Structure-Based Discovery and Development of a Series of Potent and Selective Bromodomain and Extra-Terminal Protein Inhibitors

Keyphrases

• Proteinase Inhibitor 100%
• Bromodomain 100%
• Terminal Protein 100%
• In Vivo Antitumor Activity 33%
• Xenograft Model 33%
• Antitumor Effect 33%
• High Potency 33%
• Cancer Treatment 33%
• Linker 33%
• HERG 33%
• Drug Target 33%
• Cellular Mechanisms 33%
• Drug Candidates 33%
• Antitumor Efficacy 33%
• Mechanism Study 33%
• Pharmacokinetic Profile 33%
• Oral Administration 33%
• MM.1S 33%
• Lead Optimization 33%
• Promising Drug 33%
• Bromodomain-containing Protein 4 (BRD4) 33%
• Novel Inhibitors 33%
• Protein Drug 33%
• Co-crystal Structure 33%
• Brain Penetration 33%
• Five-membered Rings 33%
• Anticancer Treatment 33%
• Activity Stability 33%
• Growth Effect 33%
• Quinoxalin-2(1H)-ones 33%
• Antitumor Growth 33%
• Hit Compound 33%
• 1,2,4-Triazol 33%

Pharmacology, Toxicology and Pharmaceutical Science

• Malignant Neoplasm 100%
• Preclinical Study 100%
• Lead Compound 100%
• Bromodomain Inhibitor 100%
• Pharmacokinetics 100%
• Oral Administration 100%

Biochemistry, Genetics and Molecular Biology

• Bromodomain 100%
• Anticancer 33%
• Preclinical Study 33%
• Pharmacokinetics 33%
• BRD4 33%