News Release

Allosteric inhibition reveals SHP2-mediated tumor immunosuppression in colon cancer by single-cell transcriptomics

Peer-Reviewed Publication

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Figure 1

image: SHP2-mediated tumor immunosuppression in colon cancer was defined by scRNA-seq. SHP2 negatively regulates type I interferon signaling. SHP2 allosteric inhibition remolds the anti-tumor TME, indicating SHP2 is a promising target for colon cancer immunotherapy. view more 

Credit: APSB

Colorectal cancer (CRC), a malignant tumor worldwide consists of microsatellite instability (MSI) and stable (MSS) phenotypes. Although SHP2 is a hopeful target for cancer therapy, its relationship with innate immunosuppression remains elusive. To address that, the authors of this article performed single-cell RNA sequencing to explore the role of SHP2 in all cell types of tumor microenvironment (TME) from murine MC38 xenografts. Intratumoral cells were found to be functionally heterogeneous and responded significantly to SHP099, a SHP2 allosteric inhibitor. The malignant evolution of tumor cells was remarkably arrested by SHP099. Mechanistically, STING-TBK1-IRF3-mediated type I interferon signaling was highly activated by SHP099 in infiltrated myeloid cells. Notably, CRC patients with MSS phenotype exhibited greater macrophage infiltration and more potent SHP2 phosphorylation in CD68+ macrophages than MSI-high phenotypes, suggesting the potential role of macrophagic SHP2 in TME.

Collectively, the authors data reveals a mechanism of innate immunosuppression mediated by SHP2, suggesting that SHP2 is a promising target for colon cancer immunotherapy.

Article reference: Gao J, Wu Z, Zhao M, Zhang R, Li M, Sun D, Cheng H, Qi X, Shen Y, XuQ, Chen H, Chen D, Sun Y, Allosteric inhibition reveals SHP2-mediated tumor immunosuppression in colon cancer by single-cell transcriptomics, Acta Pharmaceutica Sinica B, 2021, ISSN 2211-3835, https://doi.org/10.1016/j.apsb.2021.08.006

Keywords: Tumor microenvironment, PTPN11, SHP099, STING, Type I interferon, Colorectal cancers, cRNA-seq, Macrophage

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The Journal of the Institute of Materia Medica, the Chinese Academy of Medical Sciences and the Chinese Pharmaceutical Association.

For more information please visit https://www.journals.elsevier.com/acta-pharmaceutica-sinica-b/

Editorial Board: https://www.journals.elsevier.com/acta-pharmaceutica-sinica-b/editorial-board

 

APSB is available on ScienceDirect (https://www.sciencedirect.com/journal/acta-pharmaceutica-sinica-b).

 

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CiteScore: 12.5

Impact Factor: 11.413

ISSN 2211-3835


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