Publications by authors named "Iva Monique T Gramatikov"

Article Synopsis
  • BFL1, an antiapoptotic protein from the BCL2 family, is linked to hematological cancers but hasn't been extensively researched.
  • Two articles present the development of selective BFL1 inhibitors, starting from hit identification using a covalent fragment library and leading to optimized compounds.
  • One compound not only induced cell death in specific cancer cell lines but also stabilized the BFL1 protein, significantly increasing its half-life to 10.8 hours while activating cellular apoptosis markers.
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A challenge for screening new anticancer drugs is that efficacy in cell culture models is not always predictive of efficacy in patients. One limitation of standard cell culture is a reliance on non-physiological nutrient levels, which can influence cell metabolism and drug sensitivity. A general assessment of how physiological nutrients affect cancer cell response to small molecule therapies is lacking.

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Background: Genetically engineered mouse models (GEMMs) of cancer are powerful tools to study mechanisms of disease progression and therapy response, yet little is known about how these models respond to multimodality therapy used in patients. Radiation therapy (RT) is frequently used to treat localized cancers with curative intent, delay progression of oligometastases, and palliate symptoms of metastatic disease.

Methods: Here we report the development, testing, and validation of a platform to immobilize and target tumors in mice with stereotactic ablative RT (SART).

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A challenge for screening new candidate drugs to treat cancer is that efficacy in cell culture models is not always predictive of efficacy in patients. One limitation of standard cell culture is a reliance on non-physiological nutrient levels to propagate cells. Which nutrients are available can influence how cancer cells use metabolism to proliferate and impact sensitivity to some drugs, but a general assessment of how physiological nutrients affect cancer cell response to small molecule therapies is lacking.

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