Search Results - "LEURS, ROB"

International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors by Panula, Pertti, Chazot, Paul L, Cowart, Marlon, Gutzmer, Ralf, Leurs, Rob, Liu, Wai L S, Stark, Holger, Thurmond, Robin L, Haas, Helmut L

“…Histamine is a developmentally highly conserved autacoid found in most vertebrate tissues. Its physiological functions are mediated by four 7-transmembrane G…”
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The Landscape of Atypical and Eukaryotic Protein Kinases by Kanev, Georgi K., de Graaf, Chris, de Esch, Iwan J.P., Leurs, Rob, Würdinger, Thomas, Westerman, Bart A., Kooistra, Albert J.

“…Kinases are attractive anticancer targets due to their central role in the growth, survival, and therapy resistance of tumor cells. This review explores the…”
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The clinical pharmacology of non-sedating antihistamines by Yanai, Kazuhiko, Yoshikawa, Takeo, Yanai, Ai, Nakamura, Tadaho, Iida, Tomomitsu, Leurs, Rob, Tashiro, Manabu

“…We previously reported on brain H receptor occupancy measurements of antihistamines in human brain using [ C]doxepin and positron emission tomography (PET). We…”
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KLIFS: A Knowledge-Based Structural Database To Navigate Kinase–Ligand Interaction Space by van Linden, Oscar P. J., Kooistra, Albert J., Leurs, Rob, de Esch, Iwan J. P., de Graaf, Chris

“…Protein kinases regulate the majority of signal transduction pathways in cells and have become important targets for the development of designer drugs. We…”
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Structural Optimization of BIPPO Analogs as Potent Antimalarials by Zheng, Yang, Matheeussen, An, Maes, Louis, Caljon, Guy, Sterk, Geert Jan, Leurs, Rob

“…Malaria continues to pose a significant health threat, causing thousands of deaths each year. The limited availability of vaccines and medications, combined…”
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KLIFS: a structural kinase-ligand interaction database by Kooistra, Albert J, Kanev, Georgi K, van Linden, Oscar P J, Leurs, Rob, de Esch, Iwan J P, de Graaf, Chris

“…Protein kinases play a crucial role in cell signaling and are important drug targets in several therapeutic areas. The KLIFS database contains detailed…”
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Kinetics for Drug Discovery: an industry-driven effort to target drug residence time by Schuetz, Doris A., de Witte, Wilhelmus Egbertus Arnout, Wong, Yin Cheong, Knasmueller, Bernhard, Richter, Lars, Kokh, Daria B., Sadiq, S. Kashif, Bosma, Reggie, Nederpelt, Indira, Heitman, Laura H., Segala, Elena, Amaral, Marta, Guo, Dong, Andres, Dorothee, Georgi, Victoria, Stoddart, Leigh A., Hill, Steve, Cooke, Robert M., De Graaf, Chris, Leurs, Rob, Frech, Matthias, Wade, Rebecca C., de Lange, Elizabeth Cunera Maria, IJzerman, Adriaan P., Müller-Fahrnow, Anke, Ecker, Gerhard F.

“…•A public–private partnership targets drug-binding kinetics in a multilevel approach.•New experimental approaches for measuring drug residence time are…”
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Structural basis of ligand recognition and design of antihistamines targeting histamine H4 receptor by Xia, Ruixue, Shi, Shuang, Xu, Zhenmei, Vischer, Henry F., Windhorst, Albert D., Qian, Yu, Duan, Yaning, Liang, Jiale, Chen, Kai, Zhang, Anqi, Guo, Changyou, Leurs, Rob, He, Yuanzheng

“…The histamine H 4 receptor (H 4 R) plays key role in immune cell function and is a highly valued target for treating allergic and inflammatory diseases…”
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Multiplex Detection of Fluorescent Chemokine Binding to CXC Chemokine Receptors by NanoBRET by Adamska, Justyna M, Leftheriotis, Spyridon, Bosma, Reggie, Vischer, Henry F, Leurs, Rob

“…NanoLuc-mediated bioluminescence resonance energy transfer (NanoBRET) has gained popularity for its ability to homogenously measure ligand binding to G…”
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A NanoBRET-Based H3R Conformational Biosensor to Study Real-Time H3 Receptor Pharmacology in Cell Membranes and Living Cells by Ma, Xiaoyuan, Gao, Meichun, Vischer, Henry F., Leurs, Rob

“…Conformational biosensors to monitor the activation state of G protein-coupled receptors are a useful addition to the molecular pharmacology assay toolbox to…”
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Synthesis and Pharmacological Characterization of New Photocaged Agonists for Histamine H3 and H4 Receptors by Zheng, Yang, Gao, Meichun, Wijtmans, Maikel, Vischer, Henry F., Leurs, Rob

“…The modulation of biological processes with light-sensitive chemical probes promises precise temporal and spatial control. Yet, the design and synthesis of…”
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BRET-Based Biosensors to Measure Agonist Efficacies in Histamine H1 Receptor-Mediated G Protein Activation, Signaling and Interactions with GRKs and β-Arrestins by Verweij, Eléonore W. E., Bosma, Reggie, Gao, Meichun, van den Bor, Jelle, Al Araaj, Betty, de Munnik, Sabrina M., Ma, Xiaoyuan, Leurs, Rob, Vischer, Henry F.

