A positron emission tomography imaging probe selectively targeting the BD1 bromodomain and extra-terminal domain

• Published in: Chemical communications (Cambridge, England) Vol. 58; no. 69; pp. 9654 - 9657
• Main Authors: Bai, Ping, Yan, Liu, Bagdasarian, Frederick A, Wilks, Moses Q, Wey, Hsiao-Ying, Wang, Changning
• Format: Journal Article
• Language: English
• Published: CAMBRIDGE Royal Soc Chemistry 25.08.2022; Royal Society of Chemistry
• Subjects: Animals; Binding; Brain; Cell Cycle Proteins; Chemistry; Chemistry, Multidisciplinary; Emission analysis; Medical imaging; Mice; Neurological diseases; Nuclear Proteins - metabolism; Physical Sciences; Positron emission; Positron-Emission Tomography; Protein Domains; Radiochemistry; Science & Technology; Selectivity; Tomography; Transcription Factors - chemistry; DISCOVERY

The two tandem bromodomains of BET (bromodomain and extra-terminal domain) proteins (BD1 and BD2) may play distinct and critical roles in neurological diseases. To better understand the underlying mechanisms of the BD1 bromodomain and facilitate brain permeable domain-selective inhibitor development...