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Showing 1 to 20 of 60 for “"Receptor ligands"”.
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Estrogen Receptor Ligands and Regulation of Gene Expression
Keratin13 (KRT13) and calcitonin receptor (CALCR) gene expression is differentially regulated by estradiol (E2) and the selective estrogen receptor modulators (SERMs) tamoxifen and raloxifene. KRT13 is a cytoskeleton protein while CALCR mediates the biological effects of calcitonin. These two genes …
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Modulating cell behavior with engineered HER-receptor ligands
… of cells to achieve desired responses. The HER receptor tyrosine kinase (RTK) family is an attractive target for manipulation of cues and signals, as its four members - epidermal growth factor receptor (EGFR or HERI), HER2, HER3 and HER4 - influence processes as diverse as development, wound …
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Synthesis and Evaluation of Tetrahydroprotoberberines as Dopamine Receptor Ligands
<p>Dopamine (DA) receptors belong to the G-protein coupled receptors (GPCRs) family, divided in to two groups based on their high homology transmembrane domains; D1-like DA receptors (D1, D5) and D2-like DA receptors (D2-D4). DA receptor specific ligands have been exploited as a means for studying …
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Genomic and Non-Genomic Actions of Estrogen Receptor Ligands
… estrogen are mediated by its binding to estrogen receptor proteins in target cells. In the nucleus, estrogen receptor alpha (ERalpha) and estrogen receptor beta (ERbeta) serve as ligand activated transcription factors and upon estrogen binding, they can stimulate or repress transcription of …
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5-HT3 Receptor Ligands and Their Effect on Psychomotor Stimulants
… by increasing dopamine levels. 5-HT3 serotonin receptors have been shown to indirectly affect dopamine levels. Therefore, the effect of the 5-HT3 receptor partial agonist, MD-354, on the actions of psychomotor stimulants was analyzed in mouse locomotor activity assays to determine whether MD-354 …
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Development of pharmacophore and CoMFA studies for sigma2 receptor ligands
… and CoMIFA model for sigma 2 ([sigma]_2) receptor ligands. CoMFA studies were performed for 32 bioactive [sigma]_2 receptor ligands using the radioligand [H 3] (+) DTG in the presence of pentazocine. The pharmacophore was derived using Distance Comparisons (DISCOtech) from eight partially …
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The Impact of Melanocortin Receptor Ligands on Astrocyte Signalling and Metabolism
Melanocortin peptides, which act on melanocortin receptors (MCRs), play multifaceted roles in the body through various tissues and mechanisms that regulate physiological functions. MCRs, comprising a family of five subtypes (MC1R to MC5R), are 7-transmembrane receptors that can couple with G …
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Design and Synthesis of CB1 Receptor Ligands and Synthesis of Amphibian Alkaloids
… at the development of novel CB1 cannabinoid receptor antagonists that may have clinical applications for the treatment of cannabinoid and psychostimulant addiction. In this study, we designed, synthesized, and established the CB1 affinity for the 1,5-diaryl-1,2,3- triazole esters, a series of …
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Synthesis and structure-activity relationship of a series of sigma receptor ligands
Sigma receptors are involved in several biological processes, and sigma ligands might be promising as cancer treatment agents, cocaine abuse medicines, and valuable psychiatric drugs. In an attempt to elucidate effectual structure-activity relationships, a series of N-phenylpropyl- …
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Design, Synthesis, Biological Evaluation and Metabolic Stability Studies of Sigma Receptor Ligands
Sigma receptors represent a unique family of proteins that includes two subtypes: sigma-1 and sigma-2. Sigma-1 receptors have been implicated in the behavioral and motivational effects of psychostimulants as well as in the pathophysiology of depression and Alzheimer's disease. Sigma-2 receptors are …
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Novel Core Scaffolds for the Development of Subtype Selective Estrogen Receptor Ligands
… and acyclic, in our search for subtype selective ligands. During our studies we discovered ligands containing new pharmacological profiles for estrogens. The pyrazolo[1,5-a]pyrimidine ligands provided us with two new pharmacological classes of ligands: (1) ERbeta potency selective antagonists and …
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Synthesis of Amphibian Alkaloids and Synthesis and Affinity of Novel Cannabinoid Receptor Ligands
… overall yield. The search for potent cannabinoid receptor partial agonist ligands as potential marijuana addiction therapeutic agents has led to an investigation of the synthesis of diaryl ether hybrid analogues of BAY 59-3074. A series of 2-(3-alkyl-5-hydroxyphenoxy)-6- …
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The design and synthesis of novel heterocycles as potential 5-HT receptor ligands
… , 5-HT<sub>1Dα</sub> and 5-HT<sub>1Dβ</sub> receptors have been modelled using the 3-dimensional coordinates of the seven transmembrane a-helices of the bacterial protein bacteriorhodopsin as a template. The probable 5-HT binding site was identified between helices 3, 4, 5 and 6. Interactions …
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Mechanisms of action for aryl hydrocarbon receptor ligands in the PLHC-1 cell line
Aryl hydrocarbon receptor (AHR) expression and activity was characterized in the teleost hepatoma cell line, PLHC-1. This work was carried out in order to gain insights into mechanisms of halogenated aromatic hydrocarbon (HAH) toxicity. The results improve our ability to characterize the risks …
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Pharmacological Characterization of Novel Opioid Receptor Ligands Aimed at Reducing the Development of Tolerance
The three opioid receptor subtypes, mu (mu), delta (delta) and kappa (kappa) have long been associated with analgesia. Traditional opioid analgesics exert their effects through mu receptors located in the CNS. Recent studies suggest that the development of opioid analgesics displaying dual …
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Development of pharmacophore and comfa study of rigid and flexible sigma 2 receptor ligands
… and CoMFA model was derived for sigma 2 (62) receptors by using Sybyl 7.2 Software Package. The CoMFA studies used 22 bioactive molecules as a training set and 4 molecules as a test set for the o2 receptor ligands. The geometries and electrostatic charges of all molecules were calculated using …
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Molecular modeling of sigma 1 and sigma 2 receptor ligands: pharmacophore development and comparison using discotech and bioactivity prediction comparison of ab initio and density functional comfa studies for spiro and other receptor ligands
The role of the biological receptor is currently being studied by researchers in medicine. Information about sigma receptors in particular can be gained by studying the ligands associated with each type, sigma 1 or sigma 2. Sigma 1 receptor ligands consist of drug candidates that often have …
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ALPHA4BETA2 NEURONAL NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS: FROM SUBTYPE SELECTIVE TO STOICHIOMETRIC ISOPHORM SELECTIVE PARTIAL AGONISM.
… on the study of the α4β2 nicotinic acetylcholine receptors (nAChRs). This dissertation is divided into two parts. The first part is centred on the design, synthesis, and biological evaluation of compounds selective for the orthosteric and unorthodox binding sites of the α4β2 nAChRs. In the second …
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