Design of the New -Dodecarborate-Containing Gemcitabine Analogue for the Albumin-Based Theranostics Composition.
Clicks: 107
ID: 276839
2023
Article Quality & Performance Metrics
Overall Quality
Improving Quality
0.0
/100
Combines engagement data with AI-assessed academic quality
Reader Engagement
Emerging Content
30.0
/100
106 views
19 readers
Trending
AI Quality Assessment
Not analyzed
Abstract
Combination therapy is becoming an increasingly important treatment strategy because multi-drugs can maximize therapeutic effect and overcome potential mechanisms of drug resistance. A new albumin-based theranostic containing gemcitabine -dodecaborate analogue has been developed for combining boron neutron capture therapy (BNCT) and chemotheraphy. An exo-heterocyclic amino group of gemcitabine was used to introduce dodecaborate, and a 5'-hydroxy group was used to tether maleimide moiety through an acid-labile phosphamide linker. The -trifluoroacylated homocysteine thiolactone was used to attach the gemcitabine analogue to human serum albumin (HSA) bearing Cy5 or Cy7 fluorescent dyes. The half-maximal inhibitory concentration (IC) of the designed theranostic relative to T98G cells was 0.47 mM with the correlation coefficient R = 0.82. BNCT experiments resulted in a decrease in the viability of T98G cells, and the survival fraction was ≈ 0.4.
| Reference Key |
raskolupova2023designmolecules
Use this key to autocite in the manuscript while using
SciMatic Manuscript Manager or Thesis Manager
|
|---|---|
| Authors | Raskolupova, Valeria I;Wang, Meiling;Dymova, Maya A;Petrov, Gleb O;Shchudlo, Ivan M;Taskaev, Sergey Yu;Abramova, Tatyana V;Godovikova, Tatyana S;Silnikov, Vladimir N;Popova, Tatyana V; |
| Journal | molecules |
| Year | 2023 |
| DOI |
2672
|
| URL | |
| Keywords |
Citations
No citations found. To add a citation, contact the admin at info@scimatic.org
Comments
No comments yet. Be the first to comment on this article.