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Current Protocols in Pharmacology

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https://www.readbyqxmd.com/read/30325112/murine-models-of-pancreatitis-leading-to-the-development-of-pancreatic-cancer
#1
Ana S Leal, Karen T Liby
Chronic or repeated episodes of acute pancreatic inflammation, or pancreatitis, are risk factors for the development of pancreatic cancer. Pancreatic cancer is characterized by a strong fibro-inflammatory tumor microenvironment. In pancreatitis, the same fibro-inflammatory reaction is observed concurrently with a loss of normal pancreatic cells. Mouse models are commonly employed to study the progression of pancreatitis and pancreatic cancer, with genetic and pharmacological tools used to elucidate cellular and acellular interactions within pancreatic tumors...
October 16, 2018: Current Protocols in Pharmacology
https://www.readbyqxmd.com/read/30204297/modeling-chronic-graft-versus-host-disease-in-mice-using-allogeneic-bone-marrow-and-splenocyte-transfer
#2
Mark A Schroeder, Kidist Ashami, Karl Staser
This unit describes a method for allogeneic bone marrow and splenocyte transfer for the modeling of chronic graft versus host disease (cGVHD) in mice. Preclinical models provide clinically relevant platforms for mechanistic and therapeutic studies that may inform the treatment of patients suffering from cGVHD, a common and potentially severe complication of allogeneic hematopoietic stem cell transplantation (alloHSCT). Most murine models of cGVHD depend on the transfer of major histocompatibility complex (MHC)-mismatched bone marrow and whole splenocytes (or purified T cells) into an irradiated recipient...
September 11, 2018: Current Protocols in Pharmacology
https://www.readbyqxmd.com/read/30179315/the-irwin-test-and-functional-observational-battery-fob-for-assessing-the-effects-of-compounds-on-behavior-physiology-and-safety-pharmacology-in-rodents
#3
Joanne R Mathiasen, Virginia C Moser
The modified Irwin procedure or functional observational battery (FOB) can be used to achieve several goals. New chemical entities (NCEs) can be behaviorally screened for nervous system effects at a variety of doses to identify potential therapeutic uses and in the selection of appropriate doses for subsequent assays. NCEs can also be evaluated in the behavioral battery and compared with reference standards to assess liabilities in a new compound class, with an estimated therapeutic index being suggested by the doses used in comparison to therapeutic doses...
September 4, 2018: Current Protocols in Pharmacology
https://www.readbyqxmd.com/read/30168909/overview-of-transporters-in-pharmacokinetics-and-drug-discovery
#4
Yan Zhang
Transporters play important roles in absorption, distribution, metabolism, and elimination (ADME) processes, as well as drug pharmacokinetics (PK) and pharmacodynamics (PD). They are also important in maintaining the homeostasis of endogenous compounds and nutrients in the body. Increasing evidences also suggest that they are important in mediating drug-drug interactions (DDIs). While the significance of transporters in drug pharmacodynamics and DDIs are beyond the scope of this overview, the basic concepts of transporters, their contributions in membrane permeation processes, and their roles in influencing drug ADME pathway and PK will be discussed...
September 2018: Current Protocols in Pharmacology
https://www.readbyqxmd.com/read/30168908/screening-strategies-for-the-discovery-of-ion-channel-monoclonal-antibodies
#5
Caroline S Colley, Elizabeth England, John E Linley, Trevor C I Wilkinson
Ion channels play crucial roles in physiology by modulation of cellular functions that include electrical excitability, secretion, cell migration, and gene transcription. They are an important target class for drug discovery and have historically been targeted using small molecule approaches. A significant opportunity exists to target these channels with antibodies and alternative forms of biologics. Antibodies display high specificity, selectivity, and affinity for their target antigen, thus having the potential to target ion channels very precisely...
