1021685-18-6Relevant academic research and scientific papers
Fluorescent epigenetic small molecule induces expression of the tumor suppressor ras-association domain family 1A and inhibits human prostate xenograft
Sheikh, Kathryn D.,Banerjee, Partha P.,Jagadeesh, Shankar,Grindrod, Scott C.,Zhang, Li,Paige, Mikell,Brown, Milton L.
, p. 2376 - 2382 (2010)
Epigenetic silencing of Ras-association domain family 1A (RASSF1A) protein in cancer cells results in a disruption of cell cycle control, genetic instability, enhanced cell motility, and apoptotic resistance. Ectopic expression of RASSF1A reverses this tumorigenic phenotype. Thus, small molecules with the ability to restore RASSF1A expression may represent a new class of therapeutic agents. Recently, we designed and synthesized a fluorescent carbazole analogue of mahanine (alkaloid from Murraya koenigii) that restored RASSF1A mRNA expression. Our fluorescent lead compound up-regulated RASSF1A in vitro, potently inhibited human prostate cancer cell proliferation, and fluoresced at a visible wavelength, allowing for the observation of intracellular distribution. The small molecule lead was not acutely toxic up to 550 mg/kg, and dosing at 10 mg/kg reduced human xenograft tumor volume by about 40%.
FLUORESCENT REGULATORS OF RASSF1A EXPRESSION AND HUMAN CANCER CELL PROLIFERATION
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Page/Page column 32-33, (2010/04/03)
The invention provides methods for the treatment of cancer in a subject comprising administering a dansyl-carbazole compound.
CANCER THERAPY
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Page/Page column 29, (2008/12/05)
The present invention relates to methods of inducing expression of an epigenetically silenced gene, RASSFlA, in cells, particularly human cells, such as cancer cells. It also relates to methods of treating an individual, prophylactically or therapeutically, for cancer in which RASSFlA is epigenetically silenced.
