4.7 Article

Development of Son of Sevenless Homologue 1 (SOS1) Modulators To Treat Cancers by Regulating RAS Signaling

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JOURNAL OF MEDICINAL CHEMISTRY
卷 66, 期 7, 页码 4324-4341

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AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.2c01729

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Son of sevenless homologue 1 (SOS1) protein is expressed in all cells and plays a crucial role in the RAS signaling pathway by interacting with RAS and activating downstream signaling pathways. Targeting SOS1 provides a novel approach for treating RAS-driven cancers.
Son of sevenless homologue 1 (SOS1) protein is universally expressed in cells and plays an important role in the RAS signaling pathway. Specifically, this protein interacts with RAS in response to upstream stimuli to promote guanine nucleotide exchange in RAS and activates the downstream signaling pathways. Thus, targeting SOS1 is a new approach for treating RAS-driven cancers. In this Perspective, we briefly summarize the structural and functional aspects of SOS1 and focus on recent advances in the discovery of activators, inhibitors, and PROTACs that target SOS1. This review aims to provide a timely and updated overview on the strategies for targeting SOS1 in cancer therapy.

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