Safety, Tolerability, and Pharmacokinetics of the Novel Antiviral Agent Ensitrelvir Fumaric Acid, a SARS-CoV-2 3CL Protease Inhibitor, in Healthy AdultsArticle Published on 2022-10-182022-11-15 Journal: Antimicrobial Agents and Chemotherapy [Category] COVID19(2023년), SARS, 치료제, [키워드] 3CL acid administration adverse event affected agent Antiviral assessment AUC C max COVID-19 demonstrated dose doses drug-drug interaction Effect ensitrelvir first-in-human Food Intake geometric increase in Infection inhibitor Japanese mild in severity MOST novel oral dosing P450 participant Participants participants with SARS-CoV-2 pharmacokinetics phase 1 study Placebo plasma proportionality protease Protease inhibitor Randomized reduced resolved Safety SARS-CoV-2 selective single dose substrate T max Tolerability Treatment viral replication [DOI] 10.1128/aac.00632-22 PMC 바로가기
Functional map of SARS-CoV-2 3CL protease reveals tolerant and immutable sitesArticle Published on 2022-10-122022-11-15 Journal: Cell Host & Microbe [Category] COVID19(2023년), SARS, 변종, 진단, 치료제, [키워드] 3CL 3CL pro 3CL Protease approach biological property clinically conserved Coronaviruses COVID-19 deep mutational scanning develop drug resistance functional identify inhibitor inhibitors Mutation Nirmatrelvir protease protease inhibitors Protein residue reveal SARS-CoV-2 single mutant subset target therapeutic target Tolerance virus viruses [DOI] 10.1016/j.chom.2022.08.003 PMC 바로가기
Identification of Drug Combination Therapies for SARS-CoV-2: A Molecular Dynamics Simulations ApproachArticle Published on 2022-09-092022-11-15 Journal: Drug design, development and therapy [Category] SARS, 신약개발, 치료제, [키워드] 3CL antiviral activity Antiviral treatment approved approved drug binding binding site carried caused Compound compounds conformational change coronavirus COVID-19 drug drug combination drug combinations Drug repurposing drug synergy Dynamics effective Efficacy enzyme Favipiravir identification in silico in vitro in vitro assays Infectious disease inhibitor inhibitory effect Ligand ligand docking M pro molecular Molecular dynamics simulation molecular dynamics simulations multiple binding sites. pandemic predicted protease Protein target Proteins provide reduced SARS-CoV-2 SARS-CoV-2 viral screened Simulation suggested synergism synergistic Toxicity Treatment treatments for COVID-19 virus [DOI] 10.2147/DDDT.S366423 PMC 바로가기
Allosteric inhibitors of the main protease of SARS-CoV-2SARS-CoV-2의 주요 프로테아제의 알로스테릭 억제제Article Published on 2022-09-012022-09-11 Journal: Antiviral Research [Category] COVID19(2023년), SARS, 치료제, [키워드] 3CL 3CLpro affinity binding alarm Allosteric inhibitor Antiviral approval approved boceprevir characterized Compound derivative digestion docking drug effective therapy Emergency use enzymatic assay enzyme expressed FDA inhibit inhibitor library mechanism mechanism of action molecular molecular docking molecular dynamics niclosamide protease provide purified raised Remdesivir reported SARS-CoV-2 screened suggested the SARS-CoV-2 Vaccine virus virus growth [DOI] 10.1016/j.antiviral.2022.105381 PMC 바로가기 [Article Type] Article
The structure-based design of peptidomimetic inhibitors against SARS-CoV-2 3C like protease as Potent anti-viral drug candidate강력한 항바이러스 약물 후보로서 SARS-CoV-2 3C 유사 프로테아제에 대한 펩티도미메틱 억제제의 구조 기반 설계Article Published on 2022-08-052022-09-11 Journal: European journal of medicinal chemistry [Category] COVID19(2023년), SARS, 치료제, [키워드] 3C Like protease 3CL 3CL pro acute respiratory syndrome coronavirus acute respiratory syndrome coronavirus 2 anti-SARS-CoV-2 Anti-viral anti-viral drug applied complexes Compound coronavirus 2 coronavirus disease Coronavirus disease 2019 COVID-19 deficiency described develop drug candidates effective inhibit inhibitor inhibitors inhibitory activity Like Medicine pathogen Peptidomimetic inhibitors potent Prevent Pro protease Protease inhibitor protein-ligand respiratory SARS-CoV-2 screened Severe acute respiratory syndrome severe acute respiratory syndrome Coronavirus structure-based design targeting the SARS-CoV-2 Transcription treat viral replication X-ray [DOI] 10.1016/j.ejmech.2022.114458 PMC 바로가기 [Article Type] Article
Comprehensive Nonclinical Safety Assessment of Nirmatrelvir Supporting Timely Development of the SARS-COV-2 Antiviral Therapeutic, Paxlovid™SARS-COV-2 항바이러스 치료제 Paxlovid™의 적시 개발을 지원하는 Nirmatrelvir의 포괄적인 비임상 안전성 평가Article Published on 2022-08-012022-09-11 Journal: International journal of toxicology [Category] 치료제, [키워드] 3CL administration Antiviral Arrhythmias assessment blood pressure cardiovascular caused clinical development Clinical pathology coagulation time Comprehensive conducted COVID-19 COVID-19 patient COVID-19 patients death decrease decreases development dose Drug safety Effect Efficacy Endpoint enhancer enzyme functional heart rate high risk highest dose Hospitalization Increases increases in induce Infection locomotor male MPro nervous system Nirmatrelvir not affect pathology Paxlovid pharmacokinetic Potential produced profile protease RATs Replication respiratory rate Ritonavir Safety safety pharmacology SARS-CoV-2 SARS-CoV-2 virus Support Supporting target tested the SARS-CoV-2 virus toxicities Toxicity toxicology transaminase transaminases Treatment treatment of COVID-19 were assessed [DOI] 10.1177/10915818221095489 PMC 바로가기 [Article Type] Article
