Imaging Cellular Distribution of Bcl Inhibitors Using Small Molecule Drug Conjugates

DSpace/Manakin Repository

Imaging Cellular Distribution of Bcl Inhibitors Using Small Molecule Drug Conjugates

Citable link to this page

 

 
Title: Imaging Cellular Distribution of Bcl Inhibitors Using Small Molecule Drug Conjugates
Author: Giedt, Randy J.; Sprachman, Melissa M.; Yang, Katherine S.; Weissleder, Ralph

Note: Order does not necessarily reflect citation order of authors.

Citation: Giedt, 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.
Full Text & Related Files:
Abstract: Overexpression 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.
Published Version: doi:10.1021/bc500433k
Other Sources: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4240345/pdf/
Terms of Use: This article is made available under the terms and conditions applicable to Other Posted Material, as set forth at http://nrs.harvard.edu/urn-3:HUL.InstRepos:dash.current.terms-of-use#LAA
Citable link to this page: http://nrs.harvard.edu/urn-3:HUL.InstRepos:23474046
Downloads of this work:

Show full Dublin Core record

This item appears in the following Collection(s)

 
 

Search DASH


Advanced Search
 
 

Submitters