Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19

Author:

Amrhein Jennifer A.12,Beyett Tyler S.3ORCID,Feng William W.4ORCID,Krämer Andreas12,Weckesser Janik12,Schaeffner Ilse K.3,Rana Jaimin K.3,Jänne Pasi A.4,Eck Michael J.3,Knapp Stefan12ORCID,Hanke Thomas12ORCID

Affiliation:

1. Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Straße 9, 60438 Frankfurt, Germany

2. Structural Genomics Consortium, Buchman Institute for Molecular Life Science (BMLS), Max-von-Laue-Straße 15, 60438 Frankfurt, Germany

3. Department of Cancer Biology, Dana-Farber Cancer Institute, Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, Massachusetts 02215, United States

4. Lowe Center for Thoracic Oncology, Dana-Farber Cancer Institute, Department of Medical Oncology, Department of Medicine, Harvard Medical School, Boston, Massachusetts 02215, United States

Funder

Bayer

Merck KGaA

Genentech

Pfizer

Innovative Medicines Initiative

Genome Canada

Wellcome Trust

AbbVie

Funda??o de Amparo ? Pesquisa do Estado de S?o Paulo

National Institutes of Health

Boehringer Ingelheim

Merck

Janssen Pharmaceuticals

Eshelman Institute for Innovation, University of North Carolina

Canada Foundation for Innovation

Takeda Pharmaceutical Company

SGC

Ruth L. Kirschstein National Research Service Award

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

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