Bioquímica i Biomedicina Molecular: Envíos recientes
Mostrando ítems 1-20 de 917
The multimerization pathway of the glucocorticoid receptor
The glucocorticoid receptor (GR) is a leading drug target due to its antiinflammatory and immunosuppressive roles. The functional oligomeric conformation of full-length GR (FL-GR), which is key for its biological activity, ...
Synthesis and biological evaluation of novel carnosic acid derivatives with anticancer activity
Novel derivatives of carnosic acid 1 with ester or carbamate groups at C-20 and derivatives with these functional groups combined with benzylic modifications (C-7) were synthesized and evaluated in a colorectal cancer cell ...
Metabolic Singularities in Microsatellite-Stable Colorectal Cancer: Identifying Key Players in Immunosuppression to Improve the Immunotherapy Response.
Although immune checkpoint inhibitor (ICI) therapy is currently the standard of care in microsatellite-unstable (MSI) metastatic colorectal cancer (CRC), ICI therapy, alone or in combination with other therapies, is not a ...
The Glycolytic Gatekeeper PDK1 defines different metabolic states between genetically distinct subtypes of human acute myeloid leukemia
Acute myeloid leukemia remains difficult to treat due to strong genetic heterogeneity between and within individual patients. Here, we show that Pyruvate dehydrogenase kinase 1 (PDK1) acts as a targetable determinant of ...
Inhibition of the succinyl dehydrogenase complex in acute myeloid leukemia leads to a lactate-fuelled respiratory metabolic vulnerability
Metabolic programs can differ substantially across genetically distinct subtypes of acute myeloid leukemia (AML). These programs are not static entities but can change swiftly as a consequence of extracellular changes or ...
Polo-like kinase 1 inhibitors in refractory colorectal cancer: deciphering the myth of synthetic lethality
Metastatic colorectal cancer (mCRC) remains a highly lethal disease because resistance to chemotherapy and targeted agents—including anti-VEGF and anti-EGFR therapies—emerges rapidly and universally. In RAS‑mutant mCRC, ...
Metabolic plasticity drives specific mechanisms of chemotherapy and targeted therapy resistance in metastatic colorectal cancer
Microsatellite-stable metastatic colorectal cancer (MSS mCRC) is currently treated with chemotherapy and targeted agents based on RAS and BRAF mutational status. Although these therapies offer initial benefit, most patients ...
Current efficacy of immune checkpoint inhibitors in microsatellite unstable colorectal cancer and potential biomarkers
Microsatellite unstable (MSI) colorectal cancer (CRC) tumors have a high mutational load (particularly frame-shift mutations) that creates numerous neoantigens that are presented to major histocompatibility complex molecules ...
Transcriptomic profiling of endothelial progenitor cells in post-COVID-19 patients: Insights at 3- and 6-month post-infection
Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has caused significant global morbidity since 2019. Long COVID, characterized by persistent symptoms after acute infection, may involve endothelial injury. We ...
Hints on the Lateralization of Dopamine Binding to D-1 Receptors in Rat Striatum
Dopamine receptors in striatum are important for healthy brain functioning and are the target of levodopa-based therapy in Parkinson's disease. Lateralization of dopaminergic neurotransmission in striata from different ...
Determination of 3-Hydroxy-3-methylglutaryl CoA Reductase Activity in Plants
The enzyme 3-hydroxy-3-methylglutaryl CoA (HMG-CoA) reductase catalyzes the NADPH-mediated reductive deacylation of HMG-CoA to mevalonic acid, which is the first committed step of the mevalonate pathway for isoprenoid ...
Targeting and topology in the membrane of plant 3-hydroxy-3-methylglutaryl Coenzyme A reductase
The enzyme 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGR) catalyzes the synthesis of mevalonate. This is the first committed step of isoprenoid biosynthesis. A common feature of all known plant HMGR isoforms is the ...
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 ...
Identification of auxin-binding proteins using an improved assay for photoaffinity labeling with 5-N<sub>3</sub>-[7-<sup>3</sup>H]-indole-3-acetic acid
We have developed an improved assay for detection of auxin-binding proteins using photoaffinity labeling. We have synthesized 5-NH<sub>2</sub>-[7-<sup>3</sup>H]indole-3-acetic acid (IAA) and 5-N<sub>3</sub>-[7-<sup>3</sup>H]IAA ...
Identification of gcpE as a novel gene of the 2-C-methyl-D-erythritol 4-phosphate pathway for isoprenoid biosynthesis in Escherichia coli.
The 2-C-methyl-D-erythritol 4-phosphate (MEP) pathway for isoprenoid biosynthesis is essential in most eubacteria and plants and has remarkable biotechnological interest. However, only the first steps of this pathway have ...
Identification of a 23 kDa protein from maize photoaffinity labelled with 5-azido-[7-3 H]indol-3-ylacetic acid.
A 23 kDa protein (p23) was identified in microsomal extracts from maize coleoptiles by photoaffinity labelling with 5-azido-[7-<sup>3</sup>H]indol-3-ylacetic acid ([<sup>3</sup>H]N<sub>3</sub>IAA). Labelling of p23 was ...
<em>In vitro</em> uptake and processing of maize auxin-binding proteins by ER-derived microsomes
We have analyzed auxin-binding proteins from maize encoded by the Zm-ERabp gene family. Open reading frames of cDNA clones predict proteins containing N-terminal hydrophobic signal sequences. In vitro studies show that the ...
5-Hydroxypentane-2,3-dione (laurencione), a bacterial metabolite of 1-deoxy-D-threo-pentulose
Cell-free systems from the bacteria Escherichia coli and Klebsiella planticola that were incubated with 13C labeled pyruvate and D-glyceraldehyde synthesized 5-hydroxypentane-2,3-dione (laurencione) along with 1-deoxy-D- ...
Isoprenoid biosynthesis via the methylerythritol phosphate pathway: accumulation of 2-C-methyl-erythritol2,4-cyclodiphosphate in a gcpE deficient mutant of Escherichia coli
In the bacterium Escherichiacoli, gcpE is an essential gene in the methylerythritol phosphate pathway for isoprenoid biosynthesis. Incubation of [1-3H]methylerythritol with an E. coli mutant defective in the gcpE gene ...
Isoprenoid biosynthesis via the methylerythritol phosphate pathway. (E)-4-Hydroxy-3-methylbut-2-enyl diphosphate: chemical synthesis and formation from methylerythritol cyclodiphosphate by a cell-free system from Escherichia coli
2-C-Methyl-d-erythritol cyclodiphosphate is converted into (E)-4-hydroxy-3-methylbut-2-enyl diphosphate by a cell-free system from an Escherichia coli strain overexpressing the gcpE gene. The latter diphosphate, representing ...
