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Expanding the Solvent/Protein Region Occupation of the Non-Nucleoside Reverse Transcriptase Inhibitor Binding Pocket for Improved Broad-Spectrum Anti-HIV-1 Efficacy: from Rigid Phenyl-Diarylpyrimidines to Flexible Hydrophilic Piperidine-Diarylpyrimidines.
J Med Chem
November 2024
Engineering Center of Catalysis and Synthesis for Chiral Molecules, Department of Chemistry, Fudan University, Shanghai 200433, China.
Considering the nonideal antiresistance efficacy of our previously reported non-nucleoside reverse transcriptase inhibitor , a series of novel piperidine-diarylpyrimidine derivatives were designed through expanding solvent/protein region occupation. The representative compound proved to be exceptionally potent against Y188L (EC = 23 nM), F227L + V106A (EC = 15 nM) and RES056 (EC = 45 nM), significantly better than . This analog exerted strong inhibition against wild-type HIV-1 (EC = 3 nM) and single mutant strains (L100I, K103N, Y181C, E138 K).
View Article and Find Full Text PDFComparative analysis of transcriptome in oil biosynthesis between seeds and non-seed tissues of fruit.
Front Plant Sci
October 2024
State Key Laboratory of Utilization of Woody Oil Resource, Hunan Academy of Forestry, Changsha, China.
The , a woody oil plant, has garnered attention for its oil-rich fruit, which exhibits potential for both oil production and ecological restoration endeavors, thereby presenting substantial developmental value. However, the comprehension of the distinctive oil biosynthesis and deposition strategies within the fruit's various compartments, coupled with the tissue-specific biosynthetic pathways yielding optimal fatty acid profiles, remains in its infancy. This investigation was designed to delineate the tissue specificity of oil biosynthetic disparities and to elucidate the molecular underpinnings within the fruit mesocarp and seeds of , employing lipidomic and transcriptomic analyses.
View Article and Find Full Text PDFIdentification of Novel Isatin Derivative Bearing a Nitrofuran Moiety as Potent Multi-Isoform Aldehyde Dehydrogenase Inhibitor.
Molecules
June 2024
Department of Pharmacology, Penn State Cancer Institute, Penn State College of Medicine, Hershey, PA 17033, USA.
Aldehyde dehydrogenases (ALDHs) are a family of enzymes that aid in detoxification and are overexpressed in several different malignancies. There is a correlation between increased expression of ALDH and a poor prognosis, stemness, and resistance to several drugs. Several ALDH inhibitors have been generated due to the crucial role that ALDH plays in cancer stem cells.
View Article and Find Full Text PDFInborn errors of the malate aspartate shuttle - Update on patients and cellular models.
Mol Genet Metab
August 2024
Division of Pediatric Endocrinology, Diabetology and Metabolism, Department of Pediatrics, Inselspital, Bern University Hospital, University of Bern, Bern, Switzerland; University Institute of Clinical Chemistry, Inselspital, Bern University Hospital, University of Bern, Bern, Switzerland. Electronic address:
The malate aspartate shuttle (MAS) plays a pivotal role in transporting cytosolic reducing equivalents - electrons - into the mitochondria for energy conversion at the electron transport chain (ETC) and in the process of oxidative phosphorylation. The MAS consists of two pairs of cytosolic and mitochondrial isoenzymes (malate dehydrogenases 1 and 2; and glutamate oxaloacetate transaminases 1 and 2) and two transporters (malate-2-oxoglutarate carrier and aspartate glutamate carrier (AGC), the latter of which has two tissue-dependent isoforms AGC1 and AGC2). While the inner mitochondrial membrane is impermeable to NADH, the MAS forms one of the main routes for mitochondrial electron uptake by promoting uptake of malate.
View Article and Find Full Text PDFHDAC3 inhibitors: a patent review of their broad-spectrum applications as therapeutic agents.
Expert Opin Ther Pat
April 2024
Pharmaceutical Chemistry, School of Pharmacy, University of the Western Cape, Bellville, South Africa.
Introduction: Histone deacetylases (HDACs) are a class of zinc-dependent enzymes. They maintain acetylation homeostasis, with numerous biological functions and are associated with many diseases. HDAC3 strictly requires multi-subunit complex formation for activity.
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