Addressing the Biochemical Foundations of a Glucose-Based "Trojan Horse"-Strategy to Boron Neutron Capture Therapy : From Chemical Synthesis to In Vitro Assessment

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Matovic , J , Järvinen , J , Bland , H C , Sokka , I K , Imlimthan , S , Ferrando , R M , Huttunen , K M , Timonen , J , Peräniemi , S , Aitio , O , Airaksinen , A J , Sarparanta , M , Johansson , M P , Rautio , J & Ekholm , F S 2020 , ' Addressing the Biochemical Foundations of a Glucose-Based "Trojan Horse"-Strategy to Boron Neutron Capture Therapy : From Chemical Synthesis to In Vitro Assessment ' , Molecular Pharmaceutics , vol. 17 , no. 10 , pp. 3885-3899 . https://doi.org/10.1021/acs.molpharmaceut.0c00630

Title: Addressing the Biochemical Foundations of a Glucose-Based "Trojan Horse"-Strategy to Boron Neutron Capture Therapy : From Chemical Synthesis to In Vitro Assessment
Author: Matovic, Jelena; Järvinen, Juulia; Bland, Helena C.; Sokka, Iris K.; Imlimthan, Surachet; Ferrando, Ruth Mateu; Huttunen, Kristiina M.; Timonen, Juri; Peräniemi, Sirpa; Aitio, Olli; Airaksinen, Anu J.; Sarparanta, Mirkka; Johansson, Mikael P.; Rautio, Jarkko; Ekholm, Filip S.
Contributor: University of Helsinki, Department of Chemistry
University of Helsinki, Department of Chemistry
University of Helsinki, Department of Chemistry
University of Helsinki, Department of Chemistry
University of Helsinki, Department of Chemistry
University of Helsinki, Department of Chemistry
University of Helsinki, Department of Chemistry
University of Helsinki, Department of Chemistry
Date: 2020-10-05
Language: eng
Number of pages: 15
Belongs to series: Molecular Pharmaceutics
ISSN: 1543-8384
URI: http://hdl.handle.net/10138/321501
Abstract: Boron neutron capture therapy (BNCT) for cancer is on the rise worldwide due to recent developments of in-hospital neutron accelerators which are expected to revolutionize patient treatments. There is an urgent need for improved boron delivery agents, and herein we have focused on studying the biochemical foundations upon which a successful GLUT1-targeting strategy to BNCT could be based. By combining synthesis and molecular modeling with affinity and cytotoxicity studies, we unravel the mechanisms behind the considerable potential of appropriately designed glucoconjugates as boron delivery agents for BNCT. In addition to addressing the biochemical premises of the approach in detail, we report on a hit glucoconjugate which displays good cytocompatibility, aqueous solubility, high transporter affinity, and, crucially, an exceptional boron delivery capacity in the in vitro assessment thereby pointing toward the significant potential embedded in this approach.
Subject: boron neutron capture therapy
cancer therapeutics
carbohydrates
glucose transporters
medicinal chemistry
drug delivery
SQUAMOUS-CELL CARCINOMA
NECK-CANCER
CRYSTAL-STRUCTURE
RECURRENT HEAD
FORCE-FIELD
BASIS-SETS
TRANSPORTERS
DERIVATIVES
CONFORMATION
RECOGNITION
116 Chemical sciences
317 Pharmacy
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