CELLOPT: improved unit‐cell parameters for electron diffraction data of small‐molecule crystals

Authors: Gruene, Tim, Clabbers, Max T. B., Luebben, Jens, Chin, Jia Min, Reithofer, Michael R., Stowasser, Frank, Alker, André M.

Source: Journal of applied crystallography. 55(3):647-655

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100153830981.0x000001&indx=1&recIds=ETOCvdc_100153830981.0x000001

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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Copper Coordination Chemistry of Sulfur Pendant Cyclen Derivatives: An Attempt to Hinder the Reductive-Induced Demetalation in 64/67Cu Radiopharmaceuticals

Authors: Tosato, Marianna, Tiezza, Marco Dalla, May, Nóra V., Isse, Abdirisak Ahmed, Nardella, Sonia, Orian, Laura, Verona, Marco, Vaccarin, Christian, Alker, André, Mäcke, Helmut

Source: Inorganic chemistry. 60(15):11530-11547

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Modulation of Pharmacologically Relevant Properties of Piperidine Derivatives by Functional Groups in an Equatorial or Axial β‐Position to the Amino Group

Authors: Schnider, Patrick, Dolente, Cosimo, Stalder, Henri, Martin, Rainer E., Reinmüller, Viktoria, Marty, Roman, Wyss Gramberg, Caroline, Wagner, Björn, Fischer, Holger, Alker, André M., Müller, Klaus

Source: Chembiochem. 21(1-2):212-234

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RG7774 (Vicasinabin), an orally bioavailable cannabinoid receptor 2 (CB2R) agonist, decreases retinal vascular permeability, leukocyte adhesion, and ocular inflammation in animal models.

Authors: Grether, Uwe, Foxton, Richard H., Gruener, Sabine, Korn, Claudia, Kimbara, Atsushi, Osterwald, Anja, Zirwes, Elisabeth, Uhles, Sabine, Thoele, Janina, Colé, Nadine, Rogers-Evans, Mark, Röver, Stephan, Nettekoven, Matthias, Martin, Rainer E., Adam, Jean-Michel, Fingerle, Jürgen, Bissantz, Caterina, Guba, Wolfgang, Alker, André, Szczesniak, Anna M.

Source: Frontiers in Pharmacology; 2024, p1-20, 20p

Subject Terms: ANIMAL models of inflammation, CANNABINOID receptors, EYE inflammation, RETINAL diseases, DIABETIC retinopathy, THERAPEUTICS, CHO cell, RETROLENTAL fibroplasia

Ligand channel in pharmacologically stabilized rhodopsin

Authors: Mattle, Daniel, Kuhn, Bernd, Aebi, Johannes, Bedoucha, Marc, Kekilli, Demet, Grozinger, Nathalie, Alker, Andre, Rudolph, Markus G., Schmid, Georg, Schertler, Gebhard F. X., Hennig, Michael, Standfuss, Jörg, Dawson, Roger J. P.

Source: Proceedings of the National Academy of Sciences of the United States of America, 2018 Apr 01. 115(14), 3640-3645.

Access URL: https://www.jstor.org/stable/26508399

Tuning the Framework of Thioether-Functionalized Polyazamacrocycles: Searching for a Chelator for Theranostic Silver Radioisotopes.

Authors: Tosato, Marianna, Franchi, Sara, Dalla Tiezza, Marco, Orian, Laura, Gyr, Thomas, Alker, André, Zanoni, Giordano, Pastore, Paolo, Andrighetto, Alberto, Köster, Ulli, Jensen, Mikael, Mäcke, Helmut, Asti, Mattia, Di Marco, Valerio

Source: Inorganic Chemistry; 12/18/2023, Vol. 62 Issue 50, p20777-20790, 14p

Is Smaller Better? Cu²⁺/Cu⁺ Coordination Chemistry and Copper-64 Radiochemical Investigation of a 1,4,7-Triazacyclononane-Based Sulfur-Rich Chelator.

