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Identification of key residues in transmembrane 4 responsible for the secondary, low-affinity conformation of the human 1-adrenoceptor (2014)
Journal Article
Baker, J. G., Proudman, R. G., & Hill, S. J. (2014). Identification of key residues in transmembrane 4 responsible for the secondary, low-affinity conformation of the human 1-adrenoceptor. Molecular Pharmacology, 85(5), https://doi.org/10.1124/mol.114.091587

The β1-adrenoceptor exists in two agonist conformations/states: 1) a high-affinity state where responses to catecholamines and other agonists (e.g., cimaterol) are potently inhibited by β1-adrenoceptor antagonists, and 2) a low-affinity secondary con... Read More about Identification of key residues in transmembrane 4 responsible for the secondary, low-affinity conformation of the human 1-adrenoceptor.

Structure–Activity Relationships of Privileged Structures Lead to the Discovery of Novel Biased Ligands at the Dopamine D 2Receptor (2014)
Journal Article
Szabo, M., Klein Herenbrink, C., Christopoulos, A., Lane, J. R., & Capuano, B. (2014). Structure–Activity Relationships of Privileged Structures Lead to the Discovery of Novel Biased Ligands at the Dopamine D 2Receptor. Journal of Medicinal Chemistry, 57(11), 4924-4939. https://doi.org/10.1021/jm500457x

Biased agonism at GPCRs highlights the potential for the discovery and design of pathway-selective ligands and may confer therapeutic advantages to ligands targeting the dopamine D2 receptor (D2R). We investigated the determinants of efficacy, affini... Read More about Structure–Activity Relationships of Privileged Structures Lead to the Discovery of Novel Biased Ligands at the Dopamine D 2Receptor.

Targeting S1P receptors in experimental autoimmune encephalomyelitis in mice improves early deficits in locomotor activity and increases ultrasonic vocalisations (2014)
Journal Article
Sheridan, G. K., & Dev, K. K. (2014). Targeting S1P receptors in experimental autoimmune encephalomyelitis in mice improves early deficits in locomotor activity and increases ultrasonic vocalisations. Scientific Reports, 4(1), Article 5051. https://doi.org/10.1038/srep05051

Fingolimod (FTY720) is an oral therapy for relapsing remitting multiple sclerosis (MS) and targets sphingosine 1-phosphate receptors (S1PRs). FTY720 also rescues animals from experimental autoimmune encephalomyelitis (EAE), an animal model of MS. The... Read More about Targeting S1P receptors in experimental autoimmune encephalomyelitis in mice improves early deficits in locomotor activity and increases ultrasonic vocalisations.

Recombinant Human L-Ficolin Directly Neutralizes Hepatitis C Virus Entry (2014)
Journal Article
Hamed, M. R., Brown, R. J., Zothner, C., Urbanowicz, R. A., Mason, C. P., Krarup, A., …Tarr, A. W. (2014). Recombinant Human L-Ficolin Directly Neutralizes Hepatitis C Virus Entry. Journal of Innate Immunity, 6(5), 676-684. https://doi.org/10.1159/000362209

L-ficolin is a soluble pattern recognition molecule expressed by the liver that contributes to innate immune defense against microorganisms. It is well described that binding of L-ficolin to specific pathogen-associated molecular patterns activates t... Read More about Recombinant Human L-Ficolin Directly Neutralizes Hepatitis C Virus Entry.

Population genomics reveal recent speciation and rapid evolutionary adaptation in polar bears (2014)
Journal Article
Liu, S., Lorenzen, E. D., Fumagalli, M., Li, B., Harris, K., Xiong, Z., …Wang, J. (2014). Population genomics reveal recent speciation and rapid evolutionary adaptation in polar bears. Cell, 157(4), 785-794. https://doi.org/10.1016/j.cell.2014.03.054

Polar bears are uniquely adapted to life in the High Arctic and have undergone drastic physiological changes in response to Arctic climates and a hyperlipid diet of primarily marine mammal prey. We analyzed 89 complete genomes of polar bear and brown... Read More about Population genomics reveal recent speciation and rapid evolutionary adaptation in polar bears.

Terrein Biosynthesis in Aspergillus terreus and Its Impact on Phytotoxicity (2014)
Journal Article
Zaehle, C., Gressler, M., Shelest, E., Geib, E., Hertweck, C., & Brock, M. (2014). Terrein Biosynthesis in Aspergillus terreus and Its Impact on Phytotoxicity. Cell Chemistry Biology, 21(6), 719-731. https://doi.org/10.1016/j.chembiol.2014.03.010

Terrein is a fungal metabolite with ecological, antimicrobial, antiproliferative, and antioxidative activities. Although it is produced by Aspergillus terreus as one of its major secondary metabolites, not much is known about its biosynthetic pathway... Read More about Terrein Biosynthesis in Aspergillus terreus and Its Impact on Phytotoxicity.

