Bouvard, Claire Lim, Sang Min Ludka, John Yazdani, Nahid Woods, Ashley K. Chatterjee, Arnab K. Schultz, Peter G. Zhu, Shoutian 2024-01-20T02:01:16Z 2024-01-20T02:01:16Z 2021-09-01 2017-03-28 0027-8424 https://pubs.kist.re.kr/handle/201004/122936 Stauprimide is a staurosporine analog that promotes embryonic stem cell (ESC) differentiation by inhibiting nuclear localization of the MYC transcription factor NME2, which in turn results in downregulation of MYC transcription. Given the critical role the oncogene MYC plays in tumor initiation and maintenance, we explored the potential of stauprimide as an anticancer agent. Here we report that stauprimide suppresses MYC transcription in cancer cell lines derived from distinct tissues. Using renal cancer cells, we confirmed that stauprimide inhibits NME2 nuclear localization. Gene expression analysis also confirmed the selective down-regulation of MYC target genes by stauprimide. Consistent with this activity, administration of stauprimide inhibited tumor growth in rodent xenograft models. Our study provides a unique strategy for selectively targeting MYC transcription by pharmacologicalmeans as a potential treatment for MYC-dependent tumors. English NATL ACAD SCIENCES EMBRYONIC STEM-CELLS MURINE C-MYC G-QUADRUPLEX TRANSGENIC MICE TUMOR MICROENVIRONMENT NEOPLASTIC PHENOTYPE LUNG-CANCER PROMOTER INHIBITION EXPRESSION Small molecule selectively suppresses MYC transcription in cancer cells Article 10.1073/pnas.1702663114 1 PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, v.114, no.13, pp.3497 - 3502 PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA 114 13 3497 3502 scie scopus 000397607300077 2-s2.0-85016397741 Multidisciplinary Sciences Science & Technology - Other Topics Article EMBRYONIC STEM-CELLS MURINE C-MYC G-QUADRUPLEX TRANSGENIC MICE TUMOR MICROENVIRONMENT NEOPLASTIC PHENOTYPE LUNG-CANCER PROMOTER INHIBITION EXPRESSION MYC stauprimide NME2 nuclear localization cancer