Results 131 to 140 of about 10,714 (176)
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Novel PROTACs for degradation of SHP2 protein
Bioorganic Chemistry, 2021Protein tyrosine phosphatase SHP2 is a member of PTPs family associated with cancer such as leukemia, non-small cell lung cancer, breast cancer, and so on. SHP2 is a promising target for drug development, and consequently it is of great significance to develop SHP2 inhibitors.
Yirong Zhou, Hua Li, Lixia Chen
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Discovery of SHP2-D26 as a First, Potent, and Effective PROTAC Degrader of SHP2 Protein
Journal of Medicinal Chemistry, 2020Src homology 2 domain-containing phosphatase 2 (SHP2) is an attractive therapeutic target for human cancers and other human diseases. Herein, we report our discovery of potent small-molecule SHP2 degraders whose design is based upon the proteolysis-targeting chimera (PROTAC) concept.
Mingliang Wang +4 more
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The role of Shp2 (PTPN11) in cancer
Current Opinion in Genetics & Development, 2007Tyrosyl phosphorylation, which is controlled by protein-tyrosine kinases (PTKs) and protein-tyrosine phosphatases (PTPs), regulates numerous cellular processes. Altered expression and/or mutations in PTKs are linked to many forms of cancer, yet until recently little was known about the roles of PTPs in normal cells or in cancer.
M Golam, Mohi, Benjamin G, Neel
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Engineering SHP2 Phosphatase for Optical Control
Biochemistry, 2022Signal transduction pathways are responsible for maintaining cellular functions, including proliferation, differentiation, apoptosis, and cell cycle progression. These pathways are maintained through the propagation of phosphorylation signals by protein kinases, as well as the removal of phosphorylation signals by protein phosphatases. Depending on the
Amy Ryan +3 more
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SHP2 sails from physiology to pathology
European Journal of Medical Genetics, 2015Over the two past decades, mutations of the PTPN11 gene, encoding the ubiquitous protein tyrosine phosphatase SHP2 (SH2 domain-containing tyrosine phosphatase 2), have been identified as the causal factor of several developmental diseases (Noonan syndrome (NS), Noonan syndrome with multiple lentigines (NS-ML), and metachondromatosis), and malignancies (
Mylène, Tajan +4 more
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The Tyrosine Phosphatase Shp2 in Development and Cancer
2010Deregulation of signaling pathways, through mutation or other molecular changes, can ultimately result in disease. The tyrosine phosphatase Shp2 has emerged as a major regulator of receptor tyrosine kinase (RTK) and cytokine receptor signaling. In the last decade, germline mutations in the human PTPN11 gene, encoding Shp2, were linked to Noonan (NS ...
Katja S, Grossmann +3 more
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The biological function of SHP2 in human disease
Molecular Biology, 2016Tyrosyl phosphorylation participates in various pathological and physiological processes, which are regulated by protein tyrosine kinases (PTKs) and protein tyrosine phosphatases (PTPs). The Src homology-2 domain containing phosphatase SHP2 (encoded by PTPN11) is an important phosphatase, which was found to be implicated in the regulation of genetic ...
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Genentech licenses Relay’s SHP2 inhibitor
Chemical & Engineering News, 2020Genentech will pay $75 million to license RLY-1971, Relay Therapeutics’ SHP2 inhibitor, which is in a Phase 1 trial to treat solid tumors.
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The tyrosine phosphatase Shp2 (PTPN11) in cancer
Cancer and Metastasis Reviews, 2008Diverse cellular processes are regulated by tyrosyl phosphorylation, which is controlled by protein-tyrosine kinases (PTKs) and protein-tyrosine phosphatases (PTPs). De-regulated tyrosyl phosphorylation, evoked by gain-of-function mutations and/or over-expression of PTKs, contributes to the pathogenesis of many cancers and other human diseases.
Gordon, Chan +2 more
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2023
It is clear by now that CRISPR screens are a useful tool to identify and validate novel targets for the treatment of various malignancies. Furthermore, genetic screens have allowed the identification of not only the usual kinases but also other genes with different functions in the cell such as epigenetic regulators or phosphatases. SHP2 was discovered
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It is clear by now that CRISPR screens are a useful tool to identify and validate novel targets for the treatment of various malignancies. Furthermore, genetic screens have allowed the identification of not only the usual kinases but also other genes with different functions in the cell such as epigenetic regulators or phosphatases. SHP2 was discovered
openaire +1 more source