A5059468550- HIV/AIDS drug development and treatment
- HIV Research and Treatment
- Click Chemistry and Applications
- Pneumocystis jirovecii pneumonia detection and treatment
- Hepatitis C virus research
- Computational Drug Discovery Methods
- Influenza Virus Research Studies
- Biochemical and Molecular Research
- Chemical Synthesis and Analysis
- Synthesis and biological activity
- Synthesis and Characterization of Heterocyclic Compounds
- Hepatitis B Virus Studies
- Monoclonal and Polyclonal Antibodies Research
- interferon and immune responses
- Quinazolinone synthesis and applications
- HIV/AIDS Research and Interventions
- SARS-CoV-2 and COVID-19 Research
- Synthesis and Biological Evaluation
- Traditional Chinese Medicine Analysis
- RNA and protein synthesis mechanisms
- Protein Degradation and Inhibitors
- Gout, Hyperuricemia, Uric Acid
- Receptor Mechanisms and Signaling
- Cholinesterase and Neurodegenerative Diseases
- Respiratory viral infections research
Shandong University
2016-2025
Xiamen University of Technology
2024
Xiamen University
2024
Dalian Dermatosis Hospital
2024
China National Rice Research Institute
2021-2023
Yunnan Academy of Agricultural Sciences
2022
State Key Laboratory of Chemical Engineering
2021
Universidade Federal de Alagoas
2021
KU Leuven
2020
Duke University
2020
Abstract Coronavirus disease 2019 (COVID-19), caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has quickly spread worldwide and affected more than 10 million individuals. A typical feature of COVID-19 is the suppression type I III interferon (IFN)-mediated antiviral immunity. However, molecular mechanism which SARS-CoV-2 evades immunity remains elusive. Here, we reported that membrane (M) protein inhibits production IFNs induced cytosolic dsRNA-sensing pathway mediated...
An overview of the broad-ranging pharmacological applications 8-HQ derivatives.
Abstract As a highly pathogenic human coronavirus, SARS-CoV-2 has to counteract an intricate network of antiviral host responses establish infection and spread. The nucleic acid-induced stress response is essential component defense closely related innate immunity. However, whether regulates the pathway achieve immune evasion remains elusive. In this study, NSP5 N protein were found attenuate granule (avSG) formation. Moreover, suppressed IFN expression induced by Sendai virus or...
Human immunodeficiency virus (HIV) infection is now pandemic. Targeting HIV-1 reverse transcriptase (HIV-1 RT) has been considered as one of the most successful targets for development anti-HIV treatment. Among RT inhibitors, non-nucleoside inhibitors (NNRTIs) have gained a definitive place due to their unique antiviral potency, high specificity, and low toxicity in antiretroviral combination therapies used treat HIV. Until now, >50 structurally diverse classes compounds reported NNRTIs....
ADVERTISEMENT RETURN TO ISSUEPREVPerspectiveNEXTStrategies for the Design of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors: Lessons from Development Seven Representative ParadigmsDongyue Li†, Peng Zhan†, Erik De Clercq‡, and Xinyong Liu*†View Author Information† Department Medicinal Chemistry, School Pharmaceutical Sciences, Shandong University, 44, West Culture Road, 250012, Jinan, Shandong, P. R. China‡ Rega Institute Medical Research, K.U. Leuven, Minderbroedersstraat 10, B-3000...
We designed and synthesized a series of human immunodeficiency virus type 1 (HIV-1) non-nucleoside reverse transcriptase inhibitors (NNRTIs) with piperidine-substituted thiophene[3,2-d]pyrimidine scaffold, employing strategy structure-based molecular hybridization substituent decorating. Most the compounds exhibited broad-spectrum activity low (single-digit) nanomolar EC50 values toward panel wild-type (WT), single-mutant, double-mutant HIV-1 strains. Compound 27 was most potent; compared...
To address drug resistance to HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs), a series of novel diarylpyrimidine (DAPY) derivatives targeting "tolerant region I" and II" the NNRTIs binding pocket (NNIBP) were designed utilizing structure-guided scaffold-hopping strategy. The dihydrofuro[3,4-d]pyrimidine 13c2 13c4 proved be exceptionally potent against wide range strains carrying single NNRTI-resistant mutations (EC50 = 0.9–8.4 nM), which remarkably superior that etravirine...
The continuous spread of SARS-CoV-2 calls for more direct-acting antiviral agents to combat the highly infectious variants. main protease (Mpro) is an promising target anti-SARS-CoV-2 drug design. Here, we report discovery potent non-covalent non-peptide Mpro inhibitors featuring a 1,2,4-trisubstituted piperazine scaffold. We systematically modified hit MCULE-5948770040 by structure-based rational design combined with multi-site binding and privileged structure assembly strategies. optimized...
Currently, HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) are a major component of the highly active anti-retroviral therapy (HAART) regimen. However, occurrence drug-resistant strains and adverse reactions after long-term usage have inevitably compromised clinical application NNRTIs. Therefore, development novel with distinct anti-resistance profiles better pharmacological properties is still an enormous challenge. Herein, we summarize state-of-the-art medicinal chemistry...
N-Methyl-d-aspartate (NMDA) receptors, a subtype of ionotropic glutamate receptors in the central nervous system (CNS), have garnered attention for their role brain disorders. Specifically, GluN2A-containing NMDA emerged as potential therapeutic target treatment depressive disorders and epilepsy. However, development receptor-selective antagonists, represented by N-(4-(2-benzoylhydrazine-1-carbonyl)benzyl)-3-chloro-4-fluorobenzenesulfonamide (TCN-201) its derivatives, faces significant...