We have recently developed a new synthetic methodology that provided both -aryl-5-hydroxytriazoles and -pyridine-4-alkyl triazoles. A selection of these products was carried through virtual screening towards targets that are contemporary and validated for drug discovery and development. This study determined a number of potential structure target dyads of which -pyridinium-4-carboxylic-5-alkyl triazole displayed the highest score specificity towards KAT2A. Binding affinity tests of abovementioned triazole and related analogs towards KAT2A confirmed the predictions of the assay. Finally, we have run inhibition assays of selected triazoles towards KAT2A; the ensemble of binding and inhibition assays delivered pyridyl-triazoles carboxylates as the prototype of a new class of inhibitors of KAT2A.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9331200 | PMC |
| http://dx.doi.org/10.1080/14756366.2022.2097447 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Acute inflammation induces acute megakaryopoiesis with impaired platelet production during fetal hematopoiesis.
Development
January 2025
Institute for Regenerative Medicine, State Key Laboratory of Cardiology and Medical Innovation Center, Shanghai East Hospital, School of Life Sciences and Technology, Tongji University, Shanghai 200092, China.
Hematopoietic development is tightly regulated by various factors. The role of RNA m6A modification during fetal hematopoiesis, particularly in megakaryopoiesis, remains unclear. Here, we demonstrate that loss of m6A methyltransferase METTL3 induces formation of double-stranded RNAs (dsRNAs) and activates acute inflammation during fetal hematopoiesis.
View Article and Find Full Text PDFDesign and Synthesis of Hederagenin Derivatives for the Treatment of Sepsis by Targeting TAK1 and Regulating the TAK1-NF-κB/MAPK Signaling.
J Med Chem
January 2025
School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation (Yantai University), Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University, Yantai 264005, PR China.
Sepsis is a systemic inflammatory response caused by infection and is a leading cause of death worldwide. We designed and synthesized a series of hederagenin analogues with anti-inflammatory activity. The most effective compound, , reduced the release of TNF-α and IL-6 in RAW264.
View Article and Find Full Text PDFEnhanced bacteriostatic effects of phage vB_C4 and cell wall-targeting antibiotic combinations against drug-resistant .
Microbiol Spectr
January 2025
Yunnan Provincial Key Laboratory of Animal Nutrition and Feed, Faculty of Animal Science and Technology, Yunnan Agricultural University, Kunming, China.
is a vital zoonotic pathogen known for its extensive drug resistance and ability to form biofilms, which contribute to its antibiotic resistance. In this study, the phage vB_C4, specifically targeting , was isolated and subjected to bioinformatic analysis and bacteriostatic activity assays. The combination of phage vB_C4 with antibiotics such as cephalothin and cefoxitin, which target the bacterial cell wall, resulted in a significantly enhanced bacteriostatic effect compared to either the phage or antibiotics alone.
View Article and Find Full Text PDFMetabolites, Biotransformation, and Plant-Growth Dual Regulatory Activity from Uncovered by the Fermentation Interaction with a Host.
J Agric Food Chem
January 2025
Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education, Yunnan Characteristic Plant Extraction Laboratory, Functional Molecules Analysis and Biotransformation Key Laboratory of Universities in Yunnan Province, School of Chemical Science and Technology, Yunnan University, Kunming 650091, People's Republic of China.
One new azaphilone derivative () from in ordinary medium, one new phthalide derivative (), a microbial transformation product of ingredients by , a pair of new austdiol enantiomers (+)- and (-)-, one new epsilon-caprolactone derivative (), and one new ophiobolin-type sesterterpenoid () from the in host medium were reported. The structures were determined by spectroscopic analysis and single-crystal X-ray diffraction. Compounds - could completely inhibit the germination of rice seeds at 50 μg/mL, which is higher than that of the positive control.
View Article and Find Full Text PDFTinagl1 restores tamoxifen sensitivity and blocks fibronectin-induced EMT by simultaneously blocking the EGFR and β1-integrin/FAK signaling pathways in tamoxifen-resistant breast cancer cells.
IUBMB Life
January 2025
Department of General Surgery, Beijing Anzhen Hospital, Capital Medical University, Beijing, China.
Tamoxifen (TAM) is employed to treat premenopausal ER-positive breast cancer patients, but TAM resistance is the main reason affecting its efficacy. Thus, addressing TAM resistance is crucial for improving therapeutic outcomes. This study explored the potential role of Tinagl1, a secreted extracellular matrix protein, whose expression is compromised in TAM-resistant MCF-7 breast cancer cells (MCF-7R).
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!