The Development and Evaluation of a Novel Highly Selective PET Radiotracer for Targeting BET BD1.

ABSTRACT: Background/Objectives: Small molecules that interfere with the interaction between acetylated protein tails and the tandem bromodomains of BET (bromodomain and extra-terminal) family proteins are pivotal in modulating immune/inflammatory and neoplastic diseases. This study aimed to develop a novel PET imaging tracer, [¹¹C]GSK023, that targets the N-terminal bromodomain (BD1) of BET family proteins with high selectivity and potency, thereby enriching the chemical probe toolbox for epigenetic imaging. Methods: [¹¹C]GSK023, a radio-chemical probe, was designed and synthesized to specifically target the BET BD1. In vivo PET imaging evaluations were conducted on rodents, focusing on the tracer's distribution and binding specificity in various tissues. Blockin

SUBMITTER: Wang Y 

PROVIDER: S-EPMC11509907 | biostudies-literature | 2024 Sep

REPOSITORIES: biostudies-literature