Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Editorial
. 2023 Dec 13;15(1):9-11.
doi: 10.1021/acsmedchemlett.3c00521. eCollection 2024 Jan 11.

Inhibitors of Son of Sevenless Isoform 1 (SOS1) as a Potential Treatment for RAS Mutant Cancers

Affiliations
Editorial

Inhibitors of Son of Sevenless Isoform 1 (SOS1) as a Potential Treatment for RAS Mutant Cancers

Ahmed F Abdel-Magid. ACS Med Chem Lett. .

Abstract

The invention in this patent application relates to 1-aminophthalazine derivatives represented generally by formula 1. These compounds are inhibitors of the interaction of the catalytic site of SOS1 with RAS-family proteins which are involved in controlling cell proliferation. They may potentially be used as a treatment for RAS mutant cancers such as pancreatic, lung, and colorectal cancers, cholangiocarcinoma, multiple myeloma, melanoma, and thyroid cancer.

PubMed Disclaimer

Conflict of interest statement

The author declares no competing financial interest.

Similar articles

References

    1. Luo G.; Wang B.; Hou Q.; Wu X. Development of Son of Sevenless Homologue 1 (SOS1) Modulators to Treat Cancers by Regulating RAS Signaling. J. Med. Chem. 2023, 66 (7), 4324–4341. 10.1021/acs.jmedchem.2c01729. - DOI - PubMed
    1. Hillig R. C.; Bader B. Targeting RAS oncogenesis with SOS1 inhibitors. Adv. Cancer Res. 2022, 153, 169–203. 10.1016/bs.acr.2021.07.001. - DOI - PubMed
    1. Kessler D.; Gerlach D.; Kraut N.; McConnell D. B. Targeting Son of Sevenless 1: The pacemaker of KRAS. Curr. Opin. Chem. Biol. 2021, 62, 109–118. 10.1016/j.cbpa.2021.02.014. - DOI - PubMed
    1. Sheffels E.; Kortum R. L. The Role of Wild-Type RAS in Oncogenic RAS Transformation. Genes. 2021, 12 (5), 662–679. 10.3390/genes12050662. - DOI - PMC - PubMed
    1. Prior I. A.; Hood F. E.; Hartley J. L. The frequency of RAS mutations in cancer. Cancer Res. 2020, 80, 2969–2974. 10.1158/0008-5472.CAN-19-3682. - DOI - PMC - PubMed

Publication types

LinkOut - more resources