Thiol-Reactive or Redox-Active: Revising a Repurposing Screen Led to a New Invalidation Pipeline and Identified a True Noncovalent Inhibitor Against Papain-like Protease from SARS-CoV-2 DOI Creative Commons
Maria Kuzikov,

Stefano Morasso,

Jeanette Reinshagen

и другие.

ACS Pharmacology & Translational Science, Год журнала: 2024, Номер 8(1), С. 66 - 77

Опубликована: Окт. 4, 2024

The SARS-CoV-2 papain-like protease PLpro has multiple roles in the viral replication cycle, related to both its polypeptide cleavage function and ability antagonize host immune response. Targeting is recognized as a promising mechanism modulate replication, while supporting responses. However, development of PLpro-specific inhibitors remains challenging. Comprehensive investigations utilizing enzymatic, binding studies, cellular assays revealed previously reported act an unspecific manner. At present, GRL-0617 derivatives remain best-validated compounds with demonstrated antiviral activity cells mouse models. In this study, we refer pitfalls redox sensitivity PLpro. Using screening-based approach identify PLpro's proteolytic activity, made extensive efforts validate active over range conditions readouts, emphasizing need for comprehensive orthogonal data when profiling putative inhibitors. remaining compound, CPI-169, was shown be noncovalent inhibitor capable competing NMR-based experiments, suggesting that it occupied similar site inhibited Vero-E6 cells, opening new design opportunities further agents.

Язык: Английский

Ensitrelvir for the Treatment of Nonhospitalized Adults with COVID-19: Results from the SCORPIO-HR, Phase 3, Randomized, Double-blind, Placebo-Controlled Trial DOI Creative Commons
Anne F. Luetkemeyer, Kara W. Chew,

Stuart R. Lacey

и другие.

Clinical Infectious Diseases, Год журнала: 2025, Номер unknown

Опубликована: Янв. 20, 2025

Ensitrelvir, a severe acute respiratory syndrome coronavirus-2 main protease inhibitor, has demonstrated clinical and virologic efficacy in previous studies. In this global phase 3 trial, nonhospitalized adults with mild-to-moderate coronavirus disease 2019 (COVID-19) symptom onset within 5 days were randomized (1:1) to receive once-daily ensitrelvir (375 mg day 1, 125 2-5) or blinded matching placebo. The primary endpoint was the restricted mean time sustained (≥2 days) resolution of 15 COVID-19 symptoms, recorded participant daily diaries, through 29 participants starting treatment after onset. Virologic safety assessed. Of 2093 participants, 1888 started Mean 12.5 13.1 placebo, respectively (difference, -0.6 days; 95% confidence interval, -1.38 0.19; P = .14). On 4, reduced least-squares RNA by 0.72 log10 copies/mL more than placebo (95% 0.55-0.90). Among those positive viral cultures at enrollment, 274/287 (95.5%) ensitrelvir-treated versus 210/280 (75.0%) placebo-treated had negative on 4. rebound similar (<1.5%) between groups. proportion ≥1 adverse event (61.5%) (60.6%). No treatment-related serious events deaths occurred. Three (0.3%) 1 (0.1%) COVID-19-related hospitalizations 29. Despite evidence antiviral activity ensitrelvir, trial did not demonstrate significant difference resolution.

Язык: Английский

Процитировано

1

mRNA vaccine platforms: linking infectious disease prevention and cancer immunotherapy DOI Creative Commons
Dariush Haghmorad, Majid Eslami,

Niloufar Orooji

и другие.

Frontiers in Bioengineering and Biotechnology, Год журнала: 2025, Номер 13

Опубликована: Март 12, 2025

The advent of mRNA vaccines, accelerated by the global response to COVID-19 pandemic, marks a transformative shift in vaccine technology. In this article, we discuss development, current applications, and prospects vaccines for both prevention treatment infectious diseases oncology. By leveraging capacity encode antigens within host cells directly, provide versatile scalable platform suitable addressing broad spectrum pathogens tumor-specific antigens. We highlight recent advancements design, innovative delivery mechanisms, ongoing clinical trials, with particular emphasis on their efficacy combating diseases, such as COVID-19, Zika, influenza, well emerging potential cancer immunotherapy. also address critical challenges, including stability, optimization immune responses, broader issue accessibility. Finally, review strategies advancing next-generation aim overcoming limitations technology enhancing preventive therapeutic approaches oncological diseases.