“…The histamine H1 receptor (H1R) is a G protein-coupled receptor (GPCR) and plays a key role in allergic reactions upon activation by histamine which is locally…”
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CXCR4 nanobodies (VHH-based single variable domains) potently inhibit chemotaxis and HIV-1 replication and mobilize stem cells by Jähnichen, Sven, Blanchetot, Christophe, Maussang, David, Gonzalez-Pajuelo, Maria, Chow, Ken Y., Bosch, Leontien, De Vrieze, Sindi, Serruys, Benedikte, Ulrichts, Hans, Vandevelde, Wesly, Saunders, Michael, De Haard, Hans J., Schols, Dominique, Leurs, Rob, Vanlandschoot, Peter, Verrips, Theo, Smit, Martine J., Wells, James A.

“…The important family of G protein-coupled receptors has so far not been targeted very successfully with conventional monodonal antibodies. Here we report the…”
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Development of novel fluorescent histamine H1-receptor antagonists to study ligand-binding kinetics in living cells by Stoddart, Leigh A., Vernall, Andrea J., Bouzo-Lorenzo, Monica, Bosma, Reggie, Kooistra, Albert J., de Graaf, Chris, Vischer, Henry F., Leurs, Rob, Briddon, Stephen J., Kellam, Barrie, Hill, Stephen J.

“…The histamine H 1 -receptor (H 1 R) is an important mediator of allergy and inflammation. H 1 R antagonists have particular clinical utility in allergic…”
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The constitutive activity of the virally encoded chemokine receptor US28 accelerates glioblastoma growth by Heukers, Raimond, Fan, Tian Shu, de Wit, Raymond H., van Senten, Jeffrey R., De Groof, Timo W. M., Bebelman, Maarten P., Lagerweij, Tonny, Vieira, Joao, de Munnik, Sabrina M., Smits-de Vries, Laura, van Offenbeek, Jody, Rahbar, Afsar, van Hoorick, Diane, Söderberg-Naucler, Cecilia, Würdinger, Thomas, Leurs, Rob, Siderius, Marco, Vischer, Henry F., Smit, Martine J.

“…Glioblastoma (GBM) is the most aggressive and an incurable type of brain cancer. Human cytomegalovirus (HCMV) DNA and encoded proteins, including the chemokine…”
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Analysis of Missense Variants in the Human Histamine Receptor Family Reveals Increased Constitutive Activity of E4106.30×30K Variant in the Histamine H1 Receptor by Ma, Xiaoyuan, Segura, Marta Arimont, Zarzycka, Barbara, Vischer, Henry F., Leurs, Rob

“…The Exome Aggregation Consortium has collected the protein-encoding DNA sequences of almost 61,000 unrelated humans. Analysis of this dataset for G…”
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Histamine H3 Receptor Isoforms: Insights from Alternative Splicing to Functional Complexity by Gao, Meichun, Ooms, Jasper F., Leurs, Rob, Vischer, Henry F.

“…Alternative splicing significantly enhances the diversity of the G protein-coupled receptor (GPCR) family, including the histamine H3 receptor (H3R). This…”
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Predicting the target landscape of kinase inhibitors using 3D convolutional neural networks by Kanev, Georgi K, Zhang, Yaran, Kooistra, Albert J, Bender, Andreas, Leurs, Rob, Bailey, David, Würdinger, Thomas, de Graaf, Chris, de Esch, Iwan J. P, Westerman, Bart A

“…Many therapies in clinical trials are based on single drug-single target relationships. To further extend this concept to multi-target approaches using…”
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Histamine downregulates monocyte CCL2 production through the histamine H4 receptor by Dijkstra, Dorothea, MSc, Leurs, Rob, PhD, Chazot, Paul, PhD, Shenton, Fiona C., MSc, Stark, Holger, PhD, Werfel, Thomas, MD, Gutzmer, Ralf, MD

“…Background The expression of the recently cloned histamine H4 receptor (H4 R) by leukocytes suggests a role in immunomodulation. Objective The expression and…”
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The histamine H3 receptor: from gene cloning to H3 receptor drugs by Leurs, Rob, Bakker, Remko A, Timmerman, Henk, de Esch, Iwan J P

“…Since the cloning of the histamine H(3) receptor cDNA in 1999 by Lovenberg and co-workers, this histamine receptor has gained the interest of many…”
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