WebFeb 9, 2024 · The polyoxometalate [TiW 11 CoO 40] 8-(PSB-POM141) is the most potent and selective NPP1 inhibitor described to date (K i = 1.46 nM vs. ATP, human soluble NPP1); it displays an allosteric mechanism of inhibition and represents a useful pharmacological tool for evaluating the potential of NPP1 as a novel drug target. WebNov 19, 2024 · Recently, ENPP1 has emerged as a critical phosphodiesterase that degrades the stimulator of interferon genes (STING) ligand, cyclic GMP-AMP …
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WebENPP1 inhibition is superior to targeting STING directly. ENPP1 is primed by DNA damage and cytoplasmic DNA leaks (safer, specific) •ENPP1 inhibition has a broader … WebJul 1, 2024 · These results demonstrated ZXP-8202 as a potent ENPP1 inhibitor, blocking 2'3-cGAMP hydrolysis by ENPP1, subsequently activating STING pathway. ZXP-8202 was dosed in CT26 syngeneic mouse model for 14 days and achieved about 70% tumor growth inhibition. No body weight loss was observed at this efficacious dose during treatment. maik willems bastion
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WebFeb 26, 2024 · Recent studies have shown that the expression of ENPP1 is related to differentiation, death, dissemination and chemosensitivity of tumor cells. So far, there is no research in ovarian carcinoma. This study aimed at exploring the role of ENPP1 gene in ovarian carcinoma, the relationship with prognostic indicators and chemotherapy … WebENPP1 contains two somatomedin-B-like domains (i.e. SMB 1 and 2) involved in ENPP1 dimerization in animal cells. The aim of the present study was to investigate if these domains modulate ENPP1 inhibitory activity on insulin signaling in human insulin target cells (HepG2). ENPP1 (ENPP1-3'myc), ENPP1 deleted of SMB 1 (ENPP1-ΔI-3'myc) or of … WebFeb 9, 2024 · This study is an open-label, multi-site Phase 1a/1b study of RBS2418, a selective ENPP1 inhibitor, in combination with pembrolizumab or as a monotherapy in subjects with advanced unresectable, recurrent or metastatic tumors. oak end way chinnor