Discovery and Optimization of wt-RET/KDR-Selective Inhibitors of RET<sup>V804M</sup> Kinase.

Newton, Rebecca; Waszkowycz, Bohdan; Seewooruthun, Chitra; Burschowsky, Daniel; Richards, Mark; Hitchin, Samantha; Begum, Habiba; Watson, Amanda; French, Eleanor; Hamilton, Niall; Jones, Stuart; Lin, Li-Ying; Waddell, Ian; Echalier, Aude; Bayliss, Richard; Jordan, Allan M; Ogilvie, Donald

Discovery and Optimization of wt-RET/KDR-Selective Inhibitors of RET^V804M Kinase.

Newton, Rebecca; Waszkowycz, Bohdan; Seewooruthun, Chitra; Burschowsky, Daniel; Richards, Mark; Hitchin, Samantha; Begum, Habiba; Watson, Amanda; French, Eleanor; Hamilton, Niall; Jones, Stuart; Lin, Li-Ying; Waddell, Ian; Echalier, Aude; Bayliss, Richard; Jordan, Allan M; Ogilvie, Donald.

Afiliação

Newton R; Drug Discovery Unit, Cancer Research UK, Manchester Institute, University of Manchester, Alderley Park, Macclesfield SK10 4TG, U.K.
Waszkowycz B; Drug Discovery Unit, Cancer Research UK, Manchester Institute, University of Manchester, Alderley Park, Macclesfield SK10 4TG, U.K.
Seewooruthun C; Department of Molecular and Cell Biology, Henry Wellcome Building, University of Leicester, Lancaster Road, Leicester LE1 7RH, U.K.
Burschowsky D; Department of Molecular and Cell Biology, Henry Wellcome Building, University of Leicester, Lancaster Road, Leicester LE1 7RH, U.K.
Richards M; Astbury Centre for Structural Molecular Biology, Faculty of Biological Sciences, University of Leeds, Leeds LS2 9JT, U.K.
Hitchin S; Drug Discovery Unit, Cancer Research UK, Manchester Institute, University of Manchester, Alderley Park, Macclesfield SK10 4TG, U.K.
Begum H; Drug Discovery Unit, Cancer Research UK, Manchester Institute, University of Manchester, Alderley Park, Macclesfield SK10 4TG, U.K.
Watson A; Drug Discovery Unit, Cancer Research UK, Manchester Institute, University of Manchester, Alderley Park, Macclesfield SK10 4TG, U.K.
French E; Drug Discovery Unit, Cancer Research UK, Manchester Institute, University of Manchester, Alderley Park, Macclesfield SK10 4TG, U.K.
Hamilton N; Drug Discovery Unit, Cancer Research UK, Manchester Institute, University of Manchester, Alderley Park, Macclesfield SK10 4TG, U.K.
Jones S; Drug Discovery Unit, Cancer Research UK, Manchester Institute, University of Manchester, Alderley Park, Macclesfield SK10 4TG, U.K.
Lin LY; Leicester Drug Discovery & Diagnostics Centre (LD3), R407a, Hodgkin Building, Lancaster Road, Leicester LE1 7HB, U.K.
Waddell I; Drug Discovery Unit, Cancer Research UK, Manchester Institute, University of Manchester, Alderley Park, Macclesfield SK10 4TG, U.K.
Echalier A; Department of Molecular and Cell Biology, Henry Wellcome Building, University of Leicester, Lancaster Road, Leicester LE1 7RH, U.K.
Bayliss R; Astbury Centre for Structural Molecular Biology, Faculty of Biological Sciences, University of Leeds, Leeds LS2 9JT, U.K.
Jordan AM; Drug Discovery Unit, Cancer Research UK, Manchester Institute, University of Manchester, Alderley Park, Macclesfield SK10 4TG, U.K.
Ogilvie D; Drug Discovery Unit, Cancer Research UK, Manchester Institute, University of Manchester, Alderley Park, Macclesfield SK10 4TG, U.K.

ACS Med Chem Lett ; 11(4): 497-505, 2020 Apr 09.

Article em En | MEDLINE | ID: mdl-32292556

ABSTRACT

ABSTRACT

A combination of focused library and virtual screening, hit expansion, and rational design has resulted in the development of a series of inhibitors of RETV804M kinase, the anticipated drug-resistant mutant of RET kinase. These agents do not inhibit the wild type (wt) isoforms of RET or KDR and therefore offer a potential adjunct to RET inhibitors currently undergoing clinical evaluation.

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Revista: ACS Med Chem Lett Ano de publicação: 2020 Tipo de documento: Article País de afiliação: Reino Unido

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