Development of de-novo coronavirus 3-chymotrypsin-like protease (3CLpro) inhibitors since COVID-19 outbreak: A strategy to tackle challenges of persistent virus …

L Tian, T Qiang, X Yang, Y Gao, X Zhai, K Kang… - European Journal of …, 2023 - Elsevier
Although no longer a public health emergency of international concern, COVID-19 remains
a persistent and critical health concern. The development of effective antiviral drugs could …

SARS-CoV-2 resistance to monoclonal antibodies and small-molecule drugs

S Iketani, DD Ho - Cell Chemical Biology, 2024 - cell.com
Over four years have passed since the beginning of the COVID-19 pandemic. The scientific
response has been rapid and effective, with many therapeutic monoclonal antibodies and …

An orally bioavailable SARS-CoV-2 main protease inhibitor exhibits improved affinity and reduced sensitivity to mutations

M Westberg, Y Su, X Zou, P Huang, A Rustagi… - Science translational …, 2024 - science.org
Inhibitors of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main
protease (Mpro) such as nirmatrelvir (NTV) and ensitrelvir (ETV) have proven effective in …

Proof-of-concept studies with a computationally designed Mpro inhibitor as a synergistic combination regimen alternative to Paxlovid

C Papini, I Ullah, AP Ranjan, S Zhang… - Proceedings of the …, 2024 - National Acad Sciences
As the SARS-CoV-2 virus continues to spread and mutate, it remains important to focus not
only on preventing spread through vaccination but also on treating infection with direct …

[HTML][HTML] Resistance mechanisms of SARS-CoV-2 3CLpro to the non-covalent inhibitor WU-04

L Zhang, X Xie, H Luo, R Qian, Y Yang, H Yu, J Huang… - Cell Discovery, 2024 - nature.com
Drug resistance poses a significant challenge in the development of effective therapies
against SARS-CoV-2. Here, we identified two double mutations, M49K/M165V and …

Contributions of Hyperactive Mutations in Mpro from SARS-CoV-2 to Drug Resistance

JM Flynn, SN Zvornicanin, T Tsepal… - ACS Infectious …, 2024 - ACS Publications
The appearance and spread of mutations that cause drug resistance in rapidly evolving
diseases, including infections by the SARS-CoV-2 virus, are major concerns for human …

[HTML][HTML] Exploring the structural and molecular interaction landscape of nirmatrelvir and Mpro complex: The study might assist in designing more potent antivirals …

C Chakraborty, M Bhattacharya, A Alshammari… - Journal of Infection and …, 2023 - Elsevier
Background Several therapeutics have been developed and approved against SARS-CoV-2
occasionally; nirmatrelvir is one of them. The drug target of nirmatrelvir is Mpro, and …

Preparing for the next pandemic

BK Shoichet, CS Craik - Science, 2023 - science.org
Early in the COVID-19 pandemic, it was suggested that drugs to meaningfully treat the
disease would come from either the current antiviral armamentarium or from drug …

Dopamine and its precursor levodopa inactivate SARS-CoV-2 main protease by forming a quinoprotein

M Hao, Y He, T Song, H Guo, MP Rayman… - Free Radical Biology and …, 2024 - Elsevier
Many studies show either the absence, or very low levels of, SARS-CoV-2 viral RNA and/or
antigen in the brain of COVID-19 patients. Reports consistently indicate an abortive infection …

The biosafety level-2 macromolecular crystallography beamline (BL10U2) at the Shanghai Synchrotron Radiation Facility

Q Xu, HT Kong, K Liu, H Zhou, KH Zhang… - Nuclear Science and …, 2023 - Springer
BL10U2 is an undulator-based macromolecular crystallography (MX) beamline located at
the 3.5-GeV Shanghai Synchrotron Radiation Facility. BL10U2 is specifically designed for …