WebMar 13, 2024 · CX-5461 is a novel selective inhibitor of RNA polymerase I. Our previous studies have shown that CX-5461 has potent anti-inflammatory effects. Here we investigated whether CX-5461 could inhibit the development of imiquimod-induced experimental psoriasis in … WebCX-5461 is a first-in-class non-genotoxic small molecule targeted inhibitor of RNA polymerase I (Pol I) that activates the p53 pathway without causing DNA damage. …
Biomedicines Free Full-Text Targeting RNA Polymerase I ...
WebApply to this Phase 1 clinical trial treating Metastatic Cancers, Locally Advanced Solid Tumors, Neoplasm Metastasis. Get access to cutting edge treatment via CTX-471. … WebTo establish the pharmacokinetic (PK) profile of CX-5461. To observe patients for evidence of CX-5461 biological activity using pharmacodynamic (PD) assessments. To observe … djei
CX-5461 is an Orally Active rRNA Synthesis Inhibitor
WebCX-5461 is a recently discovered small-molecule selective Pol I inhibitor, which can inhibit Pol I-driven rRNA transcription via disrupting the recruitment of Pol I to rDNA promoter, but does not inhibit Pol II-driven messenger RNA (mRNA) synthesis or DNA replication or protein translation. 10 Several studies demonstrated that CX-5461 could … WebSelective RBG inhibitors, including CX-54613 [ 14, 15, 16, 17, 18 ], have been developed as anticancer agents with limited effects on normal cells. CX-5461 prevents the Pol I transcription initiation factor SL-1 from binding to the rDNA promoter and is currently being evaluated in a Phase I clinical trial for breast cancer (NCT02719977). WebNov 9, 2024 · We first tested 2-drug combinations of CX-5461 with pharmacologically relevant dosages of AZD-1390 (ATMi), AZD-6738 (ATRi), and the liposomal formulation … djei epos