Язык: Английский

Процитировано

1

12-month persistence of immune responses to self-amplifying mRNA COVID-19 vaccines: ARCT-154 versus BNT162b2 vaccine DOI Creative Commons
Yoshiaki Oda,

Yuji Kumagai,

Manabu Kanai

и другие.

The Lancet Infectious Diseases, Год журнала: 2024, Номер unknown

Опубликована: Окт. 1, 2024

Язык: Английский

Процитировано

7

Comparative Study of Ensitrelvir and Symptomatic Therapy in Healthcare Workers with Mild COVID-19: A Single Center Retrospective Analysis in Chiba, Japan. DOI
Jun Hirai, Yuki Hanai

Journal of Infection and Chemotherapy, Год журнала: 2025, Номер unknown, С. 102668 - 102668

Опубликована: Фев. 1, 2025

Язык: Английский

Процитировано

0

Genomic epidemiology and evolutionary dynamics of the Omicron variant of SARS-CoV-2 during the fifth wave of COVID-19 in Pakistan DOI Creative Commons

Aroona Razzaq,

Cyrollah Disoma, Sara Iqbal

и другие.

Frontiers in Cellular and Infection Microbiology, Год журнала: 2024, Номер 14

Опубликована: Окт. 22, 2024

Introduction The coronavirus disease 2019 (COVID-19) pandemic, caused by severe acute respiratory syndrome 2 (SARS-CoV-2), has posed extraordinary challenges to global health systems and economies. virus’s rapid evolution resulted in several variants of concern (VOCs), including the highly transmissible Omicron variant, characterized extensive mutations. In this study, we investigated genetic diversity, population differentiation, evolutionary dynamics VOC during fifth wave COVID-19 Pakistan. Methods A total 954 genomes sequenced Pakistan were analyzed. Bayesian framework was employed for phylogenetic reconstructions, molecular dating, analysis. Results Using a genomics approach, analyzed Pakistani samples, revealing low within-population diversity significant structural variation spike (S) protein. Phylogenetic analysis showed that variant originated from two distinct lineages, BA.1 BA.2, which introduced South Africa, Thailand, Spain, Belgium. Omicron-specific mutations, those receptor-binding domain, identified. estimated rate 2.562E-3 mutations per site year (95% HPD interval: 8.8067E-4 4.1462E-3). skyline plot indicated expansion at end 2021, coinciding with outbreak. Comparative other VOCs as divergent, monophyletic group, suggesting unique pathway. Conclusions This study provides comprehensive overview Omicron’s genomic epidemiology, Pakistan, emphasizing need collaboration monitoring enhancing pandemic preparedness.

Язык: Английский

Процитировано

1

Thiol-Reactive or Redox-Active: Revising a Repurposing Screen Led to a New Invalidation Pipeline and Identified a True Noncovalent Inhibitor Against Papain-like Protease from SARS-CoV-2 DOI Creative Commons
Maria Kuzikov,

Stefano Morasso,

Jeanette Reinshagen

и другие.

ACS Pharmacology & Translational Science, Год журнала: 2024, Номер 8(1), С. 66 - 77

Опубликована: Окт. 4, 2024

The SARS-CoV-2 papain-like protease PLpro has multiple roles in the viral replication cycle, related to both its polypeptide cleavage function and ability antagonize host immune response. Targeting is recognized as a promising mechanism modulate replication, while supporting responses. However, development of PLpro-specific inhibitors remains challenging. Comprehensive investigations utilizing enzymatic, binding studies, cellular assays revealed previously reported act an unspecific manner. At present, GRL-0617 derivatives remain best-validated compounds with demonstrated antiviral activity cells mouse models. In this study, we refer pitfalls redox sensitivity PLpro. Using screening-based approach identify PLpro's proteolytic activity, made extensive efforts validate active over range conditions readouts, emphasizing need for comprehensive orthogonal data when profiling putative inhibitors. remaining compound, CPI-169, was shown be noncovalent inhibitor capable competing NMR-based experiments, suggesting that it occupied similar site inhibited Vero-E6 cells, opening new design opportunities further agents.

Язык: Английский

Процитировано

0