A5066722637- RNA and protein synthesis mechanisms
- RNA modifications and cancer
- Machine Learning in Bioinformatics
- Chemical Synthesis and Analysis
- Biochemical and Molecular Research
- Click Chemistry and Applications
- Synthesis and biological activity
- Synthesis and Biological Evaluation
- HIV/AIDS drug development and treatment
- Cancer-related gene regulation
- Genomics and Phylogenetic Studies
- Bacterial Genetics and Biotechnology
- Epigenetics and DNA Methylation
- Enzyme Structure and Function
- RNA Research and Splicing
- Bacteriophages and microbial interactions
- DNA and Nucleic Acid Chemistry
- Histone Deacetylase Inhibitors Research
- Advanced biosensing and bioanalysis techniques
- Peptidase Inhibition and Analysis
- Pneumocystis jirovecii pneumonia detection and treatment
- Steroid Chemistry and Biochemistry
- Cancer Cells and Metastasis
- Cancer therapeutics and mechanisms
- Synthesis and Characterization of Heterocyclic Compounds
Zhengzhou University
2013-2024
KU Leuven
2018-2022
Ministry of Education of the People's Republic of China
2022
Rega Institute for Medical Research
2018-2021
Histone lysine specific demethylase 1 (LSD1) was reported to be overexpressed in several human cancers and recognized as a promising anticancer drug target. In the current study, we designed synthesized novel series of pyrimidine–thiourea hybrids evaluated their potential LSD1 inhibitory effect. One compounds, 6b, containing terminal alkyne appendage, shown most potent selective inhibitor vitro exhibited strong cytotoxicity against gastric cancer cells. Compound 6b also showed marked...
The pyrimidine-containing Trojan horse antibiotics albomycin and a recently discovered cytidine-containing microcin C analog target the class II seryl- aspartyl-tRNA synthetases (serRS aspRS), respectively. active components of these compounds are competitive inhibitors that mimic aminoacyl-adenylate intermediate. How they effectively substitute for interactions mediated by canonical purine group is unknown. Employing nonhydrolyzable aminoacyl-sulfamoyl nucleosides substituting base with...
Human cytosolic prolyl-tRNA synthetase (HcProRS) catalyses the formation of prolyl-tRNAPro, playing an important role in protein synthesis. Inhibition HcProRS activity has been shown to have potential benefits treatment fibrosis, autoimmune diseases and cancer. Recently, potent pyrazinamide-based inhibitors were identified by a high-throughput screening (HTS) method, but no further elaboration was reported. The pyrazinamide core is bioactive fragment found numerous clinically validated drugs...
Abstract To correctly aminoacylate tRNA Leu , leucyl-tRNA synthetase (LeuRS) catalyzes three reactions: activation of leucine by ATP to form leucyl-adenylate (Leu-AMP), transfer this amino acid and post-transfer editing any mischarged product. Although LeuRS has been well characterized biochemically, detailed structural information is currently only available for the latter two stages catalysis. We have solved crystal structures all enzymatic states Neisseria gonorrhoeae during Leu-AMP...
Emerging antibiotic resistance in pathogenic bacteria and reduction of compounds the existing antibiotics discovery pipeline is most critical concern for healthcare professionals. A potential solution aims to explore new or targets/compounds. Inhibition bacterial aminoacyl-tRNA synthetase (aaRSs) could be one such target development antibiotics. The aaRSs are a group enzymes that catalyze transfer an amino acid their cognate tRNA therefore play pivotal role translation. Thus, selective...
Aminoacyl-tRNA synthetases (aaRSs) have become viable targets for the development of antimicrobial agents due to their crucial role in protein translation. A series six amino acids were coupled purine-like 7-amino-5-hydroxymethylbenzimidazole nucleoside analogue following an optimized synthetic pathway. These compounds designed as aaRS inhibitors and can be considered 1,3-dideazaadenine analogues carrying a 2-hydroxymethyl substituent. Despite our intentions obtain N1-glycosylated...
Mycothiol (MSH), the major cellular thiol in Mycobacterium tuberculosis (Mtb), plays an essential role resistance of Mtb to various antibiotics and oxidative stresses. MshC catalyzes ATP-dependent ligation 1-O-(2-amino-2-deoxy-α-d-glucopyranosyl)-d-myo-inositol (GlcN-Ins) with l-cysteine (l-Cys) form l-Cys-GlcN-Ins, penultimate step MSH biosynthesis. The inhibition is lethal Mtb. In present study, five new cysteinyl-sulfonamides were synthesized, their binding affinity was evaluated using a...