In Silico Studies on Zinc Oxide Based Nanostructured Oil Carriers with Seed Extracts of Nigella sativa and Pimpinella anisum as Potential Inhibitors of 3CL Protease of SARS-CoV-2SARS-CoV-2의 3CL 프로테아제의 잠재적 억제제로서 Nigella sativa 및 Pimpinella anisum의 종자 추출물을 포함하는 산화아연 기반 나노구조 오일 운반체에 대한 실리코 연구Article Published on 2022-07-042022-09-11 Journal: Molecules [Category] COVID19(2023년), SARS, 변종, [키워드] 3CL 3CLpro acute respiratory syndrome acute respiratory syndrome coronavirus acute respiratory syndrome coronavirus 2 addition applicability candidate carrier characterized clinical trials Compound compounds conformational change coronavirus coronavirus disease Coronavirus disease 2019 COVID-19 docking explained Extract Health histogram imperative inhibitor investigated Ligand ligands MD simulation mixture molecular molecular docking molecular docking studies molecular dynamic simulation molecular dynamics Molecular dynamics simulation MPro nanostructure Nigella Nigella Sativa Oil oleuropein Oxide pandemic Pimpenella anisum Potential protease Protein Research RMSD RMSF SARS-CoV-2 SARS-CoV-2 main protease seed selected stability structural proteins the SARS-CoV-2 trajectory Vaccines variant Zinc zinc oxide zinc oxide nanoparticles [DOI] 10.3390/molecules27134301 PMC 바로가기 [Article Type] Article
The Extracts of Polygonum cuspidatum Root and Rhizome Block the Entry of SARS-CoV-2 Wild-Type and Omicron Pseudotyped Viruses via Inhibition of the S-Protein and 3CL ProteasePolygonum cuspidatum 뿌리 및 뿌리 줄기 추출물은 S-단백질 및 3CL 프로테아제의 억제를 통해 SARS-CoV-2 야생형 및 오미크론 의사형 바이러스의 진입을 차단합니다Article Published on 2022-06-132022-09-11 Journal: Molecules [Category] COVID19(2023년), SARS, 변종, 치료제, [키워드] 3CL ACE2 angiotensin Angiotensin-converting enzyme Anti-viral block blocked caused Chinese Compound contagious COVID-19 develop disease effective Efficacy Ethanol Extract fibroblast fibroblasts gallic acid herbal medicine Infection inhibit inhibition Interaction omicron Omicron variant pandemic pharmacological treatment phytochemical Polygoni Cuspidati Rhizoma et Radix Polygonum Protease activity Pseudotyped virus pseudovirus pseudovirus entry Radix receptor responsible resulting rhizome root S-protein SARS-CoV-2 SARS-CoV-2 pseudotyped virus SARS-CoV-2 virus shown Spike protein tested the SARS-CoV-2 the SARS-CoV-2 virus the spike protein Traditional Chinese medicine Treatment Vaccines water wild-type zebrafish zebrafish larvae. [DOI] 10.3390/molecules27123806 PMC 바로가기 [Article Type] Article
A Study of Drug Repurposing to Identify SARS-CoV-2 Main Protease (3CLpro) InhibitorsSARS-CoV-2 주요 프로테아제(3CLpro) 억제제 식별을 위한 약물 용도 변경 연구Article Published on 2022-06-092022-09-11 Journal: International Journal of Molecular Sciences [Category] Coronavirus, COVID19(2023년), SARS, 신약개발, 치료제, [키워드] 3CL 3CLpro acute respiratory syndrome acute respiratory syndrome coronavirus acute respiratory syndrome coronavirus 2 Administered Antiviral antiviral activity artificial artificial intelligence caused Cell Combination Compound compounds coronavirus coronavirus disease Coronavirus disease 2019 COVID-19 cynarine cytotoxicity docking drug Drug repurposing eravacycline FRET in silico in vitro infected with SARS-CoV-2 inhibitory activity inhibitory compounds intelligence MPro outbreak phase prexasertib protease repurposing safety profile SARS-CoV-2 SARS-CoV-2 3CL protease SARS-CoV-2 main protease selected severe acute respiratory syndrome Coronavirus tested the disease Treatment trials Vaccine VeroE6 cell VeroE6 cells were used [DOI] 10.3390/ijms23126468 PMC 바로가기 [Article Type] Article
[Nirmatrelvir plus ritonavir (Paxlovid) a potent SARS-CoV-2 3CLpro protease inhibitor combination][니르마트렐비르와 리토나비르(팍슬로비드)의 강력한 SARS-CoV-2 3CLpro 프로테아제 억제제 조합]Review Published on 2022-06-012022-09-11 Journal: Revista española de quimioterapia : publicación [Category] COVID19(2023년), SARS, 변종, 치료제, [키워드] 3CL 3CLpro Administered adverse effects Antiviral antiviral drug antiviral drugs antiviral efficacy approved average conserved coronavirus Coronaviruses death duration of treatment effective Effectiveness EMA English FDA Final Hospitalization IMPROVE indican inhibitory activity media metabolism Modification Nirmatrelvir NSP11 Pandemia pandemic Patient Paxlovid PF-07321332 polyproteins pp1a pp1ab processing protease Protease inhibitor Proteases Proteins reducing risk Ritonavir SARS-CoV-1 SARS-CoV-2 sequence shown Spanish therapeutic target Treatment Viral variants [DOI] 10.37201/req/002.2022 PMC 바로가기 [Article Type] Review