Evaluation of [¹⁸F]-ATRi as PET tracer for in vivo imaging of ATR in mouse models of brain cancer.

ABSTRACT:

Rationale

Ataxia telangiectasia and Rad3-related (ATR) threonine serine kinase is one of the key elements in orchestrating the DNA damage response (DDR). As such, inhibition of ATR can amplify the effects of chemo- and radiation-therapy, and several ATR inhibitors (ATRi) have already undergone clinical testing in cancer. For more accurate patient selection, monitoring and staging, real-time in vivo imaging of ATR could be invaluable; the development of appropriate imaging agents has remained a major challenge.

Methods

3-amino-N-(4-[¹⁸F]phenyl)-6-(4-(methylsulfonyl)phenyl)pyrazine-2-carboxamide ([¹⁸F]-ATRi), a close analogue of Ve-821, (a clinical ATRi candidate), was readily accomplished similarly to already established synthetic procedures. Structurall

SUBMITTER: Carlucci G 

PROVIDER: S-EPMC5524211 | biostudies-literature | 2017 May

REPOSITORIES: biostudies-literature