and T-cell acute lymphoblastic leukemia. These 4-anilinoquin(az)olines may also be useful tools to uncover the therapeutic potential of PKN3 inhibition in a broad range of diseases.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Neoplasias da Próstata / Inibidores de Proteínas Quinases Tipo de estudo: Diagnostic_studies Limite: Humans / Male Idioma: En Revista: ChemMedChem Assunto da revista: FARMACOLOGIA / QUIMICA Ano de publicação: 2022 Tipo de documento: Article País de afiliação: Estados Unidos
Texto completo
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Neoplasias da Próstata / Inibidores de Proteínas Quinases Tipo de estudo: Diagnostic_studies Limite: Humans / Male Idioma: En Revista: ChemMedChem Assunto da revista: FARMACOLOGIA / QUIMICA Ano de publicação: 2022 Tipo de documento: Article País de afiliação: Estados Unidos