Evaluation of [¹¹C]NMS-E973 as a PET tracer for in vivo visualisation of HSP90.

ABSTRACT: Heat shock protein 90 is an ATP-dependent molecular chaperone important for folding, maturation and clearance of aberrantly expressed proteins and is abundantly expressed (1-2% of all proteins) in the cytosol of all normal cells. In some tumour cells, however, strong expression of HSP90 is also observed on the cell membrane and in the extracellular matrix and the affinity of tumoural HSP90 for ATP domain inhibitors was reported to increase over 100-fold compared to that of HSP90 in normal cells. Here, we explore [¹¹C]NMS-E973 as a PET tracer for in vivo visualisation of HSP90 and as a potential tool for in vivo quantification of occupancy of HSP90 inhibitors. Methods: HSP90 expression was biochemically characterized in a panel of established cell lines inclu

SUBMITTER: Vermeulen K 

PROVIDER: S-EPMC6376183 | biostudies-literature | 2019

REPOSITORIES: biostudies-literature