Publications by authors named "Andriana O Jouk"

Article Synopsis
  • SMARCA2 (BRM) is a key ATPase and member of the SWI/SNF chromatin-remodeling complex, which plays a crucial role in regulating gene expression alongside its relative, BRG1 (SMARCA4).
  • Current research highlights the lack of small molecules that can specifically inhibit the ATPase activity of SWI/SNF, despite the relevance in cancer, particularly in BRG1-deficient cases.
  • New allosteric dual inhibitors targeting both BRM and BRG1 have been developed, showing potential to reduce BRM-dependent gene expression and demonstrate anti-cancer effects in a BRG1-mutant lung tumor model, providing insights into SWI/SNF functions in various health contexts.
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PTP1B is a master regulator in the insulin and leptin metabolic pathways. Hyper-activated PTP1B results in insulin resistance and is viewed as a key factor in the onset of type II diabetes and obesity. Moreover, inhibition of PTP1B expression in cancer cells dramatically inhibits cell growth in vitro and in vivo.

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The STAT3 gene is abnormally active in glioblastoma (GBM) and is a critically important mediator of tumor growth and therapeutic resistance in GBM. Thus, for poorly treated brain cancers such as gliomas, astrocytomas, and glioblastomas, which harbor constitutively activated STAT3, a STAT3-targeting therapeutic will be of significant importance. Herein, we report a most potent, small molecule, nonphosphorylated STAT3 inhibitor, 31 (SH-4-54) that strongly binds to STAT3 protein (K D = 300 nM).

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