Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a 5-Fluoro-4-(3H)-quinazolinone Aryl Urea pan-RAF Kinase Inhibitor-Reference-Cited by-同舟云学术

Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a 5-Fluoro-4-(3H)-quinazolinone Aryl Urea pan-RAF Kinase Inhibitor

Published:2021-03-29 Issue:7 Volume:64 Page:3940-3955
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Huestis Malcolm P.¹^ORCID,Dela Cruz Darlene²,DiPasquale Antonio G.³,Durk Matthew R.⁴,Eigenbrot Charles⁵,Gibbons Paul¹,Gobbi Alberto¹,Hunsaker Thomas L.²,La Hank⁴,Leung Dennis H.³,Liu Wendy¹,Malek Shiva⁶,Merchant Mark²,Moffat John G.⁷,Muli Christine S.³,Orr Christine J.²,Parr Brendan T.¹,Shanahan Frances⁶,Sneeringer Christopher J.⁷,Wang Weiru⁵,Yen Ivana⁶,Yin Jianping⁵,Siu Michael¹^ORCID,Rudolph Joachim¹

Affiliation:

1. Discovery Chemistry, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States

2. Translational Oncology, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States

3. Small Molecule Pharmaceutical Sciences, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States

4. Drug Metabolism and Pharmacokinetics, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States

5. Structural Biology, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States

6. Molecular Oncology, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States

7. Biochemical and Cellular Pharmacology, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States

Funder

Genentech

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.0c02085

Reference58 articles.

1. Targeting RAS–ERK signalling in cancer: promises and challenges

2. Current Development Status of MEK Inhibitors

3. Current Insights of BRAF Inhibitors in Cancer

4. Targeting ERK beyond the boundaries of the kinase active site in melanoma

5. Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity

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