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This research aims to assess the selectivity and efficacy of inhibitors targeting BCL-2 family protein interactions involved in apoptosis regulation.

April 20, 2022Science AdvancesOpen Access

Efficacy and specificity of inhibitors of BCL-2 family protein interactions assessed by affinity measurements in live cells

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This research aims to assess the selectivity and efficacy of inhibitors targeting BCL-2 family protein interactions involved in apoptosis regulation.
Utilized quantitative fast fluorescence lifetime imaging microscopy to measure drug effects on binding affinities of interacting protein pairs in live cells.
Assessed 15 inhibitors of four antiapoptotic proteins against six BH3 protein ligands for specificity and efficacy.
Many inhibitors effectively target the designed BCL-2 interactions; however, most exhibit unexpected selectivity.
Most inhibitors showed poor efficacy in live cell environments.

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Randomized trial evaluates efficacy and specificity of BCL-2 family protein inhibitors, suggesting complex interactions in cancer treatment.

Osterlund et al. (2022) studied this question.

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Randomized trial evaluates efficacy and specificity of BCL-2 family protein inhibitors, suggesting complex interactions in cancer treatment.