Kinetic analysis of endogenous β2‐adrenoceptor‐mediated cAMP GloSensor™ responses in HEK293 cells

Authors: Cullum, Sean A., Veprintsev, Dmitry B., Hill, Stephen J.

Source: British journal of pharmacology. 180(10):1304-1315

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Detection of cannabinoid receptor type 2 in native cells and zebrafish with a highly potent, cell-permeable fluorescent probeElectronic supplementary information (ESI) available: Supplementary figures and tables; general synthetic methods; compound synthesis and characterization; molecular docking; in vitro pharmacology; fluorescence spectroscopy; TR-FRET kinetic CB2R binding assay; FACS analysis; time-lapse confocal imaging; in vivo zebrafish imaging; NMR spectra; and N-terminal SNAP-hCB2R sequence. CCDC 1923120. For ESI and crystallographic data in CIF or other electronic format see DOI: 10.1039/d1sc06659e

Authors: Gazzi, Thais, Brennecke, Benjamin, Atz, Kenneth, Korn, Claudia, Sykes, David, Forn-Cuni, Gabriel, Pfaff, Patrick, Sarott, Roman C., Westphal, Matthias V., Mostinski, Yelena, Mach, Leonard, Wasinska-Kalwa, Malgorzata, Weise, Marie, Hoare, Bradley L., Miljuš, Tamara, Mexi, Maira, Roth, Nicolas, Koers, Eline J., Guba, Wolfgang, Alker, André, Rufer, Arne C., Kusznir, Eric A., Huber, Sylwia, Raposo, Catarina, Zirwes, Elisabeth A., Osterwald, Anja, Pavlovic, Anto, Moes, Svenja, Beck, Jennifer, Nettekoven, Matthias, Benito-Cuesta, Irene, Grande, Teresa, Drawnel, Faye, Widmer, Gabriella, Holzer, Daniela, van der Wel, Tom, Mandhair, Harpreet, Honer, Michael, Fingerle, Jürgen, Scheffel, Jörg, Broichhagen, Johannes, Gawrisch, Klaus, Romero, Julián, Hillard, Cecilia J., Varga, Zoltan V., van der Stelt, Mario, Pacher, Pal, Gertsch, Jürg, Ullmer, Christoph, McCormick, Peter J., Oddi, Sergio, Spaink, Herman P., Maccarrone, Mauro, Veprintsev, Dmitry B., Carreira, Erick M., Grether, Uwe, Nazaré, Marc

Source: Chemical science. 13(19):5539-5545

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Michaelis-Menten Quantification of Ligand Signaling Bias Applied to the Promiscuous Vasopressin V2 Receptor

Authors: Heydenreich, Franziska Marie ^*, Plouffe, Bianca, Rizk, Aurélien, Milić, Dalibor, Zhou, Joris, Breton, Billy, Le Gouill, Christian, Inoue, Asuka, Bouvier, Michel ^*, Veprintsev, Dmitry B. ^*

Source: In Molecular Pharmacology September 2022 102(3):139-149

A Modified Cell-Penetrating Peptide Enhances Insulin and Oxytocin Delivery across an RPMI 2650 Nasal Epithelial Cell Barrier In Vitro.

Authors: Wong, Sara, Brown, Alexander D., Abrahams, Abigail B., Nurzak, An Nisaa, Eltaher, Hoda M., Sykes, David A., Veprintsev, Dmitry B., Fone, Kevin C. F., Dixon, James E., King, Madeleine V.

Source: Pharmaceutics; Oct2024, Vol. 16 Issue 10, p1267, 16p

Subject Terms: CELL-penetrating peptides, EPITHELIAL cell culture, PEPTIDES, CYTOTOXINS, OXYTOCIN, BIOAVAILABILITY

Kinetic analysis of endogenous β2‐adrenoceptor‐mediated cAMP GloSensor™ responses in HEK293 cells.

Authors: Cullum, Sean A.^1,2 (AUTHOR), Veprintsev, Dmitry B.^1,2 (AUTHOR), Hill, Stephen J.^1,2 (AUTHOR) stephen.hill@nottingham.ac.uk

Source: British Journal of Pharmacology. May2023, Vol. 180 Issue 10, p1304-1315. 12p. 3 Charts, 7 Graphs.

