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Evaluation of TK1 targeting carboranyl thymidine analogs as potential delivery agents for neutron capture therapy of brain tumors.

Abstract
In this report we describe studies with N5-2OH, a carboranyl thymidine analog (CTA), which is a substrate for thymidine kinase 1 (TK1), using the F98 rat glioma model. In vivo BNCT studies have demonstrated that intracerebral (i.c.) osmotic pump infusion of N5-2OH yielded survival data equivalent to those obtained with i.v. administration of boronophenylalanine (BPA). The combination of N5-2OH and BPA resulted in a modest increase in MST of F98 glioma bearing rats compared to a statistically significant increase with the RG2 glioma model, as has been previously reported by us (Barth et al., 2008). This had lead us to synthesize a second generation of CTAs that have improved in vitro enzyme kinetics and in vivo tumor uptake (Agarwal et al., 2015).
AuthorsRolf F Barth, Weilian Yang, Robin J Nakkula, Youngjoo Byun, Werner Tjarks, Lai Chu Wu, Peter J Binns, Kent J Riley
JournalApplied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine (Appl Radiat Isot) Vol. 106 Pg. 251-5 (Dec 2015) ISSN: 1872-9800 [Electronic] England
PMID26282567 (Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov't, Validation Study)
CopyrightCopyright © 2015 Elsevier Ltd. All rights reserved.
Chemical References
  • Thymidine Kinase
  • thymidine kinase 1
  • Thymidine
Topics
  • Animals
  • Boron Neutron Capture Therapy
  • Brain Neoplasms (radiotherapy)
  • Rats
  • Thymidine (administration & dosage, analogs & derivatives)
  • Thymidine Kinase (drug effects)

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