Therapeutic strategies for COVID-19: progress and lessons learned

G Li, R Hilgenfeld, R Whitley, E De Clercq - Nature Reviews Drug …, 2023 - nature.com
Abstract The coronavirus disease 2019 (COVID-19) pandemic has stimulated tremendous
efforts to develop therapeutic strategies that target severe acute respiratory syndrome …

Small-molecule discovery through DNA-encoded libraries

AA Peterson, DR Liu - Nature Reviews Drug Discovery, 2023 - nature.com
The development of bioactive small molecules as probes or drug candidates requires
discovery platforms that enable access to chemical diversity and can quickly reveal new …

Transmissible SARS-CoV-2 variants with resistance to clinical protease inhibitors

SA Moghadasi, E Heilmann, AM Khalil, C Nnabuife… - Science …, 2023 - science.org
Vaccines and drugs have helped reduce disease severity and blunt the spread of severe
acute respiratory syndrome coronavirus 2 (SARS-CoV-2). However, ongoing virus …

Structure and function of SARS-CoV and SARS-CoV-2 main proteases and their inhibition: A comprehensive review

X Li, Y Song - European journal of medicinal chemistry, 2023 - Elsevier
Severe acute respiratory syndrome-associated coronavirus (SARS-CoV) identified in 2003
infected∼ 8000 people in 26 countries with 800 deaths, which was soon contained and …

Alkyne derivatives of SARS-CoV-2 main protease inhibitors including nirmatrelvir inhibit by reacting covalently with the nucleophilic cysteine

L Brewitz, L Dumjahn, Y Zhao, CD Owen… - Journal of Medicinal …, 2023 - ACS Publications
Nirmatrelvir (PF-07321332) is a nitrile-bearing small-molecule inhibitor that, in combination
with ritonavir, is used to treat infections by severe acute respiratory syndrome coronavirus-2 …

Reversible male contraception by targeted inhibition of serine/threonine kinase 33

AF Ku, KL Sharma, HM Ta, CM Sutton, KM Bohren… - Science, 2024 - science.org
Men or mice with homozygous serine/threonine kinase 33 (STK33) mutations are sterile
owing to defective sperm morphology and motility. To chemically evaluate STK33 for male …

Highly pure DNA-encoded chemical libraries by dual-linker solid-phase synthesis

M Keller, D Petrov, A Gloger, B Dietschi, K Jobin… - Science, 2024 - science.org
The first drugs discovered using DNA-encoded chemical library (DEL) screens have entered
late-stage clinical development. However, DEL technology as a whole still suffers from poor …

Non-covalent SARS-CoV-2 Mpro inhibitors developed from in silico screen hits

GG Rossetti, MA Ossorio, S Rempel, A Kratzel… - Scientific reports, 2022 - nature.com
Mpro, the main protease of the severe acute respiratory syndrome coronavirus 2 (SARS-
CoV-2), is essential for the viral life cycle. Accordingly, several groups have performed in …

Structural biology of SARS-CoV-2 Mpro and drug discovery

Y Duan, H Wang, Z Yuan, H Yang - Current Opinion in Structural Biology, 2023 - Elsevier
Since its outbreak in late 2019, the COVID-19 pandemic has drawn enormous attention
worldwide as a consequence of being the most disastrous infectious disease in the past …

[HTML][HTML] Medicinal chemistry strategies towards the development of non-covalent SARS-CoV-2 Mpro inhibitors

L Song, S Gao, B Ye, M Yang, Y Cheng, D Kang… - … Pharmaceutica Sinica B, 2024 - Elsevier
The main protease (M pro) of SARS-CoV-2 is an attractive target in anti-COVID-19 therapy
for its high conservation and major role in the virus life cycle. The covalent M pro inhibitor …