September 2018: Current Protocols in Pharmacology
https://www.readbyqxmd.com/read/30152172/protocols-for-measuring-glutamate-uptake-dose-response-and-kinetic-assays-in-in-vitro-and-ex-vivo-systems
#6
Andréia C K Fontana
This article presents detailed descriptions of procedures and troubleshooting tips for basic in vitro and ex vivo uptake assays for the functional characterization of glutamate transporters and the assessment of the effect of compounds that modulate their activity. Assays are performed in cell lines that transiently or stably express a particular transporter under investigation, in primary cultures of astrocytes, or in ex vivo synaptosomal preparations that endogenously express these transporters. Two main assays are described, including dose-response assays to measure potencies of test compounds for stimulation or inhibition of function (EC50 or IC50 values, respectively) and kinetic functional assays to calculate apparent affinity (KM ) and maximal velocity (Vmax ) of radiolabeled substrate uptake into the cells...
September 2018: Current Protocols in Pharmacology
https://www.readbyqxmd.com/read/30129249/utilizing-miniature-fluorescence-microscopy-to-image-hippocampal-place-cell-ensemble-function-in-thy1-gcamp6f-transgenic-mice
#7
Tim Indersmitten, Tamara Berdyyeva, Leah Aluisio, Timothy Lovenberg, Pascal Bonaventure, Ryan M Wyatt
Imaging neuronal activity in awake behaving mice with miniature fluorescence microscopes requires the implementation of a variety of procedures. Surgeries are performed to gain access to the cell population of interest and to implant microscope components. After a recovery period, mice are trained to exhibit a desired behavior. Finally, neuronal activity is imaged and synchronized with that behavior. To take full advantage of the technology, selection of the calcium indicator and experimental design must be carefully considered...
September 2018: Current Protocols in Pharmacology
https://www.readbyqxmd.com/read/29927084/reagent-validation-to-facilitate-experimental-reproducibility
#8
Michael Williams
Many results reported in the biomedical research literature cannot be independently reproduced, undermining the basic foundations of science. This overview is intended for researchers who are committed to improving the quality and integrity of biomedical science by raising awareness of both the sources of irreproducibility, and activities specifically targeted to address the issue. The irreproducibility of biomedical research is due to a variety of factors, known and unknown, that markedly influence experimental outcomes...
June 2018: Current Protocols in Pharmacology
https://www.readbyqxmd.com/read/29927081/overview-of-genetically-engineered-mouse-models-of-prostate-cancer-and-their-applications-in-drug-discovery
#9
Gianluca Civenni, Giuseppina M Carbone, Carlo V Catapano
Prostate cancer (PCa) is the most common malignant visceral neoplasm in males in Western countries. Despite progress made in the early treatment of localized malignancies, there remains a need for therapies effective against advanced forms of the disease. Genetically engineered mouse (GEM) models are valuable tools for addressing this issue, particularly in defining the cellular and molecular mechanisms responsible for tumor initiation and progression. While cell and tissue culture systems are important models for this purpose as well, they cannot recapitulate the complex interactions within heterotypic cells and the tumor microenvironment that are crucial in the initiation and progression of prostate tumors...
June 2018: Current Protocols in Pharmacology
https://www.readbyqxmd.com/read/29927074/reconstitution-and-electrophysiological-characterization-of-ion-channels-in-lipid-bilayers
#10
Dan A Klaerke, Maria de Los Angeles Tejada, Vibeke Grøsfjeld Christensen, Mette Lassen, Per Amstrup Pedersen, Kirstine Calloe
Detergent-solubilized purified ion channels can be reconstituted into lipid bilayers for electrophysiological analysis. Traditionally, ion channels were inserted into vesicles and subsequently fused with planar "black lipid membranes" formed from lipids dissolved in a hydrophobic solvent such as decane. Provided in this article is a step-by-step guide to reconstitute purified ion channel proteins into giant unilamellar vesicles (GUVs). This procedure results in the formation of proteoliposomes that can be used for planar bilayer formation and electrophysiological characterization of single-channel currents...
