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Restrict the search for
tyrosine
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Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
UNC1062, pyrazolopyrimidine sulfonamide, was identified as a potent and selective inhibitor of C-MER proto-oncogene tyrosine kinase (MERTK. C-MER proto-oncogene tyrosine kinase (MERTK) is a receptor tyrosine kinase with oncogenic properties that is often overexpressed or activated in various malignancies. UNC1062 induced apoptosis in culture, reduced colony formation in soft agar, and inhibited invasion of melanoma cells. UNC1062 attenuates neoplastic phenotype in solid tumor cell lines: reduces cell motility in head and neck cancer cells, inhibits proliferation in gastric cancer cells and inhibits colony formation in non-small cell lung cancer cells.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
PD-153035 is a potent and selective ATP-competitive inhibitor of the epidermal growth factor receptor tyrosine kinase EGFR. PD 153035 shows a potent and selective inhibitory effect on tyrosine phosphorylation induced by EGF in Swiss 3T3 fibroblast and A-431 human epidermoid carcinoma cells. PD153035 shows dose-dependent growth inhibitory effects in cultures of EGF receptor-overexpressing human cancer cell lines (A431, Difi, DU145, MDA-MB-468, and ME180) and in nasopharyngeal carcinoma (NPC) cell lines (NPC-TW01, NPC-TW04, and HONE1). Pretreatment of EGFR inhibitors by 24 hours significantly enhances the cytotoxic effect of doxorubicin, paclitaxel, cisplatin, and 5-fluorouracil in NPCTW04 cells. PD153035 abolishes COX-2 expression induced by the PAR(2)-activating peptide 2-furoyl-LIGRLO-NH(2) (2fLI) in Caco-2 colon cancer cells. In A431 human epidermoid tumors grown as xenografts in immunodeficient nude mice, PD153035 at 80 mg/kg i.p. inhibit EGF receptor tyrosine kinase activity. PD153035 improves glucose tolerance, insulin sensitivity, and signaling and reduces subclinical inflammation in HFD-fed mice.
