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DEtermination of Orphan Receptor PHysiological Agonists and sigNals

CORDIS provides links to public deliverables and publications of HORIZON projects.

Links to deliverables and publications from FP7 projects, as well as links to some specific result types such as dataset and software, are dynamically retrieved from OpenAIRE .

Publications

Structural insight to mutation effects uncover a common allosteric site in class C GPCRs

Author(s): Kasper Harpsøe, Michael W. Boesgaard, Christian Munk, Hans Bräuner-Osborne, David E. Gloriam
Published in: Bioinformatics, 2016, Page(s) btw784, ISSN 1367-4803
Publisher: Oxford University Press
DOI: 10.1093/bioinformatics/btw784

The GPR139 reference agonists 1a and 7c, and tryptophan and phenylalanine share a common binding site

Author(s): Anne Cathrine Nøhr, Willem Jespers, Mohamed A. Shehata, Leonard Floryan, Vignir Isberg, Kirsten Bayer Andersen, Johan Åqvist, Hugo Gutiérrez-de-Terán, Hans Bräuner-Osborne, David E. Gloriam
Published in: Scientific Reports, Issue 7/1, 2017, ISSN 2045-2322
Publisher: Nature Publishing Group
DOI: 10.1038/s41598-017-01049-z

GPCRdb: the G protein-coupled receptor database - an introduction

Author(s): C Munk, V Isberg, S Mordalski, K Harpsøe, K Rataj, A S Hauser, P Kolb, A J Bojarski, G Vriend, D E Gloriam
Published in: British Journal of Pharmacology, Issue 173/14, 2016, Page(s) 2195-2207, ISSN 0007-1188
Publisher: Wiley-Blackwell
DOI: 10.1111/bph.13509

Selective Negative Allosteric Modulation Of Metabotropic Glutamate Receptors – A Structural Perspective of Ligands and Mutants

Author(s): Kasper Harpsøe, Vignir Isberg, Benjamin G. Tehan, Dahlia Weiss, Angela Arsova, Fiona H. Marshall, Hans Bräuner-Osborne, David E. Gloriam
Published in: Scientific Reports, Issue 5/1, 2015, ISSN 2045-2322
Publisher: Nature Publishing Group
DOI: 10.1038/srep13869

Selectivity determinants of GPCR–G-protein binding

Author(s): Tilman Flock, Alexander S. Hauser, Nadia Lund, David E. Gloriam, Santhanam Balaji, M. Madan Babu
Published in: Nature, Issue 545/7654, 2017, Page(s) 317-322, ISSN 0028-0836
Publisher: Nature Publishing Group
DOI: 10.1038/nature22070

Trends in GPCR drug discovery: new agents, targets and indications

Author(s): Alexander S. Hauser, Misty M. Attwood, Mathias Rask-Andersen, Helgi B. Schiöth, David E. Gloriam
Published in: Nature Reviews Drug Discovery, Issue 16/12, 2017, Page(s) 829-842, ISSN 1474-1776
Publisher: Nature Publishing Group
DOI: 10.1038/nrd.2017.178

Pharmacogenomics of GPCR Drug Targets

Author(s): Alexander S. Hauser, Sreenivas Chavali, Ikuo Masuho, Leonie J. Jahn, Kirill A. Martemyanov, David E. Gloriam, M. Madan Babu
Published in: Cell, Issue 172/1-2, 2018, Page(s) 41-54.e19, ISSN 0092-8674
Publisher: Cell Press
DOI: 10.1016/j.cell.2017.11.033

GPCRdb in 2018: adding GPCR structure models and ligands

Author(s): Gáspár Pándy-Szekeres, Christian Munk, Tsonko M Tsonkov, Stefan Mordalski, Kasper Harpsøe, Alexander S Hauser, Andrzej J Bojarski, David E Gloriam
Published in: Nucleic Acids Research, Issue 46/D1, 2017, Page(s) D440-D446, ISSN 0305-1048
Publisher: Oxford University Press
DOI: 10.1093/nar/gkx1109

