Choose an application

• Reference Manager
• EndNote
• RefWorks (Direct export to RefWorks)

G protein-coupled receptors (GPCRs) are integral membrane proteins forming the fourth largest superfamily in the human genome. Many of these receptors play key physiological roles and several pathologies have been associated with receptor functional abnormalities. GPCRs therefore represent important goals for drug design in pharmaceutical companies since they constitute the target of about one third of the drugs currently on the market. However, endogenous GPCRs are most often difficult to study because of a lack of tools to target them specifically and single out their response to physiological or drug-elicited stimulations. Hence, studies mostly focused on recombinant receptors expressed in a variety of cellular models that do not always closely reflect the receptor natural environment and often deal with levels of expression exceeding by far physiological ranges. Recent technological developments combining for example genetically modified animals and advanced imaging approaches have improved our ability to visualize endogenous GPCRs. To date, trailing receptor activation, subsequent intracellular redistribution, changes in signaling cascade up to integrated response to a drug-elicited stimulation is at hand though the impact of a physiological challenge on receptor dynamics remains a major issue. Data however suggest that the receptor may embrace a different fate depending on the type of stimulation in particular if sustained or repeated. This suggests that current drugs may only partially mimic the genuine response of the receptor and may explain, at least in part, their secondary effects. Commonalities and specificities between physiological and drug-induced activation can thus represent valuable guidelines for the design of future drugs.

opioid receptors --- G protein coupled receptors --- CGamP mice --- FLIM --- fluorescent knock-in mice --- receptor heteromerization --- Endogenous receptors --- cannabinoid receptors --- biased signaling --- Opiate tolerance

Choose an application

• Reference Manager
• EndNote
• RefWorks (Direct export to RefWorks)

The interest in opioids such as morphine, the prototypical opioid ligand, has been maintained through the years. The identification of endogenous opioids and their receptors (mu, delta, kappa, and nociceptin), molecular cloning, and the elucidation of the crystal structures of opioid receptors represent key milestones in opioid research. The opioid system modulates numerous pharmacological responses, with therapeutic (i.e., analgesia) and detrimental side effects (i.e., addiction). The medical use and misuse of opioids have dramatically increased, leading to the 21st century opioid crisis. This book presents recent developments in opioid drug discovery, specifically in the medicinal chemistry and pharmacology of new ligands targeting the opioid receptors as effective and safe therapeutics for human diseases. Furthermore, it draws a special attention to advancing concepts and strategies in opioid drug discovery to mitigate opioid liabilities. The diversity among the discussed topics is a testimony to the complexity of the opioid system, which results from the expression, regulation, and functional role of ligands and receptors. The array of multidisciplinary research areas illustrates the rapidly developing basic research and translational activities in opioid drug discovery. This book will serve as a useful reference while also stimulating continued research in the chemistry and pharmacology of opioids and their receptors, with the prospect of developing improved therapies for human diseases, but also improving health and quality of life in general.

