Guangmei Luo's research while affiliated with China Pharmaceutical University and other places

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Publications (4)


Discovery of Novel Phenoxyaryl Pyridones as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with High Selectivity for the Second Bromodomain (BD2) to Potentially Treat Acute Myeloid Leukemia
  • Article

January 2024

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7 Reads

Journal of Medicinal Chemistry

Wenhua Jiang

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Qiangqiang Hou

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Hongrui Xu

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[...]

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

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.


Citations (2)


... 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. ...

Reference:

Discovery of Novel SOS1 Inhibitors Using Machine Learning
Development of Son of Sevenless Homologue 1 (SOS1) Modulators To Treat Cancers by Regulating RAS Signaling
  • Citing Article
  • 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. ...

Discovery of a Novel Src Homology-2 Domain Containing Protein Tyrosine Phosphatase-2 (SHP2) and Cyclin-Dependent Kinase 4 (CDK4) Dual Inhibitor for the Treatment of Triple-Negative Breast Cancer
  • Citing Article
  • April 2022

Journal of Medicinal Chemistry