Chemistry:SHP099
From HandWiki
SHP099 is a drug that acts as an inhibitor of the protein tyrosine phosphatase enzyme SHP-2 (PTPN11). It was developed as a potential agent for the treatment of cancer, but while it is potent, orally active and effective at inhibiting SHP-2 activity and slowing tumor growth, it was not developed for clinical use because of dose-limiting side effects. However it continues to be widely used in cancer research and a number of related derivatives have been developed.[1][2][3][4][5][6][7] It has also been used to research the role of SHP-2 in other processes such as regulation of bone growth during development.[8][9]
See also
- SA-8
- Vociprotafib
References
- ↑ "Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases". Nature 535 (7610): 148–152. July 2016. doi:10.1038/nature18621. PMID 27362227. Bibcode: 2016Natur.535..148C.
- ↑ "Allosteric Inhibition of SHP2: Identification of a Potent, Selective, and Orally Efficacious Phosphatase Inhibitor". Journal of Medicinal Chemistry 59 (17): 7773–7782. September 2016. doi:10.1021/acs.jmedchem.6b00680. PMID 27347692.
- ↑ "Phosphatase-independent functions of SHP2 and its regulation by small molecule compounds". Journal of Pharmacological Sciences 144 (3): 139–146. November 2020. doi:10.1016/j.jphs.2020.06.002. PMID 32921395.
- ↑ "Allosteric Inhibitors of SHP2: An Updated Patent Review (2015-2020)". Current Medicinal Chemistry 28 (19): 3825–3842. 2021. doi:10.2174/1568011817666200928114851. PMID 32988341.
- ↑ "A patent review of SHP2 allosteric inhibitors (2018-present)". Expert Opinion on Therapeutic Patents 34 (5): 383–396. May 2024. doi:10.1080/13543776.2024.2365410. PMID 38842843.
- ↑ "SHP2 is a multifunctional target in anaplastic thyroid carcinoma: Cell intrinsic and immune-dependent anti-tumor effects". Biomedicine & Pharmacotherapy 190. September 2025. doi:10.1016/j.biopha.2025.118384. PMID 40752423.
- ↑ "Structural insights into the binding modes of SHP2 allosteric inhibitors". In Silico Pharmacology 14 (1). 2026. doi:10.1007/s40203-025-00551-x. PMID 41613633.
- ↑ "From Stem to Sternum: The Role of Shp2 in the Skeleton". Calcified Tissue International 112 (4): 403–421. April 2023. doi:10.1007/s00223-022-01042-3. PMID 36422682.
- ↑ "SHP2 inhibition by SHP099 attenuates IL-6-driven osteoclastogenesis in growth plate injury". Frontiers in Immunology 16. 2025. doi:10.3389/fimmu.2025.1659230. PMID 40895539.
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