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

Author:

Moccia Marialuisa1,Frett Brendan23,Zhang Lingtian2,Lakkaniga Naga Rajiv2ORCID,Briggs David C.4,Chauhan Rakhee4,Brescia Annalisa1,Federico Giorgia1,Yan Wei2,Santoro Massimo1,McDonald Neil Q.45,Li Hong-yu23ORCID,Carlomagno Francesca16ORCID

Affiliation:

1. Dipartimento di Medicina Molecolare e Biotecnologie Mediche, Università di Napoli “Federico II”, 80131 Napoli, Italy

2. Department of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, Little Rock, Arkansas 72205, United States

3. Synactix Pharmaceuticals, Inc., Tucson, Arizona 85718, United States

4. Signalling and Structural Biology Laboratory, The Francis Crick Institute, London NW1 1AT, U.K.

5. Institute of Structural and Molecular Biology, Department of Biological Sciences, Birkbeck College, London WC1E 7HX, U.K.

6. Istituto di Endocrinologia ed Oncologia Sperimentale del CNR, 80131 Napoli, Italy

Funder

National Cancer Institute

European Commission

Ministero dell?Istruzione, dell?Universit? e della Ricerca

Associazione Italiana per la Ricerca sul Cancro

University of Arkansas for Medical Sciences

Wellcome Trust

American Thyroid Association

National Institute of General Medical Sciences

Regione Campania

Cancer Research UK

Association for Multiple Endocrine Neoplasia Disorders

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

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