Institut de Biomedicina (IBUB): Recent submissions
Now showing items 1-20 of 337
Intergenerational effects of maternal childhood maltreatment on newborns' stress regulation: The role of maternal depressive symptoms
Background: Maternal childhood maltreatment (CM) has been repeatedly associated with negative offspring's emotional outcomes. The dysregulation of the Hypothalamic-Pituitary-Adrenal (HPA) axis has emerged as the main ...
Reinterpreting anomalous competitive binding experiments within G protein-coupled receptor homodimers using a dimer receptor model
An increasing number of G protein-coupled receptors (GPCRs) have been reported to be expressed in the plasma membrane as dimers. Since most ligand binding data are currently fitted by classical equations developed only for ...
Design of a true bivalent ligand with picomolar affinity for a G protein-coupled receptor homodimer
Bivalent ligands have emerged as chemical tools to study G protein-coupled receptor dimers. Using a combination of computational, chemical, and biochemical tools, here we describe the design of bivalent ligand 13 with high ...
Elafibranor upregulates the EMT-inducer S100A4 via PPARbeta/delta
Elafibranor is a dual peroxisome proliferator-activated receptor (PPAR)α and β/δ agonist that has reached a phase III clinical trial for the treatment of metabolic dysfunction-associated steatotic liver disease (MASLD). ...
Model-driven discovery of long-chain fatty acid metabolic reprogramming in heterogeneous prostate cancer cells.
Epithelial-mesenchymal-transition promotes intra-tumoral heterogeneity, by enhancing tumor cell invasiveness and promoting drug resistance. We integrated transcriptomic data for two clonal subpopulations from a prostate ...
Alternative access to functionalized 2,8-ethanonoradamantane derivatives
7a-(Methoxycarbonyl)-N-methyl-1,3a,5,6,7,7a-hexahydro-4H-1,4,6-(epiethane[1,1,2]triyl) indene-4,9-dicarboximide has been prepared through a modification of a previous synthetic sequence, in which the benzyloxymethyl hydroxyl ...
Induction of oxidative metabolism by the p38α/MK2 pathway
Adequate responses to environmental stresses are essential for cell survival. The regulation of cellular energetics that involves mitochondrial energy production and oxidative stress is central in the process of stress ...
Oleate Reverses Palmitate-induced Insulin Resistance and Inflammation in Skeletal Muscle Cells
Here we report that in skeletal muscle cells the contribution to insulin resistance and inflammation of two common dietary long-chain fatty acids depends on the channeling of these lipids to distinct cellular metabolic ...
A heterobivalent ligand for the adenosine A2A-dopamine D2 receptor heteromer
A G protein-coupled receptor heteromer that fulfills the established criteria for its existence in vivo is the complex between adenosine A2A (A2AR) and dopamine D2 (D2R) receptors. Here, we have designed and synthesized ...
A synthetic approach to ervatamine-silicine alkaloids. Enantioselective total synthesis of (-)-episilicine
Starting from an appropriate unsaturated phenylglycinol-derived oxazolopiperidone lactam, the synthesis of (-)-16-episilicine is reported, the key steps being a stereoselective conjugate addition, a stereoselective alkylation, ...
Unique pharmacodynamic properties and low abuse liability of the µ-opioid receptor ligand (S)-methadone
(R,S)-methadone ((R,S)-MTD) is a µ-opioid receptor (MOR) agonist comprised of (R)-MTD and (S)-MTD enantiomers. (S)-MTD is being developed as an antidepressant and is considered an N-methyl-D-aspartate receptor (NMDAR) ...
Brown adipose tissue bioenergetics: a new methodological approach
The rediscovery of brown adipose tissue (BAT) in humans and its capacity to oxidize fat and dissipate energy as heat has put the spotlight on its potential as a therapeutic target in the treatment of several metabolic ...
Targeting FGF21 for the treatment of nonalcoholic steatohepatitis
Nonalcoholic steatohepatitis (NASH), the severe stage of nonalcoholic fatty liver disease (NAFLD), is defined as the presence of hepatic steatosis with inflammation, hepatocyte injury, and different degrees of fibrosis. ...
Neuroprotective effects of the multitarget agent AVCRI104P3 in brain of middle-aged mice
Molecular factors involved in neuroprotection are key in the design of novelmultitarget drugs in aging and neurodegeneration. AVCRI104P3 is a huprine derivative that exhibits potent inhibitory effects on human AChE, BuChE, ...
Determination of the aqueous pKa of very insoluble drugs by capillary electrophoresis: Internal standards for methanol-water extrapolation
A fast determination of acidity constants (pKa) of very insoluble drugs has become a necessity in drug discovery process because it often produces molecules that are highly lipophilic and sparingly soluble in water. In ...
Fructose effects on human health: Molecular insights from experimental models
Podeu consultar el llibre complet a: http://hdl.handle.net/2445/63704
HIF drives lipid deposition and cancer in ccRCC via repression of fatty acid metabolism
Clear cell renal cell carcinoma (ccRCC) is histologically defined by its lipid and glycogen-rich cytoplasmic deposits. Alterations in the VHL tumor suppressor stabilizing the hypoxiainducible factors (HIFs) are the most ...
SiNoPsis: single nucleotide polymorphisms selection and promoter profiling
Motivation: The selection of a single nucleotide polymorphism (SNP) using bibliographic methods can be a very time-consuming task. Moreover, a SNP selected in this way may not be easily visualized in its genomic context ...
Studies on the Synthesis of Phlegmarine-Type Lycopodium Alkaloids: Enantioselective Synthesis of (−)-Cermizine B, (+)-Serratezomine E, and (+)-Luciduline
The synthesis of the Lycopodium alkaloids, (-)-cermizine B, (+)-serratezomine E, and (+)-luciduline using phenylglycinol-derived tricyclic lactams as chiral scaffolds, is reported. The requisite lactams are prepared by a ...
