A covalent chemical probe for Chikungunya nsP2 cysteine protease with antialphaviral activity and proteome-wide selectivity.

• Tác giả: Cheryl H Arrowsmith, Kesatebrhan Haile Asressu, Peter J Brown, Jane Burdick, Aurora Cabrera, Rafael M Couñago, Bennett J Davenport, Anirban Ghoshal, Mark T Heise, Laura E Herring, Mohammad Anwar Hossain, Stefanie Howell, Isabella Law, Sabian A Martinez, Eric M Merten, Nathaniel J Moorman, Noah L Morales, Angie L Mordant, Thomas E Morrison, Kenneth H Pearce, Sumera Perveen, John D Sears, Daniel N Streblow, Zachary J Streblow, Edwin G Tse, Thomas S Webb, Timothy M Willson
• Ngôn ngữ: eng
• Thông tin xuất bản: England : Scientific reports , 2025
• Bộ sưu tập: NCBI
• ID: 741320

Tóm tắt

Chikungunya is a mosquito-borne viral disease that causes fever and severe joint pain for which there is no direct acting drug treatments. Vinyl sulfone SGC-NSP2PRO-1 (3) was identified as a potent inhibitor of the nsP2 cysteine protease (nsP2pro) that reduced viral titer against infectious isolates of Chikungunya and other alphaviruses. The covalent warhead in 3 captured the active site C478 and inactivated nsP2pro with a k