七号无翅型同源物1（SOS1）异构体抑制剂作为RAS突变型癌症的潜在治疗方法
Inhibitors of Son of Sevenless Isoform 1 (SOS1) as a Potential Treatment for RAS Mutant Cancers.
作者信息
Abdel-Magid Ahmed F
机构信息
Therachem Research Medilab, LLC, 100 Jade Park, Chelsea, Alabama 35043, United States.
出版信息
ACS Med Chem Lett. 2023 Dec 13;15(1):9-11. doi: 10.1021/acsmedchemlett.3c00521. eCollection 2024 Jan 11.
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.
摘要
本专利申请中的发明涉及一般由式1表示的1-氨基酞嗪衍生物。这些化合物是SOS1催化位点与参与控制细胞增殖的RAS家族蛋白相互作用的抑制剂。它们有可能用于治疗RAS突变型癌症，如胰腺癌、肺癌、结直肠癌、胆管癌、多发性骨髓瘤、黑色素瘤和甲状腺癌。
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本文引用的文献
1
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J Med Chem. 2023 Apr 13;66(7):4324-4341. doi: 10.1021/acs.jmedchem.2c01729. Epub 2023 Mar 28.
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Targeting RAS oncogenesis with SOS1 inhibitors.针对 SOS1 抑制剂的 RAS 致癌作用。
Adv Cancer Res. 2022;153:169-203. doi: 10.1016/bs.acr.2021.07.001. Epub 2021 Sep 15.
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The Role of Wild-Type RAS in Oncogenic RAS Transformation.野生型 RAS 在致癌性 RAS 转化中的作用。
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Targeting Son of Sevenless 1: The pacemaker of KRAS.靶向 Sevenless 同源物 1：KRAS 的起搏器。
Curr Opin Chem Biol. 2021 Jun;62:109-118. doi: 10.1016/j.cbpa.2021.02.014. Epub 2021 Apr 10.
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SOS GEFs in health and disease.SOS GEFs 在健康和疾病中的作用。
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