Genes involved in the induction of liver growth by peroxisome proliferators (2014)
Journal Article
Amer, A. H., Wall, R. J., Malla, S., Sang, F., Aboobaker, A., Avery, S. V., …Bell, D. R. (2014). Genes involved in the induction of liver growth by peroxisome proliferators. Toxicology Research, 3(5), 315-323. https://doi.org/10.1039/c3tx50110h

The mechanisms regulating the induction of hepatic DNA synthesis by PPARα agonists are currently incompletely understood, and we set out to determine whether there are different mechanisms of induction for PPARα agonists and other hepatic growth agen... Read More about Genes involved in the induction of liver growth by peroxisome proliferators.

Characterisation of the horse transcriptome from immunologically active tissues (2014)
Journal Article
Moreton, J., Malla, S., Aboobaker, A., Tarlinton, R. E., & Emes, R. D. (2014). Characterisation of the horse transcriptome from immunologically active tissues. PeerJ, 2, Article e382. https://doi.org/10.7717/peerj.382

The immune system of the horse has not been well studied, despite the fact that the horse displays several features such as sensitivity to bacterial lipopolysaccharide that make them in many ways a more suitable model of some human disorders than the... Read More about Characterisation of the horse transcriptome from immunologically active tissues.

Biased Agonism at G Protein‐Coupled Receptors: The Promise and the Challenges—A Medicinal Chemistry Perspective (2014)
Journal Article
Shonberg, J., Christopoulos, A., Lopez, L., Scammells, P. J., Capuano, B., & Lane, J. R. (2014). Biased Agonism at G Protein‐Coupled Receptors: The Promise and the Challenges—A Medicinal Chemistry Perspective. Medicinal Research Reviews, 34(6), 1286-1330. https://doi.org/10.1002/med.21318

Historically, determination of G protein‐coupled receptor (GPCR) ligand efficacy has often been restricted to identifying the ligand as an agonist or antagonist at a given signaling pathway. This classification was deemed sufficient to predict compou... Read More about Biased Agonism at G Protein‐Coupled Receptors: The Promise and the Challenges—A Medicinal Chemistry Perspective.

High throughput screening for inhibitors of the HECT ubiquitin E3 ligase ITCH identifies antidepressant drugs as regulators of autophagy (2014)
Journal Article
Amelio, I., Rossi, M., Rotblat, B., Ansell, K., Cavasotto, C. N., Caraglia, M., …Melino, G. (2014). High throughput screening for inhibitors of the HECT ubiquitin E3 ligase ITCH identifies antidepressant drugs as regulators of autophagy. Cell Death and Disease, 5(5), Article e1203. https://doi.org/10.1038/cddis.2014.113

Inhibition of distinct ubiquitin E3 ligases might represent a powerful therapeutic tool. ITCH is a HECT domain-containing E3 ligase that promotes the ubiquitylation and degradation of several proteins, including p73, p63, c-Jun, JunB, Notch and c-FLI... Read More about High throughput screening for inhibitors of the HECT ubiquitin E3 ligase ITCH identifies antidepressant drugs as regulators of autophagy.

A sequence-based approach for prediction of CsrA/RsmA targets in bacteria with experimental validation in Pseudomonas aeruginosa (2014)
Journal Article
Kulkarni, P. R., Jia, T., Kuehne, S. H., Kerkering, T. M., Morris, E. R., Searle, M. S., …Kulkarni, R. V. (in press). A sequence-based approach for prediction of CsrA/RsmA targets in bacteria with experimental validation in Pseudomonas aeruginosa. Nucleic Acids Research, 42(11), https://doi.org/10.1093/nar/gku309

CsrA/RsmA homologs are an extensive family of ribonucleic acid (RNA)-binding proteins that function as global post-transcriptional regulators controlling important cellular processes such as secondary metabolism, motility, biofilm formation and the p... Read More about A sequence-based approach for prediction of CsrA/RsmA targets in bacteria with experimental validation in Pseudomonas aeruginosa.

