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Design of a Potent, Selective, and Brain-Penetrant Inhibitor of Wnt-Deactivating Enzyme Notum by Optimization of a Crystallographic Fragment Hit.
Willis, Nicky J; Mahy, William; Sipthorp, James; Zhao, Yuguang; Woodward, Hannah L; Atkinson, Benjamin N; Bayle, Elliott D; Svensson, Fredrik; Frew, Sarah; Jeganathan, Fiona; Monaghan, Amy; Benvegnù, Stefano; Jolly, Sarah; Vecchia, Luca; Ruza, Reinis R; Kjær, Svend; Howell, Steven; Snijders, Ambrosius P; Bictash, Magda; Salinas, Patricia C; Vincent, Jean-Paul; Jones, E Yvonne; Whiting, Paul; Fish, Paul V.
Afiliação
  • Willis NJ; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K.
  • Mahy W; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K.
  • Sipthorp J; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K.
  • Zhao Y; The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, U.K.
  • Woodward HL; Division of Structural Biology, Wellcome Centre for Human Genetics, University of Oxford, The Henry Wellcome Building for Genomic Medicine, Roosevelt Drive, Oxford OX3 7BN, U.K.
  • Atkinson BN; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K.
  • Bayle ED; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K.
  • Svensson F; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K.
  • Frew S; The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, U.K.
  • Jeganathan F; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K.
  • Monaghan A; The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, U.K.
  • Benvegnù S; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K.
  • Jolly S; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K.
  • Vecchia L; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K.
  • Ruza RR; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K.
  • Kjær S; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K.
  • Howell S; Division of Structural Biology, Wellcome Centre for Human Genetics, University of Oxford, The Henry Wellcome Building for Genomic Medicine, Roosevelt Drive, Oxford OX3 7BN, U.K.
  • Snijders AP; Division of Structural Biology, Wellcome Centre for Human Genetics, University of Oxford, The Henry Wellcome Building for Genomic Medicine, Roosevelt Drive, Oxford OX3 7BN, U.K.
  • Bictash M; The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, U.K.
  • Salinas PC; The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, U.K.
  • Vincent JP; The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, U.K.
  • Jones EY; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K.
  • Whiting P; Department of Cell and Developmental Biology, Laboratory for Molecular and Cellular Biology, University College London, London WC1E 6BT, U.K.
  • Fish PV; The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, U.K.
J Med Chem ; 65(10): 7212-7230, 2022 05 26.
Article em En | MEDLINE | ID: mdl-35536179
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Inibidores Enzimáticos / Esterases Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2022 Tipo de documento: Article País de afiliação: Reino Unido
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Inibidores Enzimáticos / Esterases Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2022 Tipo de documento: Article País de afiliação: Reino Unido