Search results for "Receptor"

Brain Opioid Activity and Oxidative Injury: Different Molecular Scenarios Connecting Celiac Disease and Autistic Spectrum Disorder

2020

Celiac Disease (CD) is an immune-mediated disease triggered by the ingestion of wheat gliadin and related prolamins from other cereals, such as barley and rye. Immunity against these cereal-derived proteins is mediated by pro-inflammatory cytokines produced by both innate and adaptive system response in individuals unable to adequately digest them. Peptides generated in this condition are absorbed across the gut barrier, which in these patients is characterized by the deregulation of its permeability. Here, we discuss a possible correlation between CD and Autistic Spectrum Disorder (ASD) pathogenesis. ASD can be induced by an excessive and inappropriate brain opioid activity during the neon…

The Role of Fc Receptors on the Effectiveness of Therapeutic Monoclonal Antibodies.

2021

Since the approval of the first monoclonal antibody (mAb) in 1986, a huge effort has been made to guarantee safety and efficacy of therapeutic mAbs. As of July 2021, 118 mAbs are approved for the European market for a broad range of clinical indications. In order to ensure clinical efficacy and safety aspects, (pre-)clinical experimental approaches evaluate the respective modes of action (MoA). In addition to antigen-specificity including binding affinity and -avidity, MoA comprise Fc-mediated effector functions such as antibody dependent cellular cytotoxicity (ADCC) and the closely related antibody dependent cellular phagocytosis (ADCP). For this reason, a variety of cell-based assays have…

Case-specific performance of MM-PBSA, MM-GBSA, and SIE in virtual screening.

2015

In drug discovery the reliable prediction of binding free energies is of crucial importance. Methods that combine molecular mechanics force fields with continuum solvent models have become popular because of their high accuracy and relatively good computational efficiency. In this research we studied the performance of molecular mechanics generalized Born surface area (MM-GBSA), molecular mechanics Poisson-Boltzmann surface area (MM-PBSA), and solvated interaction energy (SIE) both in their virtual screening efficiency and their ability to predict experimentally determined binding affinities for five different protein targets. The protein-ligand complexes were derived with two different app…

Suitability of MMGBSA for the selection of correct ligand binding modes from docking results

2019

The estimation of the correct binding mode and affinity of a ligand into a target protein using computational methods is challenging. However, docking can introduce poses from which the correct binding mode could be identified using other methods. Here, we analyzed the reliability of binding energy estimation using the molecular mechanics‐generalized Born surface area (MMGBSA) method without and with energy minimization to identify the likely ligand binding modes within docking results. MMGBSA workflow (a) outperformed docking in recognizing the correct binding modes of androgen receptor ligands and (b) improved the correlation coefficient of computational and experimental results of rescor…

Modelo predictivo de mortalidad a largo plazo en el trasplante hepático del adulto

2015

El trasplante hepático es el tratamiento de elección de muchas hepatopatías terminales y un procedimiento que ha ido evolucionando desde sus inicios, mejorando sus resultados con el paso del tiempo. A pesar de que nuestro país es uno de los que presentan las tasas de donación más altas del mundo, debido al incremento en el número de indicaciones para la realización de un trasplante hepático, porcentaje de pacientes que fallecen en lista de espera se cifra en torno al 5 %. Por ello se continúa investigando y buscando modelos predictivos y de asignación de injertos a fin de mejorar la eficiencia global del procedimiento. En nuestro trabajo planteamos como objetivo el desarrollo de un modelo p…

Effects of cannabinoids on spontaneous mechanical activity of mouse ileal longitudinal muscle.

2007

Proprioceptive response strength in the primary sensorimotor cortex is invariant to the range of finger movement

2023

Available online 13 February 2023 Proprioception is the sense of body position and movement that relies on afference from the proprioceptors in muscles and joints. Proprioceptive responses in the primary sensorimotor (SM1) cortex can be elicited by stim- ulating the proprioceptors using evoked (passive) limb movements. In magnetoencephalography (MEG), propri- oceptive processing can be quantified by recording the movement evoked fields (MEFs) and movement-induced beta power modulations or by computing corticokinematic coherence (CKC) between the limb kinematics and cortical activity. We examined whether cortical proprioceptive processing quantified with MEF peak strength, relative beta supp…

A dynamic multiple receptor conformations (MD-MRC) approach to enhance early enrichment in virtual screening. A case study on PPAR-alpha

2016

POSTURE AND POSTUROLOGY, ANATOMICAL AND PHYSIOLOGICAL PROFILES: OVERVIEW AND CURRENT STATE OF ART

2017

Background and aim of work: posture is the position of the body in the space, and is controlled by a set of anatomical structures. The maintenance and the control of posture are a set of interactions between muscle-skeletal, visual, vestibular, and skin system. Lately there are numerous studies that correlate the muscle-skeletal and the maintenance of posture. In particular, the correction of defects and obstruction of temporomandibular disorders, seem to have an impoact on posture. The aim of this work is to collect information in literature on posture and the influence of the stomatognatich system on postural system. Methods: Comparison of the literature on posture and posturology by cons…

Myostatin/activin blocking combined with exercise reconditions skeletal muscle expression profile of mdx mice

2015

Duchenne Muscular Dystrophy is characterized by muscle wasting and decreased aerobic metabolism. Exercise and blocking of myostatin/activin signaling may independently or combined counteract muscle wasting and dystrophies. The effects of myostatin/activin blocking using soluble activin receptor-Fc (sActRIIB-Fc) administration and wheel running were tested alone or in combination for seven weeks in dystrophic mdx mice. Expression microarray analysis revealed decreased aerobic metabolism in the gastrocnemius muscle of mdx mice compared to healthy mice. This was not due to reduced home-cage physical activity, and was further downregulated upon sActRIIB-Fc treatment in enlarged muscles. However…