opioid receptors --- neurokinin-1 receptor --- peptide synthesis --- receptor binding studies --- functional assay --- writhing test --- tolerance --- Leu-enkephalin --- beta-arrestin --- mu opioid receptor --- delta opioid receptor --- biased signaling --- DADLE --- ischemia --- plasma stability --- morphinan --- BNTX --- δ opioid receptor antagonist --- 1H-NMR experiments --- mechanism elucidation --- peripheral antinociception --- 14-methoxycodeine-6-O-sulfate --- codeine-6-O-sulfate --- opioid peptides and peptidomimetics --- DAMGO --- DALDA --- [Dmt1]DALDA --- KGOP01 --- binding --- molecular docking --- structure-activity relationships --- β2-amino acids --- β2-Homo-amino acids --- µ-opioid receptor --- opioid peptides --- TAPP --- racemic synthesis of β2-amino acids --- peripheral µ-opioid receptors --- analgesia --- peripheral analgesic tolerance --- dysbiosis --- opioid --- bifunctional ligands --- (−)-N-phenethylnorhydromorphone analogs --- [35S]GTPgammaS assay --- forskolin-induced cAMP accumulation assays --- β-arrestin recruitment assays --- MOR and DOR agonists --- respiratory depression --- bias factor --- molecular modeling &amp --- simulation --- δ opioid receptor --- NTI derivative --- sulfonamide --- inverse agonist --- neutral antagonist --- agonist --- opioids --- mu receptor --- opioid side effects --- biased agonism --- partial agonism --- zerumbone --- chronic constriction injury (CCI) --- allodynia --- hyperalgesia --- potassium channels --- over-the-counter drugs --- misuse --- abuse --- opioid drugs --- pharmacology --- codeine --- dihydrocodeine --- loperamide --- opioid peptide --- macrocyclic tetrapeptide --- multifunctional ligands --- kappa opioid receptor --- analgesics --- opioid liabilities --- μ opioid receptor --- receptor model --- biased ligands --- dependence --- pain therapy --- neonatal opioid withdrawal syndrome --- naltrexone --- 6β-naltrexol --- buprenorphine --- G-protein bias --- arrestin recruitment --- respiration --- mitragynine --- heteromer --- internalization --- primary hippocampal culture --- lysosomes --- µ opioid receptor --- molecular dynamics --- docking --- interaction fingerprints --- biased agonists --- SR-17018 --- PZM21 --- morphine --- fentanyl --- diphenethylamines --- design and synthesis --- structure–activity relationships --- partial agonist --- biased agonist --- antagonist --- binding affinity --- selectivity --- n/a

Choose an application

• Reference Manager
• EndNote
• RefWorks (Direct export to RefWorks)

Positron emission tomography (PET) and single-photon emission computed tomography (SPECT) are in vivo molecular imaging methods which are widely used in nuclear medicine for diagnosis and treatment follow-up of many major diseases. These methods use target-specific molecules as probes, which are labeled with radionuclides of short half-lives that are synthesized prior to the imaging studies. These probes are called radiopharmaceuticals. The use of PET and SPECT for brain imaging is of special significance since the brain controls all the body’s functions by processing information from the whole body and the outside world. It is the source of thoughts, intelligence, memory, speech, creativity, emotion, sensory functions, motion control, and other important body functions. Protected by the skull and the blood–brain barrier, the brain is somehow a privileged organ with regard to nutrient supply, immune response, and accessibility for diagnostic and therapeutic measures. Invasive procedures are rather limited for the latter purposes. Therefore, noninvasive imaging with PET and SPECT has gained high importance for a great variety of brain diseases, including neurodegenerative diseases, motor dysfunctions, stroke, epilepsy, psychiatric diseases, and brain tumors. This Special Issue focuses on radiolabeled molecules that are used for these purposes, with special emphasis on neurodegenerative diseases and brain tumors.

SV2A --- SV2B --- SV2C --- microPET --- [18F]UCB-H --- epilepsy --- PBIF --- distribution volume --- blocking assay --- preclinical imaging --- Alzheimer’s disease (AD) --- network measure --- graph theory --- brain network --- positron emission tomography (PET) --- persistent homology --- Phosphodiesterase 2A (PDE2A) --- Positron Emission Tomography (PET) --- Benzoimidazotriazine (BIT) --- fluorinated --- Mouse Liver Microsomes (MLM) --- cyclic nucleotide phosphodiesterase --- PDE2A radioligand --- nitro-precursor --- fluorine-18 --- in vitro autoradiography --- PET imaging --- opioid receptors --- positron emission tomography --- radiotracers --- μOR-, δOR-, κOR- and ORL1-ligands --- movement disorders --- pain --- drug dependence --- GBM --- biomarkers --- Sigma 1 --- Sigma 2 --- PD-L1 --- PARP --- IDH --- Alzheimer’s disease --- Parkinson’s disease --- β-amyloid plaques --- neurofibrillary tangles --- α-synucleinopathy --- diagnostic imaging probes --- orexin receptors --- PET --- radiotracer --- imaging --- alpha 7 --- nicotinic acetylcholine receptors --- nAChR --- autoradiography --- amino acid --- FET --- FACBC --- FDOPA --- immunoPET --- molecular imaging --- glioma --- brain metastases --- adenosine A2A receptor --- rotenone-based mouse model --- [18F]FESCH --- two-step one-pot radiosynthesis

