January 2024
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7 Reads
Journal of Medicinal Chemistry
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January 2024
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7 Reads
Journal of Medicinal Chemistry
September 2023
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14 Reads
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1 Citation
Journal of Medicinal Chemistry
March 2023
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7 Reads
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10 Citations
Journal of Medicinal Chemistry
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.
April 2022
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18 Reads
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11 Citations
Journal of Medicinal Chemistry
... Small molecule SOS1 inhibitors modulate RAS activation by binding to the SOS1 protein pocket, affecting the interaction between SOS1 and RAS. 8,9 Fig. 2 shows some examples of reported SOS1 compounds. For instance, Hillig et al. reported an aminoquinazoline inhibitor, BAY-293, based on fragment and high-throughput screening for the KRAS-SOS1 binding site. ...
March 2023
Journal of Medicinal Chemistry
... In a similar vein, we found that the SF 5 -CB moiety is compatible with S N Ar conditions. [47] That is, we converted 5 to 58 and in 70 % isolated yield. In both cases, note that the SF 5 -CB survived heating under basic conditions. ...
April 2022
Journal of Medicinal Chemistry