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).
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Authors | Rolf F Barth, Weilian Yang, Robin J Nakkula, Youngjoo Byun, Werner Tjarks, Lai Chu Wu, Peter J Binns, Kent J Riley |
Journal | Applied 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 |
PMID | 26282567
(Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov't, Validation Study)
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Copyright | Copyright © 2015 Elsevier Ltd. All rights reserved. |
Chemical References |
- Thymidine Kinase
- thymidine kinase 1
- Thymidine
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Topics |
- Animals
- Boron Neutron Capture Therapy
- Brain Neoplasms
(radiotherapy)
- Rats
- Thymidine
(administration & dosage, analogs & derivatives)
- Thymidine Kinase
(drug effects)
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