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Directed evolution of diacylglycerol acyltransferases 2 promotes lipids and triglyceride accumulation.
Plant Mol Biol
January 2025
College of Life Sciences, Northwest A & F University, Xi'an, 710000, China.
Triacylglycerol (TAG) is a major component of plant-neutral lipids. Diacylglycerol acyltransferase 2 (DGAT2) plays an important role in plant oil accumulation by catalyzing the final step of the Kennedy pathway. In this study, ten DGAT2 sequences were originating from different oil crops into the TAG-deficient yeast strain H1246, to compare their enzyme activity of oil synthesis and filter out potential amino acid residue sites for directed evolution.
View Article and Find Full Text PDFValsartan Loaded Solid Self-Nanoemulsifying Delivery System to Enhance Oral Absorption and Bioavailability.
AAPS PharmSciTech
January 2025
College of Pharmacy, Jiangxi University of Chinese Medicine, Nanchang, 330004, China.
Valsartan (VST) is an angiotensin II receptor antagonist with low oral bioavailability. The present study developed a solid self-nanoemulsifying drug delivery system (S-SNEDDS) to enhance the oral absorption and bioavailability of VST. VST-loaded liquid SNEDDS (VST@L-SNEDDS) was prepared by investigating the solubility of VST and constructing the pseudo-ternary phase diagrams.
View Article and Find Full Text PDFSynthesis and biological evaluation of rationally designed pyrazoles as insecticidal agents.
Mol Divers
January 2025
Department of Pharmaceutics, College of Pharmacy, King Saud University, 11451, Riyadh, Saudi Arabia.
The current research focused on the synthesis of two series of pyrazole derivatives and evaluation of their insecticidal effectiveness. In the first series, seven pyrazole Schiff bases 3a-g were successfully synthesized with yields (79-95%) by condensing phenylfuran-2-carbaldehyde with substituted pyrazole rings. In the second series, eleven amino acid-pyrazole conjugates 6a-k were synthesized utilizing acetic acid, sulfuric acid, morpholine, and EDC.
View Article and Find Full Text PDFA Novel Peptide Mapping Method Utilizing Cysteine as a Reducing Agent.
Pharm Res
January 2025
Institute of Drug Metabolism and Pharmaceutical Analysis, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, 310058, China.
Purposes: In the peptide mapping reduction process for monoclonal antibodies (mAbs) and other proteins, the conventional reducing reagents β-mercaptoethanol (β-ME) and dithiothreitol (DTT) pose challenges due to their strong odor and toxicity at high concentrations. Cysteine (Cys), an essential amino acid for new protein synthesis, is an overlooked, nontoxic, and odorless reducing agent. This study presents a novel peptide mapping method using Cys as the reducing agent.
View Article and Find Full Text PDFPharmacological and structural insights into nanvuranlat, a selective LAT1 (SLC7A5) inhibitor, and its N-acetyl metabolite with implications for cancer therapy.
Sci Rep
January 2025
Department of Bio-System Pharmacology, Graduate School of Medicine, Osaka University, 2-2, Yamadaoka, Suita, Osaka, 565-0871, Japan.
L-type amino acid transporter 1 (LAT1, SLC7A5), overexpressed in various cancers, mediates the uptake of essential amino acids crucial for tumor growth. It has emerged as a promising target for cancer therapy. Nanvuranlat (JPH203/KYT-0353), a LAT1 inhibitor, has shown antitumor activity in preclinical studies and efficacy in biliary tract cancer during clinical trials.
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