Identification Of A Novel Potent And Orally Bioavailable Guanidine Src homology 2 domain containing protein tyrosine phosphatase 2 (shp2) is a highly attractive therapeutic target for treating kirsten rat sarcoma viral oncogene (kras) mutant cancers. in this work, a series of guanidine based shp2 allosteric inhibitors were discovered via virtual screening and rational structural optimization. notably, lead compound 23 with potent shp2 inhibitory activity. In this work, a series of guanidine based shp2 allosteric inhibitors were discovered via virtual screening and ratio … identification of a novel, potent, and orally bioavailable guanidine based shp2 allosteric inhibitor from virtual screening and rational structural optimization for the treatment of kras mutant cancers.
Figure 1 From Identification And Preclinical Characterization Of Az 23 Doi: 10.1021 acs.jmedchem.3c00992 corpus id: 263150999; identification of a novel, potent, and orally bioavailable guanidine based shp2 allosteric inhibitor from virtual screening and rational structural optimization for the treatment of kras mutant cancers. In this work, a series of guanidine based shp2 allosteric inhibitors were discovered via virtual screening and rational structural optimization. notably, lead compound 23 with potent shp2 inhibitory activity (ic 50 = 17.7 nm) effectively inhibited the proliferation, migration, and invasion of mia paca 2 pancreatic cancer cells. Here we report the discovery of a highly potent (ic50 = 0.071 μm), selective and orally bioavailable small molecule shp2 inhibitor, shp099, that stabilizes shp2 in an auto inhibited conformation. Identification of a novel, potent, and orally bioavailable guanidine based shp2 allosteric inhibitor from virtual screening and rational structural optimization for the treatment of kras mutant cancers.
Figure 3 From Identification And Preclinical Characterization Of Az 23 Here we report the discovery of a highly potent (ic50 = 0.071 μm), selective and orally bioavailable small molecule shp2 inhibitor, shp099, that stabilizes shp2 in an auto inhibited conformation. Identification of a novel, potent, and orally bioavailable guanidine based shp2 allosteric inhibitor from virtual screening and rational structural optimization for the treatment of kras mutant cancers. Identification of a novel, potent, and orally bioavailable guanidine based shp2 allosteric inhibitor from virtual screening and rational structural optimization for the treatment of kras mutant cancers. qiangqiang hou, wenhua jiang, wenqiang li, chenyang huang, kexin yang, xiaoyu chen, mengchen huang, chengxia shu, guangmei luo, haopeng sun. Src homology 2 domain containing protein tyrosine phosphatase 2 (shp2) is a highly attractive therapeutic target for treating kirsten rat sarcoma viral oncogene (kras) mutant cancers. in this work, a series of guanidine based shp2 allosteric inhibitors were discovered via virtual screening and rational structural optimization. notably, lead compound 23 with potent shp2 inhibitory activity.
Pdf Identification And Characterization Of Ndt 9513727 A Novel Identification of a novel, potent, and orally bioavailable guanidine based shp2 allosteric inhibitor from virtual screening and rational structural optimization for the treatment of kras mutant cancers. qiangqiang hou, wenhua jiang, wenqiang li, chenyang huang, kexin yang, xiaoyu chen, mengchen huang, chengxia shu, guangmei luo, haopeng sun. Src homology 2 domain containing protein tyrosine phosphatase 2 (shp2) is a highly attractive therapeutic target for treating kirsten rat sarcoma viral oncogene (kras) mutant cancers. in this work, a series of guanidine based shp2 allosteric inhibitors were discovered via virtual screening and rational structural optimization. notably, lead compound 23 with potent shp2 inhibitory activity.
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