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Antagomir-221 is a chemically modified, cholesterol-conjugated single-stranded RNA analogue designed to silence microRNA-221 (miR-221). miR-221 is an oncogenic microRNA (oncomiR) that is frequently overexpressed in various malignancies, including pancreatic ductal adenocarcinoma, where it promotes tumor growth and progression by downregulating target genes such as the cell cycle inhibitor p27kip1. Antagomir-221 functions by binding with high affinity to the mature miR-221 sequence, leading to its degradation or sequestration and thereby restoring the expression of its target tumor suppressor genes. In preclinical research, antagomir-221 has demonstrated significant antiproliferative activity and has been explored as a potential therapeutic strategy, either alone or in combination with other anticancer agents like benzyl isothiocyanate (BITC).
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