Imaging Cellular Distribution of Bcl Inhibitors Using Small Molecule Drug Conjugates
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CitationGiedt, Randy J., Melissa M. Sprachman, Katherine S. Yang, and Ralph Weissleder. 2014. “Imaging Cellular Distribution of Bcl Inhibitors Using Small Molecule Drug Conjugates.” Bioconjugate Chemistry 25 (11): 2081-2085. doi:10.1021/bc500433k. http://dx.doi.org/10.1021/bc500433k.
AbstractOverexpression of anti-apoptotic proteins such as Bcl-2 is a cellular mechanism to evade apoptosis; consequently, Bcl-2 inhibitors are being developed as anticancer agents. In this work, we have synthesized a fluorescent version of ABT-199 in an effort to visualize a drug surrogate by high resolution imaging. We show that this fluorescent conjugate has comparable Bcl-2 binding efficacy and cell line potency to the parent compound and can be used as an imaging agent in several cancer cell types. We anticipate that this agent will be a valuable tool for studying the single-cell distribution and pharmacokinetics of ABT-199 as well the broader group of BH3-mimetics.
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