Development of New Positron Emission Tomography Radiotracer for BET Imaging
The bromodomain and extraterminal domain (BET) inhibitors have been extensively studied for tumor treatment in the past few years. Recently, BET-containing proteins have been reported to play a key role in brain functions, such as learning and memory. BET proteins have also been shown to be a potential therapeutic target for substance abuse disorders. Development of a molecular probe for noninvasive imaging will elucidate the distribution and functional roles of BET in the living subject and accelerate medical research and drug discovery in this domain. Herein, we describe the synthesis and pilot imaging of a novel BET imaging agent, [ 11 C]MS417. Our imaging results demonstrate that this probe has moderate brain uptake, good specificity, good selectivity, and appropriate kinetics and distribution. [ 11 C]MS417 is an ideal lead compound for further optimization of clinical BET PET radiotracer tools and MS417 could be used as a blood-brain-barrier-penetrant compound for preclinical research. Graphic Abstract
- 원문이 없습니다.
NDSL에서는 해당 원문을 복사서비스하고 있습니다. 위의 원문복사신청 또는 장바구니 담기를 통하여 원문복사서비스 이용이 가능합니다.
- 이 논문과 함께 출판된 논문 + 더보기