Dataset Information

Bench-to-bedside: Innovation of small molecule anti-SARS-CoV-2 drugs in China.

ABSTRACT: The ongoing COVID-19 pandemic has resulted in millions of deaths globally, highlighting the need to develop potent prophylactic and therapeutic strategies against SARS-CoV-2. Small molecule inhibitors (remdesivir, Paxlovid, and molnupiravir) are essential complements to vaccines and play important roles in clinical treatment of SARS-CoV-2. Many advances have been made in development of anti-SARS-CoV-2 inhibitors in China, but progress in discovery and characterization of pharmacological activity, antiviral mechanisms, and clinical efficacy are limited. We review development of small molecule anti-SARS-CoV-2 drugs (azvudine [approved by the NMPA of China on July 25, 2022], VV116 [approved by the NMPA of China on January 29, 2023], FB2001, WPV01, pentarlandir, and cepharanthine) in China and summarize their pharmacological activity, potential mechanisms of action, clinical trials and use, and important milestones in their discovery. The role of structural biology in drug development is also reviewed. Future studies should focus on development of diverse second-generation inhibitors with excellent oral bioavailability, superior plasma half-life, increased antiviral activity against SARS-CoV-2 and its variants, high target specificity, minimal side effects, reduced drug-drug interactions, and improved lung histopathology.

SUBMITTER: Yang L

PROVIDER: S-EPMC10193775 | biostudies-literature | 2023 Sep

REPOSITORIES: biostudies-literature

ACCESS DATA

Publications

Bench-to-bedside: Innovation of small molecule anti-SARS-CoV-2 drugs in China.

Yang Liyan L Wang Zhonglei Z

European journal of medicinal chemistry 20230518

The ongoing COVID-19 pandemic has resulted in millions of deaths globally, highlighting the need to develop potent prophylactic and therapeutic strategies against SARS-CoV-2. Small molecule inhibitors (remdesivir, Paxlovid, and molnupiravir) are essential complements to vaccines and play important roles in clinical treatment of SARS-CoV-2. Many advances have been made in development of anti-SARS-CoV-2 inhibitors in China, but progress in discovery and characterization of pharmacological activity ...[more]

PMID: 37229831

Similar Datasets

Project description:Purpose of reviewThe current standard care of treatment for glioblastoma multiforme (GBM) is never curative and exclusively involves the use of cytoxics upfront (e.g., radiation and chemotherapy). Current clinical protocols involve the use of single-agent targeted therapies, which inhibit specific pathways. Given the functional redundancies present in human tumors and escape mechanisms, it is highly unlikely that such a monotherapy approach will be successful in the treatment of GBM. Future directions of therapy for GBMs will likely involve the use of therapeutic cocktails, including more than one target specific inhibitors based on tumor escape mechanism, genetic, epigenetic and molecular signatures. This review addresses some of the relevant issues.Recent findingsCorrelative clinical studies from various clinical trials and preclinical studies have provided the meticulous use of chemotherapeutics and radiation based on molecular profiling of tumors. Alkylating agents such as temozolomide lose their efficacy if DNA repair enzyme expression is upregulated. The alternative strategies include targeting the enzyme or one can use poly (ADP) ribose inhibitor to inhibit base excision repair pathway rather than mismatch repair pathway. Currently, several inhibitors in this category are in clinical trials. Next, we have addressed new avenues including radiosensitizers, hypoxia, metabolism, angiogenesis, invasive and infiltrative nature of tumors and potential molecular targets, which can be exploited for clinical trials. Finally, we have included some aspect of genome-wide association studies and correlative analysis and the lessons learned to design better clinical trials.SummaryAdvances in profiling the noncoding RNAs, genetic, epigenetic profiles, metabolomics, genomics and proteomics may uncover important resistance mechanisms in GBM. Personalized therapy using various therapeutic cocktails targeting these resistance mechanisms may prove even more effective in the future management of GBMs.

Dataset Information

Bench-to-bedside: Innovation of small molecule anti-SARS-CoV-2 drugs in China.

Publications

Bench-to-bedside: Innovation of small molecule anti-SARS-CoV-2 drugs in China.

Similar Datasets

OmicsDI is part of the ELIXIR infrastructure

Tweets