Discovery of a novel mycobacterial F-ATP synthase inhibitor and its potency in combination with diarylquinolines

• Main Authors: Hotra, Adam, Ragunathan, Priya, Ng, Pearly Shuyi, Seankongsuk, Pattarakiat, Harikishore, Amaravadhi, Sarathy, Jickky Palmae, Saw, Wuan-Geok, Lakshmanan, Umayal, Sae-Lao, Patcharaporn, Kalia, Nitin Pal, Shin, Joon, Kalyanasundaram, Revathy, Anbarasu, Sivaraj, Parthasarathy, Krupakar, Pradeep, Chaudhari Namrata, Makhija, Harshyaa, Dröge, Peter, Poulsen, Anders, Tan, Jocelyn Hui Ling, Pethe, Kevin, Dick, Thomas, Bates, Roderick Wayland, Grüber, Gerhard
• Other Authors: School of Biological Sciences
• Format: Article
• Language: English
• Published: 2021
• Subjects: Science::Biological sciences::Biochemistry; ATP Synthesis; Drug Discovery
• Online Access: https://hdl.handle.net/10356/149233
• Institution: Nanyang Technological University

The F1 FO -ATP synthase is required for growth and viability of Mycobacterium tuberculosis and is a validated clinical target. A mycobacterium-specific loop of the enzyme's rotary γ subunit plays a role in the coupling of ATP synthesis within the enzyme complex. We report the discovery of a nov...