Search results for "Receptor"

Prediction of properties of chiral compounds by molecular topology

1998

Abstract A common assumption in chemistry is that chiral behavior is associated with 3-D geometry. However, chiral information is related to symmetry, which allows the topological handling of chiral atoms by weighted graphs and the calculation of new descriptors that give a weight to the corresponding entry in the main diagonal of the topological matrix. In this study, it is demonstrated that, operating in this way, chiral topological indices are obtained that can differentiate the pharmacological activity between pairs of enantiomers. The 50% inhibitory concentration (IC50) values of the D2 dopamine receptor and the σ receptor for a group of 3-hydroxy phenyl piperidines are specifically pr…

Receptor-mediated uptake of boron-rich neuropeptide y analogues for boron neutron capture therapy.

2014

Peptidic ligands selectively targeting distinct G protein-coupled receptors that are highly expressed in tumor tissue represent a promising approach in drug delivery. Receptor-preferring analogues of neuropeptide Y (NPY) bind and activate the human Y1 receptor subtype (hY1 receptor), which is found in 90% of breast cancer tissue and in all breast-cancer-derived metastases. Herein, novel highly boron-loaded Y1 -receptor-preferring peptide analogues are described as smart shuttle systems for carbaboranes as (10) B-containing moieties. Various positions in the peptide were screened for their susceptibility to carbaborane modification, and the most promising positions were chosen to create a mu…

CO2 Fixation by Copper(II) Complexes of a Terpyridinophane Aza Receptor

2004

CO2 is fixed by a Cu2+ complex of a macrocyclic terpyridinophane ligand forming a carbamate group. Several features of the structure mimic the enzyme rubisco.

Biodistribution of Insulin-Nanogels in Mouse: A Preliminary Study for the Treatment of Alzheimer's Disease

2017

A growing body of evidence shows that Insulin, Insulin Receptor (IR) and IR signaling are involved in brain cognitive functions and their dysfunction is implicated in Alzheimer's disease (AD) neurodegeneration. Thus, administration of insulin could be a strategy for AD treatment. For this aim we have designed, synthesized and characterized a nanogel system (NG) that has been conjugated to insulin molecules (NG-In) to deliver the protein into the brain, as a tool for the development of a new therapy against AD. In our preclinical study in mice, intraperitoneal injection of fluorescent-labeled NG has allowed to determine the biodistribution of NG vs time in the whole body and its clearance th…

Magnetofection of acoustically active „magnetic microspheres“ (Magnetobubbles) — Induction of angiogenesis via non-viral transfection of VEGF

2009

Adenoviral transduction of the VEGF gene in an oversized skin flap increases flap survival and perfusion. In this study we investigated the potential of magnetofection of magnetic lipospheres containing VEGF165-cDNA on survival and perfusion of ischemic skin flaps and evaluated the method with respect to the significance of applied magnetic field and ultrasound.

The Fundamental Role of Melanocortins in Brain Processes

2003

The discoveries of the latest ten years have shed new light in understanding the roles of melanocortins and their receptors in brain functions and in the development of different pathologies. Since 1992 when genes encoded melanocortin receptor five subtypes were identified, cloned and characterized, the molecular mechanisms underlying different effects such as skin darkening, behaviour, food intake, anti-inflammatory action, analgesia have been clarified. The contribution of melanocortins and their receptors in the physiological control of organism homeostasis has become as the background for the search of agonists and antagonists of separate receptor subtypes, that can be targeted to the m…

DEVELOPMENT AND QUALIFICATION OF BIOANALYTICAL METHODS FOR DEAMIDATED IFNβ-1a AND INVESTIGATION ABOUT THE MECHANISM OF ACTION

2021

Interferon beta-1a (IFNβ-1a) is a recombinant IFNβ with the tradename Rebif involved in several biological activities. Recently, it has been reported that artificial deamidation of IFNb-1a increases its biological response. Given the therapeutical potential, an investigation on the deamidated variant has been carried out via different approaches to discover the mechanism underlying this biological effect. The antiviral and immunomodulatory activity of deamidated cytokine was assessed using two precise and accurate cell-based assays. As expected, deamidated IFNβ-1a showed an increase in the biological response and its canonical pathway and receptor binding affinity were thorough analysed. De…

Intranasal Insulin Administration to Prevent Delayed Neurocognitive Recovery and Postoperative Neurocognitive Disorder: A Narrative Review

2021

Delayed neurocognitive recovery and postoperative neurocognitive disorders are major complications of surgery, hospitalization, and anesthesia that are receiving increasing attention. Their incidence is reported to be 10–80% after cardiac surgery and 10–26% after non-cardiac surgery. Some of the risk factors include advanced age, level of education, history of diabetes mellitus, malnutrition, perioperative hyperglycemia, depth of anesthesia, blood pressure fluctuation during surgery, chronic respiratory diseases, etc. Scientific evidence suggests a causal association between anesthesia and delayed neurocognitive recovery or postoperative neurocognitive disorders, and various pathophysiologi…

Ion pair recognition by ditopic crown ether based bis-urea and uranyl salophen receptors

2016

Variation in the TonB-dependent outer-membrane proteins in plant-associated strains of Pseudomonas fluorescens

2011

International audience; Genomic sequences of ten strains of plant-associated Pseudomonas spp. were surveyed for the presence of TonB-dependent outer-membrane proteins (TBDPs), which function in the uptake of substrates from the environment by many Gram-negative bacteria. The ten strains represent P. fluorescens, P. chlororaphis, and P. synxantha isolated from the phyllosphere, rhizosphere or soil. 14 to 45 TBDPs were identified in each strain, and phylogenetic analysis of the TBDPs identified five that are conserved across all ten genomes. Comparisons to proteins with known functions allowed the assignment of putative roles in uptake of heme, vitamin B12, copper, and the siderophore ferrich…