Bioisosteric Discovery of NPA101.3, a Second-Generation RET/VEGFR2 Inhibitor Optimized for Single-Agent Polypharmacology

[Image: see text] RET receptor tyrosine kinase is a driver oncogene in human cancer. We recently identified the clinical drug candidate Pz-1, which targets RET and VEGFR2. A key in vivo metabolite of Pz-1 is its less active demethylated pyrazole analogue. Using bioisosteric substitution methods, her...

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Detalles Bibliográficos
Autores principales: Moccia, Marialuisa, Frett, Brendan, Zhang, Lingtian, Lakkaniga, Naga Rajiv, Briggs, David C., Chauhan, Rakhee, Brescia, Annalisa, Federico, Giorgia, Yan, Wei, Santoro, Massimo, McDonald, Neil Q., Li, Hong-yu, Carlomagno, Francesca
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2020
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7901654/
https://www.ncbi.nlm.nih.gov/pubmed/32298114
http://dx.doi.org/10.1021/acs.jmedchem.9b01336

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