[¹⁸F]FE-OTS964: a Small Molecule Targeting TOPK for In Vivo PET Imaging in a Glioblastoma Xenograft Model.

ABSTRACT:

Purpose

Lymphokine-activated killer T cell-originated protein kinase (TOPK) is a fairly new cancer biomarker with great potential for clinical applications. The labeling of a TOPK inhibitor with F-18 can be exploited for positron emission tomography (PET) imaging allowing more accurate patient identification, stratification, and disease monitoring.

Procedures

[¹⁸F]FE-OTS964 was produced starting from OTS964, a preclinical drug which specifically binds to TOPK, and using a two-step procedure with [¹⁸F]fluoroethyl p-toluenesulfonate as a prosthetic group. Tumors were generated in NSG mice by subcutaneous injection of U87 glioblastoma cells. Animals were injected with [¹⁸F]FE-OTS964 and PET imaging and ex vivo biodistribution analysis was carrie

SUBMITTER: Pirovano G 

PROVIDER: S-EPMC6482100 | biostudies-literature | 2019 Aug

REPOSITORIES: biostudies-literature