In the cover paper of this week's issue of Oncotarget (Volume 12, Issue 9), titled, "Creation of a new class of radiosensitizers for glioblastoma based on the mibefradil pharmacophore," researchers conducted a study to create mibefradil analogs as superior radiosensitizers for glioblastomas.
In the current study, based on their previous findings, the researchers from Yale University used structure activity relationship analysis and EJ-DR assays to create, synthesize, and profile a series of 140 mibefradil analogs. Their goal was to develop superior mibefradil analogues, with reduced off-target effects and improved potency.
After successfully reducing the known off-target liabilities of mibefradil, the team selected the top 12 analogues for further in vitro and in vivo pharmacokinetic studies. These analogs were tested in vivo to verify that they cross the blood-brain barrier and accumulate in mouse brain tissue.
“We then tested the pharmacokinetic parameters of the synthesized analogues and validated their ability to cross the blood-brain barrier (BBB) and accumulate in mouse brain tissue, at levels similar to that observed with mibefradil.”
DOI - https://doi.org/10.18632/oncotarget.27933
Full text - https://www.oncotarget.com/article/27933/text/
Correspondence to - Yulia V. Surovtseva - yulia.surovtseva@yale.edu and Ranjit S. Bindra - ranjit.bindra@yale.edu
Keywords - glioblastoma, radiosensitizers, mibefradil, DNA repair, alternative non-homologous end joining
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