Epithelial mesenchymal transition in early invasive breast cancer: an immunohistochemical and reverse phase protein array study (2014)
Journal Article
Aleskandarany, M. A., Negm, O. H., Green, A. R., Ahmed, M. A. H., Nolan, C. C., Tighe, P. J., …Rakha, E. A. (2014). Epithelial mesenchymal transition in early invasive breast cancer: an immunohistochemical and reverse phase protein array study. Breast Cancer Research and Treatment, 145(2), 339-348. https://doi.org/10.1007/s10549-014-2927-5

Epithelial mesenchymal transition (EMT), as defined by loss of epithelial characteristics and gain of a mesenchymal phenotype, has been reported in vivo although the occurrence of events remains unclear. This study aims at exploration of EMT portrait... Read More about Epithelial mesenchymal transition in early invasive breast cancer: an immunohistochemical and reverse phase protein array study.

Population heterogeneity and dynamics in starter culture and lag phase adaptation of the spoilage yeast Zygosaccharomyces bailii to weak acid preservatives (2014)
Journal Article
Stratford, M., Steels, H., Nebe-von-Caron, G., Avery, S., Novodvorska, M., & Archer, D. (2014). Population heterogeneity and dynamics in starter culture and lag phase adaptation of the spoilage yeast Zygosaccharomyces bailii to weak acid preservatives. International Journal of Food Microbiology, 181, 40-47. https://doi.org/10.1016/j.ijfoodmicro.2014.04.017

The food spoilage yeast Zygosaccharomyces bailii shows great resistance to weak-acid preservatives, including sorbic acid (2, 4-hexadienoic acid). That extreme resistance was shown to be due to population heterogeneity, with a small sub-population of... Read More about Population heterogeneity and dynamics in starter culture and lag phase adaptation of the spoilage yeast Zygosaccharomyces bailii to weak acid preservatives.

Effect of a toggle switch mutation in TM6 of the human adenosine A3 receptor on Gi protein-dependent signalling and Gi-independent receptor internalization (2014)
Journal Article
Stoddart, L. A., Kellam, B., Briddon, S. J., & Hill, S. J. (2014). Effect of a toggle switch mutation in TM6 of the human adenosine A3 receptor on Gi protein-dependent signalling and Gi-independent receptor internalization. British Journal of Pharmacology, 171(16), https://doi.org/10.1111/bph.12739

Background and Purpose: The highly conserved tryptophan (W6.48) in transmembrane domain 6 of GPCRs has been shown to play a central role in forming an active conformation in response to agonist binding. We set out to characterize the effect of this m... Read More about Effect of a toggle switch mutation in TM6 of the human adenosine A3 receptor on Gi protein-dependent signalling and Gi-independent receptor internalization.

Colicin import into E. coli cells: A model system for insights into the import mechanisms of bacteriocins (2014)
Journal Article
Kim, Y. C., Tarr, A. W., & Penfold, C. N. (2014). Colicin import into E. coli cells: A model system for insights into the import mechanisms of bacteriocins. Biochimica et Biophysica Acta (BBA) - Molecular Cell Research, 1843(8), 1717-1731. https://doi.org/10.1016/j.bbamcr.2014.04.010

Bacteriocins are a diverse group of ribosomally synthesized protein antibiotics produced by most bacteria. They range from small lanthipeptides produced by lactic acid bacteria to much larger multi domain proteins of Gram negative bacteria such as th... Read More about Colicin import into E. coli cells: A model system for insights into the import mechanisms of bacteriocins.

Extracting DNA from within intact foraminiferal shells (2014)
Journal Article
Seears, H. A., & Wade, C. M. (2014). Extracting DNA from within intact foraminiferal shells. Marine Micropaleontology, 109, 46-53. https://doi.org/10.1016/j.marmicro.2014.04.001

Here we present an evaluation of several methods for extracting DNA from within intact foraminiferal shells. We tested 12 lysis buffers under carefully optimised incubation conditions, evaluating their success in terms of efficiency in evacuating cel... Read More about Extracting DNA from within intact foraminiferal shells.

Purified coronavirus spike protein nanoparticles induce coronavirus neutralizing antibodies in mice (2014)
Journal Article
Coleman, C. M., Liu, Y. V., Mu, H., Taylor, J. K., Massare, M., Flyer, D. C., …Frieman, M. B. (2014). Purified coronavirus spike protein nanoparticles induce coronavirus neutralizing antibodies in mice. Vaccine, 32(26), 3169-3174. https://doi.org/10.1016/j.vaccine.2014.04.016

Development of vaccination strategies for emerging pathogens are particularly challenging because of the sudden nature of their emergence and the long process needed for traditional vaccine development. Therefore, there is a need for development of a... Read More about Purified coronavirus spike protein nanoparticles induce coronavirus neutralizing antibodies in mice.