Subject Terms: *BIOSENSORS, *ALBUTEROL, *BISOPROLOL

GPCR Solubilization and Quality Control

Authors: Miljus, Tamara, Sykes, David A., Harwood, Clare R., Vuckovic, Ziva, Veprintsev, Dmitry B.

Source: Methods in molecular biology. 2127:105-128

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Molecular recognition of an odorant by the murine trace amine-associated receptor TAAR7f.

Authors: Gusach, Anastasiia, Lee, Yang, Khoshgrudi, Armin Nikpour, Mukhaleva, Elizaveta, Ma, Ning, Koers, Eline J., Chen, Qingchao, Edwards, Patricia C., Huang, Fanglu, Kim, Jonathan, Mancia, Filippo, Veprintsev, Dmitry B., Vaidehi, Nagarajan, Weyand, Simone N., Tate, Christopher G.

Source: Nature Communications; 8/30/2024, Vol. 15 Issue 1, p1-12, 12p

Subject Terms: CELL receptors, OLFACTORY receptors, G protein coupled receptors, BINDING sites, CHARGE-charge interactions

Highly Selective Drug-Derived Fluorescent Probes for the Cannabinoid Receptor Type 1 (CB1R).

Authors: Mach, Leonard, Omran, Anahid, Bouma, Jara, Radetzki, Silke, Sykes, David A., Guba, Wolfgang, Li, Xiaoting, Höffelmeyer, Calvin, Hentsch, Axel, Gazzi, Thais, Mostinski, Yelena, Wasinska-Kalwa, Malgorzata, de Molnier, Fabio, van der Horst, Cas, von Kries, Jens Peter, Vendrell, Marc, Hua, Tian, Veprintsev, Dmitry B., Heitman, Laura H., Grether, Uwe

Source: Journal of Medicinal Chemistry; 7/25/2024, Vol. 67 Issue 14, p11841-11867, 27p

Proteins of the S100 Family Regulate the Oligomerization of p53 Tumor Suppressor

Authors: Fernandez-Fernandez, Maria Rosario, Veprintsev, Dmitry B., Fersht, Alan R.

Source: Proceedings of the National Academy of Sciences of the United States of America, 2005 Mar . 102(13), 4735-4740.

Access URL: https://www.jstor.org/stable/3375119

Combined docking and machine learning identify key molecular determinants of ligand pharmacological activity on β2 adrenoceptor

Authors: Jiménez‐Rosés, Mireia, Morgan, Bradley Angus, Jimenez Sigstad, Maria, Tran, Thuy Duong Zoe, Srivastava, Rohini, Bunsuz, Asuman, Borrega‐Román, Leire, Hompluem, Pattarin, Cullum, Sean A., Harwood, Clare R., Koers, Eline J., Sykes, David A., Styles, Iain B., Veprintsev, Dmitry B.

Source: Pharmacology research & perspectives. 10(5)

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Exploring the kinetic selectivity of drugs targeting the β1‐adrenoceptor

Authors: Sykes, David A., Jiménez‐Rosés, Mireia, Reilly, John, Fairhurst, Robin A., Charlton, Steven J., Veprintsev, Dmitry B.

Source: Pharmacology research & perspectives. 10(4)

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100155657861.0x000001&indx=1&recIds=ETOCvdc_100155657861.0x000001

CRINEPT-TROSY NMR Reveals p53 Core Domain Bound in an Unfolded form to the Chaperone Hsp90

Authors: Rüdiger, Stefan, Veprintsev, Dmitry B., Fersht, Alan R.

Source: Proceedings of the National Academy of Sciences of the United States of America, 2002 Aug . 99(17), 11085-11090.

Access URL: https://www.jstor.org/stable/3059526

A Peptide That Binds and Stabilizes p53 Core Domain: Chaperone Strategy for Rescue of Oncogenic Mutants

Authors: Friedler, Assaf, Hansson, Lars O., Veprintsev, Dmitry B., Rippin, Thomas M., Nikolova, Penka V., Proctor, Mark R., Rüdiger, Stefan, Fersht, Alan R.