June 2018: Current Protocols in Pharmacology
https://www.readbyqxmd.com/read/29927058/measuring-histone-deacetylase-inhibition-in-the-brain
#11
Doodipala Samba Reddy, Xin Wu, Victoria M Golub, W Mohaiza Dashwood, Roderick H Dashwood
Histone deacetylases (HDACs) represent a family of enzymes that are targets for epigenetic modulation of genomic activity and may be beneficial in the treatment of many diseases, including cancer and central nervous system disorders. In animal models, HDAC inhibitors have neuroprotective, antiepileptogenic, and antidepressant effects. Assaying HDAC activity provides a robust method for identifying HDAC inhibitors and for assessing their effects under various physiological conditions or after pathological insults...
June 2018: Current Protocols in Pharmacology
https://www.readbyqxmd.com/read/30040217/quantitative-intracerebral-microdialysis-studies-to-determine-unbound-extracellular-fluid-drug-concentrations-in-discrete-areas-of-the-brain
#12
Matthew R Durk
Intracerebral microdialysis is a powerful technique for quantifying unbound brain extracellular fluid concentrations of drugs and drug candidates over time in live, conscious, freely moving animals. The results provide crucial information on the brain penetrance of the administered agent. This unit details the surgical procedures, study planning and execution, and data analysis required for a brain microdialysis study following intravenous infusion of a test substance to steady state. The accumulated data makes possible the determination of the area under the concentration-time curve ratio and steady-state concentration ratio for unbound compound in rat brain extracellular fluid as compared to that in plasma (Kpu,u )...
March 2018: Current Protocols in Pharmacology
https://www.readbyqxmd.com/read/30040212/three-decades-of-chloride-intracellular-channel-proteins-from-organelle-to-organ-physiology
#13
Shubha Gururaja Rao, Devasena Ponnalagu, Neel J Patel, Harpreet Singh
Intracellular organelles are membranous structures central for maintaining cellular physiology and the overall health of the cell. To maintain cellular function, intracellular organelles are required to tightly regulate their ionic homeostasis. Any imbalance in ionic concentrations can disrupt energy production (mitochondria), protein degradation (lysosomes), DNA replication (nucleus), or cellular signaling (endoplasmic reticulum). Ionic homeostasis is also important for volume regulation of intracellular organelles and is maintained by cation and anion channels as well as transporters...
March 2018: Current Protocols in Pharmacology
https://www.readbyqxmd.com/read/30040205/binding-assays-for-bromodomain-proteins-their-utility-in-drug-discovery-in-oncology-and-inflammatory-disease
#14
Nina I Zolotarjova, Richard Wynn
Bromodomains are protein domains that recognize acetylated lysine residues and are important for recruiting a large number of protein and multiprotein complexes to sites of lysine acetylation. They play an important role in chromatin biology and are popular targets for drug discovery. Compound screening in this area requires the use of biochemical assays to assess the binding potency of potential drug candidates. Foremost among the efforts to target bromodomains are those aimed at identifying compounds that interact with the bromodomain and extra-terminal domain (BET) family of bromodomain-containing proteins (BRD2, BRD3, BRD4, and BRDT)...
March 2018: Current Protocols in Pharmacology
https://www.readbyqxmd.com/read/30040204/in-vitro-enzyme-assays-for-jmjc-domain-containing-lysine-histone-demethylases-jmjc-kdms
#15
Hanna Tarhonskaya, Anthony Tumber, Akane Kawamura, Christopher J Schofield
Histone modifications, including lysine methylation marks on histone tails, modulate the accessibility of genes for transcription. Changes in histone tail methylation patterns can cause transcriptional activation or repression. The dynamic regulation of lysine methylation patterns is enabled by two distinct groups of enzymes: histone methyltransferases (KMTs) and demethylases (KDMs). The Jumonji C (JmjC) domain-containing lysine histone demethylases (JmjC-KDMs) alter the methylation levels of histone tails by removing tri-, di-, or mono-methylation marks...
