Design, synthesis and biological evaluation of pyridine derivatives as selective SHP2 inhibitors.
Sign Up to like & getrecommendations! Published in 2020 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2020.103875
Abstract: SHP2 is a non-receptor protein tyrosine phosphatase encoded by the PTPN11 gene, which affects the transduction of multiple signaling pathways, including RAS-ERK, PI3K-AKT and JAK-STAT. SHP2 also plays an important role in the programmed cell… read more here.
Keywords: selective shp2; shp2; shp2 inhibitors; activity ... See more keywords
From Pyrazolones to Azaindoles: Evolution of Active-Site SHP2 Inhibitors Based on Scaffold Hopping and Bioisosteric Replacement.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.0c01265
Abstract: The tyrosine phosphatase SHP2 controls the activity of pivotal signaling pathways, including MAPK, JAK-STAT, and PI3K-Akt. Aberrant SHP2 activity leads to uncontrolled cell proliferation, tumorigenesis, and metastasis. SHP2 signaling was recently linked to drug resistance… read more here.
Keywords: shp2; shp2 inhibitors; scaffold hopping; hopping bioisosteric ... See more keywords
6-Amino-3-methylpyrimidinones as Potent, Selective, and Orally Efficacious SHP2 Inhibitors.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.8b01726
Abstract: Protein tyrosine phosphatase SHP2 is an oncoprotein associated with cancer as well as a potential immune modulator because of its role in the programmed cell death PD-L1/PD-1 pathway. In the preceding manuscript, we described the… read more here.
Keywords: shp2; potent selective; amino methylpyrimidinones; methylpyrimidinones potent ... See more keywords
Targeting SHP2 phosphatase in hematological malignancies
Sign Up to like & getrecommendations! Published in 2022 at "Expert Opinion on Therapeutic Targets"
DOI: 10.1080/14728222.2022.2066518
Abstract: ABSTRACT Introduction Src homology-2-containing protein tyrosine phosphatase 2 (SHP2) is a ubiquitously expressed, non-receptor protein tyrosine phosphatase encoded by the PTPN11 gene. Gain-of-function (GOF) mutations in PTPN11 are associated with the development of various hematological… read more here.
Keywords: phosphatase; shp2 inhibitors; hematological malignancies; drug resistance ... See more keywords
Data-Driven Computational Modeling Identifies Determinants of Glioblastoma Response to SHP2 Inhibition
Sign Up to like & getrecommendations! Published in 2021 at "Cancer Research"
DOI: 10.1158/0008-5472.can-20-1756
Abstract: These findings demonstrate that allosteric SHP2 inhibitors have multivariate and context-dependent effects in glioblastoma that may make them useful components of some combination therapies, but not others. Oncogenic protein tyrosine phosphatases have long been viewed… read more here.
Keywords: glioblastoma; response; shp2 inhibitors; shp2 ... See more keywords
Abstract 1176: Preclinical characterization of the pharmacokinetic-pharmacodynamics-efficacy relationship of novel allosteric SHP2 inhibitors
Sign Up to like & getrecommendations! Published in 2017 at "Cancer Research"
DOI: 10.1158/1538-7445.am2017-1176
Abstract: SHP2 is a non-receptor protein tyrosine phosphatase downstream of receptor tyrosine kinases (RTK). Mutations yielding constitutive activation of SHP2 primarily lead to activation of the MAPK pathway and have been found in multiple tumor types.… read more here.
Keywords: novel allosteric; shp2; allosteric shp2; shp2 inhibitors ... See more keywords
Shipping Out MEK Inhibitor Resistance with SHP2 Inhibitors.
Sign Up to like & getrecommendations! Published in 2018 at "Cancer discovery"
DOI: 10.1158/2159-8290.cd-18-0915
Abstract: RAS is one of the most frequently altered oncogenes, yet RAS-driven tumors are largely refractory to anticancer therapies. Fedele and colleagues demonstrate that SHP2 inhibitors prevent adaptive MEK inhibitor resistance; therefore, combining MEK and SHP2… read more here.
Keywords: inhibitor resistance; shp2 inhibitors; mek inhibitor;
SHP2 Inhibitors Show Anti-Myeloma Activity and Synergize With Bortezomib in the Treatment of Multiple Myeloma
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Pharmacology"
DOI: 10.3389/fphar.2022.841308
Abstract: Multiple myeloma (MM) is a plasma cell malignancy that remains incurable. The protein tyrosine phosphatase SHP2 is a central node regulating RAS/mitogen-activated protein kinase (MAPK)/extracellular signal regulated kinase (ERK) signaling pathway which plays a crucial… read more here.
Keywords: myeloma; shp2 inhibitors; activity; shp2 ... See more keywords
Toward a Treatment of Cancer: Design and In Vitro/In Vivo Evaluation of Uncharged Pyrazoline Derivatives as a Series of Novel SHP2 Inhibitors
Sign Up to like & getrecommendations! Published in 2022 at "International Journal of Molecular Sciences"
DOI: 10.3390/ijms23073497
Abstract: Src homology 2 domain-containing protein tyrosine phosphatase 2 (SHP2) is a non-receptor protein tyrosine phosphatase (PTP) encoded by the PTPN11 gene, which is involved in the RAS/MAPK cell signaling transduction process. SHP2 has been shown… read more here.
Keywords: vitro vivo; toward treatment; series; pyrazoline derivatives ... See more keywords
The Discovery of Potent SHP2 Inhibitors with Anti-Proliferative Activity in Breast Cancer Cell Lines
Sign Up to like & getrecommendations! Published in 2022 at "International Journal of Molecular Sciences"
DOI: 10.3390/ijms23084468
Abstract: Despite available treatments, breast cancer is the leading cause of cancer-related death. Knowing that the tyrosine phosphatase SHP2 is a regulator in tumorigenesis, developing inhibitors of SHP2 in breast cells is crucial. Our study investigated… read more here.
Keywords: breast; breast cancer; activity; shp2 inhibitors ... See more keywords