Evaluation of TK1 targeting carboranyl thymidine analogs as potential delivery agents for neutron capture therapy of brain tumors.
Appl Radiat Isot
; 106: 251-5, 2015 Dec.
Article
in En
| MEDLINE
| ID: mdl-26282567
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).
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Thymidine
/
Thymidine Kinase
/
Brain Neoplasms
/
Boron Neutron Capture Therapy
Limits:
Animals
Language:
En
Journal:
Appl Radiat Isot
Year:
2015
Document type:
Article