The synthesis of the analogs of N-3-oxododecanoyl-L-homoserine lactone (1) and their structure-activity relationship for the apoptotic induction in macrophages, P388D1 cells, are described. It was revealed that the position of the oxo group in the acyl side chain in addition to the presence of the L-homoserine lactone unit is crucial for the apoptosis-inducing activity. Furthermore, the long acyl side chains with hydrophobic distal ends are preferable for the activity.
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http://dx.doi.org/10.1016/j.bmcl.2006.01.054 | DOI Listing |
J Lipid Res
January 2025
Laboratory of Molecular Pharmacology, Biosignal Research Center, Kobe University, Kobe, 657-8501, Japan. Electronic address:
At least 10% of proteins constituting the human proteome are subject to S-acylation by a long-chain fatty acid, thioesterified to a Cys thiol side chain. Fatty S-acylation (prototypically, S-palmitoylation) operates across eukaryotic phylogeny and cell type. S-palmitoylation is carried out in mammalian cells by a family of 23-24 dedicated zDHHC palmitoyl transferase enzymes, and mutation of zDHHCs is associated with a number of human pathophysiologies.
View Article and Find Full Text PDFNeurogenetics
January 2025
Department of Otolaryngology & Head and Neck, Liuzhou Worker's Hospital of Guangxi Zhuang Autonomous Region, 156 Heping Road, Liuzhou, 545007, China.
Background: Mutations in the LARS2 gene are correlated with Perrault syndrome, a rare autosomal recessive genetic disorder, that is typically characterized by sensorineural hearing loss and ovarian insufficiency.
Methods: Whole-exome sequencing and mutational analysis were employed to identify hearing loss-causing genes in a Chinese family from the Guangxi Zhuang Autonomous Region. Clinical phenotypes, audiological data, and color Doppler ultrasound of the family were collected, and a series of computer software were used to analyze the impact of genetic variations on protein structure and function.
EMBO J
January 2025
Cambridge Institute for Medical Research, University of Cambridge, Cambridge, CB2 0XY, UK.
Biogenesis of membrane-bound organelles involves the synthesis, remodeling, and degradation of their constituent phospholipids. How these pathways regulate organelle size remains poorly understood. Here we demonstrate that a lipid-degradation pathway inhibits expansion of the endoplasmic reticulum (ER) membrane.
View Article and Find Full Text PDFJ Agric Food Chem
January 2025
State Key Laboratory of Vegetable Biobreeding, Institute of Vegetables and Flowers, Chinese Academy of Agricultural Sciences, Beijing 100081, China.
Texenomycins are a family of linear lipopeptaibols with a long polyketide side chain at the N-terminus and 21 amino acid residues at the -terminus, presenting demonstrated potential as antibiotics against plant fungal pathogens. In this study, texenomycins were identified and isolated from the fungus strain TTI-0396 and showed effective antifungal properties against two plant pathogens and . Through analysis of the whole-genome data of strain TTI-0396, we discovered a hybrid PKS-NRPS system with the polyketide synthase (PKS: TexQ), thioesterase (TexO), acyl-CoA ligase (TexI), and three nonribosomal peptide synthetases (NRPSs: TexG, TexJ, TexV) in the gene cluster that were proposed to be responsible for the biosynthesis of texenomycins and another related lipopeptaibol, lipohexin.
View Article and Find Full Text PDFPharmacol Res
January 2025
School of Pharmacy, Macau University of Science and Technology, Macau 999078, China; Laboratory of Cardiovascular Diseases, Xiyuan Hospital, China Academy of Chinese Medical Sciences, Beijing 100091, China. Electronic address:
Atherosclerosis (AS) is a major etiological factor underpinning a spectrum of cardiovascular diseases, leading to cerebral infarction, coronary artery disease, and peripheral vascular disease. The chronic progression of AS, spanning from initial plaque formation to the occurrence of acute cardiovascular events, underscores the complexity of AS and the challenges it presents in terms of treatment. Currently, the clinical management of AS relies predominantly on statins and proprotein convertase subtilisin/kexin type 9 inhibitors, which primarily aim to reduce low-density lipoprotein levels and have demonstrated some therapeutic efficacy.
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