Choose an application

• Reference Manager
• EndNote
• RefWorks (Direct export to RefWorks)

Aquaculture is an important economic activity for food production all around the world that has experienced an exponential growth during the last few decades. However, several weaknesses and bottlenecks still need to be addressed in order to improve the aquaculture productive system. The recent fast development of the omics technologies has provided scientists with meaningful tools to elucidate the molecular basis of their research interests. This reprint compiles different works about the use of transcriptomics and genomics technologies in different aspects of the aquaculture research, such as immunity, stress response, development, sexual dimorphism, among others, in a variety of fish and shellfish, and even in turtles. Different transcriptome (mRNAs and non-coding RNAs (ncRNAs)), genome (Single Nucleotide Polymorphisms (SNPs)), and metatranscriptome analyses were conducted to unravel those different aspects of interest.

Research & information: general --- Biology, life sciences --- Fisheries & related industries --- RNA-Seq --- lncRNAs --- Dicentrarchus labrax --- viral infection --- nodavirus --- immune response --- fish --- T lymphocytes --- infection --- malnutrition --- inflammation --- aquaculture --- histopathology --- immunohistochemistry --- enteromyxosis --- Philasterides dicentrarchi --- turbot --- transcriptomics --- Chinese mitten crab --- Eriocheir sinensis --- transportome --- transporters --- salinity --- osmoregulation --- transcriptome --- meta-analysis --- gills --- short pentraxins --- c-reactive protein --- zebrafish --- transcript expression --- antiviral --- SVCV --- rag1 mutants --- skin --- mucosal immunity --- hypoxia --- hypo-metabolic state --- growth --- swimming performance --- metabolic landmarks --- muscle transcriptome --- glycolysis --- lipid metabolism --- protein turnover --- gilthead sea bream --- hepatopancreas necrosis disease --- metatranscriptomics sequencing --- hepatopancreatic flora --- teleost --- B cells --- single cell transcriptomics --- immunoglobulins --- immune markers --- transcription factors --- long non-coding RNAs --- hepatic transcript expression --- salmon --- microarray --- omega-6/omega-3 ratio --- nutrigenomics --- fatty acids --- liver --- muscle --- Misgurnus anguillicaudatus --- sexual size dimorphism --- polyploid size dimorphism --- comparative transcriptome --- gene expression --- edible red sea urchin --- Loxechinus albus --- RNA-seq --- reference transcriptome --- Chinese soft-shelled turtle --- Aeromonas hydrophila --- hemorrhagic sepsis --- molecular immunopathogenesis --- tripartite motif proteins --- B30.2 domain --- antiviral immunity --- Ctenopharyngodon idella --- grass carp reovirus --- metamorphosis --- brain --- RNA --- sequencing --- intermuscular bone --- development --- Megalobrama amblycephala --- Oreochromis niloticus --- histological structure --- Atlantic salmon --- smoltification --- genome --- mRNAs --- miRNAs --- sox family genes --- Pelodiscus sinensis --- estradiol --- pseudo-female --- sex-related --- heterosis --- heterobeltiosis --- environment --- transgressive genes --- conserved miRNA --- high-throughput sequencing --- lumpfish --- novel miRNA --- RT-qPCR --- heat shock protein --- co-chaperon network --- salinity-alkalinity adaptation --- molecular evolution --- Lateolabrax maculatus --- genomics --- stress response --- HPI-axis --- neuroendocrine-immune interaction --- common carp --- poly-unsaturated fatty acid --- fatty acid elongase --- association study --- genomic selection --- bulked segregant analysis --- SNP --- association analysis --- joint effect --- seawater adaptation --- microRNAs --- small-RNA sequencing --- microarray transcriptome --- European seabass --- chronic inflammation --- opioid receptors --- immune status --- whole-transcriptome sequencing --- sex differentiation --- non-coding RNAs --- ceRNA --- red cusk-eel --- thermal stress --- liver transcriptome --- oxidative damage --- protein folding --- hepatic enzymes --- n/a