March 2018: Current Protocols in Pharmacology
https://www.readbyqxmd.com/read/29261229/in-vitro-histone-acetylation-assay
#16
James A L Brown
Acetylation is a core cellular process involved in maintaining genomic integrity, gene regulation, and metabolism. Histone acetyltransferases (HATs) are an enzyme family that regulates these processes by catalyzing the transfer of an acetyl moiety onto target proteins. Perturbations of cellular acetylation profiles have been associated with a variety of disease states, including cancer. Changes in acetylation profiles can be achieved by mechanisms associated with acetyltransferases, such as gene down-regulation or alterations in the activity of key acetyltransferase enzymes...
December 20, 2017: Current Protocols in Pharmacology
https://www.readbyqxmd.com/read/29261228/overview-of-monoamine-transporters
#17
REVIEW
Shaili Aggarwal, Ole V Mortensen
The dopamine (DAT), serotonin (SERT), and norepinephrine (NET) transporters, which are collectively referred to as monoamine transporters (MATs), play significant roles in regulating the neuronal response to these neurotransmitters. MATs terminate the action of these neurotransmitters by translocating them from the synaptic space into the presynaptic neurons. These three transmitters are responsible for controlling a number of physiological, emotional, and behavioral functions, with their transporters being the site of action of drugs employed for the treatment of a variety of conditions, including depression, anxiety, ADHD, schizophrenia, and psychostimulant abuse...
December 20, 2017: Current Protocols in Pharmacology
https://www.readbyqxmd.com/read/29261227/overview-of-microrna-modulation-in-analgesic-research
#18
REVIEW
Sujay Ramanathan, Botros B Shenoda, Seena K Ajit
MicroRNA(miRNA)-mediated gene regulation underlies cellular processes, playing an important role in homeostasis and diseases. The expression and function of miRNAs are altered by various pharmacological agents, with differences in the endogenous levels of miRNAs influencing drug efficacy and toxicity. Thus, miRNA levels could be a biomarker for predicting treatment response, efficacy, and safety. In addition, elucidating the mechanistic significance of miRNA alterations can aid in the identification of therapeutic targets and patient selection, and guide personalized therapy...
December 20, 2017: Current Protocols in Pharmacology
https://www.readbyqxmd.com/read/29261226/in-vitro-assays-for-the-functional-characterization-of-the-dopamine-transporter-dat
#19
Shaili Aggarwal, Ole V Mortensen
Detailed in this unit are protocols for studying the in vitro uptake of dopamine (DA) as a means for defining the functional characteristics of dopamine transporters. All assays are performed using commercially available cell lines that transiently express the transporter under investigation. The three main assays provided are: a kinetic assay to calculate the affinity (KM ) and maximal velocity (Vmax ) of radiolabeled DA uptake into cells; concentration-response assays to measure the potencies (IC50 /Ki values) of test compounds as transport inhibitors; and an efflux assay to assess the ability and potency (EC50 ) of a ligand to elicit reverse transport of DA accumulated in the cell...
December 20, 2017: Current Protocols in Pharmacology
https://www.readbyqxmd.com/read/29261225/in-vitro-validation-of-mirna-mediated-gene-expression-linked-to-drug-metabolism
#20
Botros B Shenoda, Sujay Ramanathan, Seena K Ajit
Pharmacogenomic approaches used to investigate how genes affect drug responses are critical for designing personalized therapies aimed at maximizing efficacy and minimizing adverse effects. Drug efficacy is often dependent on the sequence and expression levels of drug target genes or those involved in the metabolism and transport of the therapeutic agent. Expression of these genes, in turn, is negatively regulated by small noncoding miRNAs. The levels of miRNAs in bodily fluids have been studied extensively as potential diagnostic and prognostic biomarkers...
December 20, 2017: Current Protocols in Pharmacology
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