Techniques, influencing factors,advantages,disadvantages and advances in improvement of disease resistance using in vitro selection and somaclonal variation were summarized.
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Sci Rep
January 2025
Barcelona Institute for Global Health (ISGlobal, Hospital Clínic-University of Barcelona), Rosselló 149-153, Barcelona, 08036, Spain.
We recently characterized the potent antiplasmodial activity of the aggregated protein dye YAT2150, whose presumed mode of action is the inhibition of protein aggregation in the malaria parasite. Using single-dose and ramping methods, assays were done to select Plasmodium falciparum parasites resistant to YAT2150 concentrations ranging from 3× to 0.25× the in vitro IC of the compound (in the two-digit nM range) and performed a cross-resistance assessment in P.
View Article and Find Full Text PDFAnal Chem
January 2025
Center for Advanced Analytical Science, Guangzhou Key Laboratory of Sensing Materials and Devices, Guangdong Engineering Technology Research Center for Sensing Materials and Devices, School of Chemistry and Chemical Engineering, Guangzhou University, Guangzhou 510006, P. R. China.
The screening of glycoprotein markers has become an integral part of the in vitro diagnosis of malignant tumors. Herein, an electrochemical method based on alkaline phosphatase (ALP)-mediated enzymatic silver deposition is reported for the highly sensitive detection of glycoprotein tumor markers, in which ALP enzymes are decorated to the glycan moieties of targets via the lectin-carbohydrate interactions. As glycoproteins are conjugated with multiple glycan chains, lectin-mediated labeling can result in the decoration of each target with multiple ALP enzymes.
View Article and Find Full Text PDFJ Med Chem
January 2025
Guangdong Key Laboratory of Animal Conservation and Resource Utilization, Guangdong Public Laboratory of Wild Animal Conservation and Utilization, Institute of Zoology, Guangdong Academy of Sciences, Guangzhou, Guangdong 510260, China.
Pulmonary inflammation is the main cause of lung injury. Phosphodiesterase 4 (PDE4) is a promising anti-inflammatory target for the treatment of respiratory diseases. Herein, we designed and synthesized 43 compounds in two novel series of benzimidazole derivatives as PDE4 inhibitors.
View Article and Find Full Text PDFPLoS One
January 2025
Department of Medical Microbiology and Parasitology, School of Medical Sciences, Universiti Sains Malaysia, Kelantan, Malaysia.
Mushrooms are considered one of the safe and effective medications because they have great economic importance due to countless biological properties. Cordyceps militaris contains bioactive compounds with antioxidant, antimicrobial and anti-cancerous properties. This study was projected to analyze the potentials of biometabolites and to extract antimicrobial peptides and protein from the C.
View Article and Find Full Text PDFJ Med Chem
January 2025
Guangdong Provincial Key Laboratory of New Drug Screening, NMPA Key Laboratory for Research and Evaluation of Drug Metabolism, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, China.
Based on our previous work, a series of imidazole-based small molecules were designed and synthesized as HDAC3 inhibitors. Among them, compound showed selective HDAC3 inhibition activity with an IC of 53 nM (SI = 75 for HDAC3 over HDAC1). Further studies revealed that could dose-dependently induce the expression of PD-L1 in MC38 cells by activating the PD-L1 transcription.
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