Source: Proceedings of the National Academy of Sciences of the United States of America, 2002 Jan . 99(2), 937-942.

Access URL: https://www.jstor.org/stable/3057669

Ligand-Independent Assembly of Recombinant Human CD1 by Using Oxidative Refolding Chromatography

Authors: Altamirano, Myriam M., Woolfson, Adrian, Donda, Alena, Shamshiev, Abdijapar, Briseño-Roa, Luis, Foster, Nicholas W., Veprintsev, Dmitry B., De Libero, Gennaro, Fersht, Alan R., Milstein, César

Source: Proceedings of the National Academy of Sciences of the United States of America, 2001 Mar . 98(6), 3288-3293.

Access URL: https://www.jstor.org/stable/3055228

Flipping the GPCR Switch: Structure-Based Development of Selective Cannabinoid Receptor 2 Inverse Agonists.

Authors: Kosar, Miroslav, Sarott, Roman C., Sykes, David A., Viray, Alexander E. G., Vitale, Rosa Maria, Tomašević, Nataša, Li, Xiaoting, Ganzoni, Rudolf L. Z., Kicin, Bilal, Reichert, Lisa, Patej, Kacper J., Gómez-Bouzó, Uxía, Guba, Wolfgang, McCormick, Peter J., Hua, Tian, Gruber, Christian W., Veprintsev, Dmitry B., Frank, James A., Grether, Uwe, Carreira, Erick M.

Source: ACS Central Science; 5/22/2024, Vol. 10 Issue 5, p956-968, 13p

Mechano-sensitivity of β2-adrenoceptors enhances constitutive activation of cAMP generation that is inhibited by inverse agonists.

Authors: Cullum, Sean A., Platt, Simon, Dale, Natasha, Isaac, Oliver C., Wragg, Edward S., Soave, Mark, Veprintsev, Dmitry B., Woolard, Jeanette, Kilpatrick, Laura E., Hill, Stephen J.

Source: Communications Biology; 4/5/2024, Vol. 7 Issue 1, p1-16, 16p

Subject Terms: G protein coupled receptors, CELL receptors, SITE-specific mutagenesis

Native Mass Spectrometry Gives Insight into the Allosteric Binding Mechanism of M2 Pyruvate Kinase to Fructose-1, 6-Bisphosphate

Authors: Gavriilidou, Agni F. M., Holding, Finn P., Mayer, Daniel, Coyle, Joseph E., Veprintsev, Dmitry B., Zenobi, Renato

Source: Biochemistry. 57(11):1685-1689

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Insights into the Basal Activity and Activation Mechanism of the β1 Adrenergic Receptor Using Native Mass Spectrometry

Authors: Gavriilidou, Agni F. M., Hunziker, Hanna, Mayer, Daniel, Vuckovic, Ziva, Veprintsev, Dmitry B., Zenobi, Renato

Source: Journal of the American Society for Mass Spectrometry. 30(3):529-537

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100130425505.0x000001&indx=1&recIds=ETOCvdc_100130425505.0x000001

ThermoBRET: A Ligand‐Engagement Nanoscale Thermostability Assay Applied to GPCRs.

Authors: Hoare, Bradley L., Tippett, David N., Kaur, Amandeep, Cullum, Sean A., Miljuš, Tamara, Koers, Eline J., Harwood, Clare R., Dijon, Nicola, Holliday, Nicholas D., Sykes, David A., Veprintsev, Dmitry B.

Source: ChemBioChem; Jan2024, Vol. 25 Issue 2, p1-11, 11p

Hsp90-Tau Complex Reveals Molecular Basis for Specificity in Chaperone Action

Authors: Karagöz, G. Elif, Duarte, Afonso M.S., Akoury, Elias, Ippel, Hans, Biernat, Jacek, Morán Luengo, Tania, Radli, Martina, Didenko, Tatiana, Nordhues, Bryce A., Veprintsev, Dmitry B., Dickey, Chad A., Mandelkow, Eckhard, Zweckstetter, Markus, Boelens, Rolf, Madl, Tobias, Rüdiger, Stefan G.D.

Source: In Cell 27 February 2014 156(5):963-974