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SGC-AAK1-1: A Chemical Probe Targeting AAK1 and BMP2K.
Wells, Carrow; Couñago, Rafael M; Limas, Juanita C; Almeida, Tuanny L; Cook, Jeanette Gowen; Drewry, David H; Elkins, Jonathan M; Gileadi, Opher; Kapadia, Nirav R; Lorente-Macias, Alvaro; Pickett, Julie E; Riemen, Alexander; Ruela-de-Sousa, Roberta R; Willson, Timothy M; Zhang, Cunyu; Zuercher, William J; Zutshi, Reena; Axtman, Alison D.
Afiliação
  • Wells C; Structural Genomics Consortium (SGC), UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill (UNC-CH), Chapel Hill, North Carolina 27599, United States.
  • Couñago RM; Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, UNC-CH, Chapel Hill, North Carolina 27599, United States.
  • Limas JC; SGC, Departamento de Genética e Evolução, Instituto de Biologia, Universidade Estadual de Campinas (UNICAMP), Campinas, SP 13083-886, Brazil.
  • Almeida TL; Centro de Química Medicinal, Centro de Biologia Molecular e Engenharia Genética, UNICAMP, Campinas, SP 13083-875, Brazil.
  • Cook JG; Department of Pharmacology, UNC-CH, Chapel Hill, North Carolina 27599, United States.
  • Drewry DH; SGC, Departamento de Genética e Evolução, Instituto de Biologia, Universidade Estadual de Campinas (UNICAMP), Campinas, SP 13083-886, Brazil.
  • Elkins JM; Centro de Química Medicinal, Centro de Biologia Molecular e Engenharia Genética, UNICAMP, Campinas, SP 13083-875, Brazil.
  • Gileadi O; Department of Biochemistry and Biophysics, UNC-CH, Chapel Hill, North Carolina 27599, United States.
  • Kapadia NR; Structural Genomics Consortium (SGC), UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill (UNC-CH), Chapel Hill, North Carolina 27599, United States.
  • Lorente-Macias A; Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, UNC-CH, Chapel Hill, North Carolina 27599, United States.
  • Pickett JE; SGC, Departamento de Genética e Evolução, Instituto de Biologia, Universidade Estadual de Campinas (UNICAMP), Campinas, SP 13083-886, Brazil.
  • Riemen A; SGC, Nuffield Department of Clinical Medicine, University of Oxford, Old Road Campus Research Building, Oxford, OX3 7DQ, U.K.
  • Ruela-de-Sousa RR; SGC, Departamento de Genética e Evolução, Instituto de Biologia, Universidade Estadual de Campinas (UNICAMP), Campinas, SP 13083-886, Brazil.
  • Willson TM; SGC, Nuffield Department of Clinical Medicine, University of Oxford, Old Road Campus Research Building, Oxford, OX3 7DQ, U.K.
  • Zhang C; Structural Genomics Consortium (SGC), UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill (UNC-CH), Chapel Hill, North Carolina 27599, United States.
  • Zuercher WJ; Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, UNC-CH, Chapel Hill, North Carolina 27599, United States.
  • Zutshi R; Departamento de Química Farmacéutica y Orgánica, University of Granada, Granada, 18071, Spain.
  • Axtman AD; Structural Genomics Consortium (SGC), UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill (UNC-CH), Chapel Hill, North Carolina 27599, United States.
ACS Med Chem Lett ; 11(3): 340-345, 2020 Mar 12.
Article em En | MEDLINE | ID: mdl-32184967
ABSTRACT
Inhibitors based on a 3-acylaminoindazole scaffold were synthesized to yield potent dual AAK1/BMP2K inhibitors. Optimization furnished a small molecule chemical probe (SGC-AAK1-1, 25) that is potent and selective for AAK1/BMP2K over other NAK family members, demonstrates narrow activity in a kinome-wide screen, and is functionally active in cells. This inhibitor represents one of the best available small molecule tools to study the functions of AAK1 and BMP2K.
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Texto completo: 1 Base de dados: MEDLINE Idioma: En Ano de publicação: 2020 Tipo de documento: Article
Texto completo
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XML
PubMed Links
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Texto completo: 1 Base de dados: MEDLINE Idioma: En Ano de publicação: 2020 Tipo de documento: Article