Authors: Tosato, Marianna, Franchi, Sara, Isse, Abdirisak Ahmed, Del Vecchio, Alessandro, Zanoni, Giordano, Alker, André, Asti, Mattia, Gyr, Thomas, Di Marco, Valerio, Mäcke, Helmut

Source: Inorganic Chemistry; 12/18/2023, Vol. 62 Issue 50, p20621-20633, 13p

Is Smaller Better? Cu2+/Cu+Coordination Chemistry and Copper-64 Radiochemical Investigation of a 1,4,7-Triazacyclononane-Based Sulfur-Rich Chelator

Authors: Tosato, Marianna, Franchi, Sara, Isse, Abdirisak Ahmed, Del Vecchio, Alessandro, Zanoni, Giordano, Alker, André, Asti, Mattia, Gyr, Thomas, Di Marco, Valerio, Mäcke, Helmut

Source: Inorganic Chemistry; December 2023, Vol. 62 Issue: 50 p20621-20633, 13p

2′-Deoxy-4′-azido Nucleoside Analogs Are Highly Potent Inhibitors of Hepatitis C Virus Replication Despite the Lack of 2′-α-Hydroxyl Groups

Authors: Klumpp, Klaus, Kalayanov, Genadiy, Ma, Han, Le Pogam, Sophie, Leveque, Vincent, Jiang, Wen-Rong, Inocencio, Nicole, De Witte, Anniek, Rajyaguru, Sonal, Tai, Ezra, Chanda, Sushmita, Irwin, Michael R., Sund, Christian, Winqist, Anna, Maltseva, Tatiana, Eriksson, Staffan, Usova, Elena, Smith, Mark, Alker, Andre, Najera, Isabel, Cammack, Nick, Martin, Joseph A., Johansson, Nils Gunnar, Smith, David B.

Source: In Journal of Biological Chemistry 25 January 2008 283(4):2167-2175

Is adamantane a suitable substituent to pre-organize the acid orientation in E-selectin antagonists?

Authors: Titz, Alexander, Patton, John, Alker, André M., Porro, Michele, Schwardt, Oliver, Hennig, Michael, Francotte, Eric, Magnani, John, Ernst, Beat

Source: In Bioorganic & Medicinal Chemistry 2008 16(2):1046-1056

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New short access to pyrrolo[2,3-c]pyridazin-6-ones via β-spirolactams

Authors: Stoll, Theodor, Alker, André, Kolczewski, Sabine, Menzi, Andrea, Revil-Baudard, Vincent

Source: In Tetrahedron Letters 4 February 2015 56(6):772-774

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Ring opening of cyclic sulfamidates with bromophenyl metal reagents: complementarity of sulfamidates and aziridines

Authors: Hebeisen, Paul, Weiss, Urs, Alker, André, Staempfli, Andreas

Source: In Tetrahedron Letters 12 October 2011 52(41):5229-5233

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Piperidinyl-nicotinamides as potent and selective somatostatin receptor subtype 5 antagonists

Authors: Alker, André, Binggeli, Alfred, Christ, Andreas D., Green, Luke, Maerki, Hans Peter, Martin, Rainer E., Mohr, Peter

Source: In Bioorganic & Medicinal Chemistry Letters 1 August 2010 20(15):4521-4525

Discovery of potent, balanced and orally active dual NK1/NK3 receptor ligands

Authors: Peters, Jens-Uwe, Hoffmann, Torsten, Schnider, Patrick, Stadler, Heinz, Koblet, Andreas, Alker, André, Poli, Sonia Maria, Ballard, Theresa M., Spooren, Will, Steward, Lucinda, Sleight, Andrew J.

Source: In Bioorganic & Medicinal Chemistry Letters 1 June 2010 20(11):3405-3408

Benzoxazole piperidines as selective and potent somatostatin receptor subtype 5 antagonists

Authors: Martin, Rainer E., Mohr, Peter, Maerki, Hans Peter, Guba, Wolfgang, Kuratli, Christoph, Gavelle, Olivier, Binggeli, Alfred, Bendels, Stefanie, Alvarez-Sánchez, Rubén, Alker, André, Polonchuk, Liudmila, Christ, Andreas D.

Source: In Bioorganic & Medicinal Chemistry Letters 2009 19(21):6106-6113