941582-89-4Relevant academic research and scientific papers
Development of anti-coxsackievirus agents targeting 3C protease
Kim, Bo-Kyoung,Kim, Jeong-Hyun,Kim, Na-Ri,Lee, Won-Gil,Lee, So-Deok,Kim, Yong-Chul,Yun, Soo-Hyeon,Jeon, Eun-Seok
, p. 6952 - 6956,5 (2012)
Peptidomimetic anti-viral agents against Coxsackievirus B3 (CVB3) were developed using a strategy involving the inhibition of 3C protease (CVB3 3C pro), a target for CVB3-mediated myocarditis or pericarditis. In an attempt to improve the inhibi
Peptidomimetic ethyl propenoate covalent inhibitors of the enterovirus 71 3C protease: A P2-P4 study
Ang, Melgious J. Y.,Lau, Qiu Ying,Ng, Fui Mee,Then, Siew Wen,Poulsen, Anders,Cheong, Yuen Kuen,Ngoh, Zi Xian,Tan, Yong Wah,Peng, Jianhe,Keller, Thomas H.,Hill, Jeffrey,Chu, Justin J. H.,Brian Chia
, p. 332 - 339 (2016)
Enterovirus 71 (EV71) is a highly infectious pathogen primarily responsible for Hand, Foot, and Mouth Disease, particularly among children. Currently, no approved antiviral drug has been developed against this disease. The EV71 3C protease is deemed an attractive drug target due to its crucial role in viral polyprotein processing. Rupintrivir, a peptide-based inhibitor originally developed to target the human rhinovirus 3C protease, was found to inhibit the EV71 3C protease. In this communication, we report the inhibitory activities of 30 Rupintrivir analogs against the EV71 3C protease. The most potent inhibitor, containing a P2 ring-constrained phenylalanine analog (compound 9), was found to be two-fold more potent than Rupintrivir (IC50 value 3.4 ± 0.4 versus 7.3 ± 0.8 M). Our findings suggest that employing geometrically constrained residues in peptide-based protease inhibitors can potentially enhance their inhibitory activities.