GPCRdb: an information system for G protein-coupled receptors

Author(s): Vignir Isberg, Stefan Mordalski, Christian Munk, Krzysztof Rataj, Kasper Harpsøe, Alexander S. Hauser, Bas Vroling, Andrzej J. Bojarski, Gert Vriend, David E. Gloriam
Published in: Nucleic Acids Research, Issue 44/D1, 2016, Page(s) D356-D364, ISSN 0305-1048
Publisher: Oxford University Press
DOI: 10.1093/nar/gkv1178

Novel Agonist Bioisosteres and Common Structure-Activity Relationships for The Orphan G Protein-Coupled Receptor GPR139

Author(s): Shehata MA, Nøhr AC, Lissa D, Bisig C, Isberg V, Andersen KB, Harpsøe K, Björkling F, Bräuner-Osborne H, Gloriam DE
Published in: Scientific Reports, 2016, ISSN 2045-2322
Publisher: Nature Publishing Group
DOI: 10.1038/srep36681

The orphan G protein-coupled receptor GPR139 is activated by the peptides: Adrenocorticotropic hormone (ACTH), α-, and β-melanocyte stimulating hormone (α-MSH, and β-MSH), and the conserved core motif HFRW

Author(s): Anne Cathrine Nøhr, Mohamed A. Shehata, Alexander S. Hauser, Vignir Isberg, Jacek Mokrosinski, I. Sadaf Farooqi, Daniel Sejer Pedersen, David E. Gloriam, Hans Bräuner-Osborne
Published in: Neurochemistry International, 2016, ISSN 0197-0186
Publisher: Elsevier BV
DOI: 10.1016/j.neuint.2016.11.012

Total synthesis and structure–activity relationship studies of a series of selective G protein inhibitors

Author(s): Xiao-Feng Xiong, Hang Zhang, Christina R. Underwood, Kasper Harpsøe, Thomas J. Gardella, Mie F. Wöldike, Michael Mannstadt, David E. Gloriam, Hans Bräuner-Osborne, Kristian Strømgaard
Published in: Nature Chemistry, Issue 8/11, 2016, Page(s) 1035-1041, ISSN 1755-4330
Publisher: Nature Publishing Group
DOI: 10.1038/nchem.2577

Receptor selectivity between the G proteins Gα 12 and Gα 13 is defined by a single leucine-to-isoleucine variation

Author(s): Amanda E. Mackenzie, Tezz Quon, Li-Chiung Lin, Alexander S. Hauser, Laura Jenkins, Asuka Inoue, Andrew B. Tobin, David E. Gloriam, Brian D. Hudson, Graeme Milligan
Published in: The FASEB Journal, Issue 33/4, 2019, Page(s) 5005-5017, ISSN 0892-6638
Publisher: Federation of American Societies for Experimental Biology
DOI: 10.1096/fj.201801956r

Discovery of Human Signaling Systems: Pairing Peptides to G Protein-Coupled Receptors

Author(s): Simon R. Foster, Alexander S. Hauser, Line Vedel, Ryan T. Strachan, Xi-Ping Huang, Ariana C. Gavin, Sushrut D. Shah, Ajay P. Nayak, Linda M. Haugaard-Kedström, Raymond B. Penn, Bryan L. Roth, Hans Bräuner-Osborne, David E. Gloriam
Published in: Cell, Issue 179/4, 2019, Page(s) 895-908.e21, ISSN 0092-8674
Publisher: Cell Press
DOI: 10.1016/j.cell.2019.10.010

Identification of a novel scaffold for a small molecule GPR139 receptor agonist

Author(s): Anne Cathrine Nøhr, Mohamed A. Shehata, Daniel Palmer, Rina Pokhrel, Maria Vallianou, Simon R. Foster, Patrick R. Gentry, David E. Gloriam, Hans Bräuner-Osborne
Published in: Scientific Reports, Issue 9/1, 2019, ISSN 2045-2322
Publisher: Nature Publishing Group
DOI: 10.1038/s41598-019-40085-9

Pharmacology and function of the orphan GPR139 G protein‐coupled receptor

Author(s): Line Vedel, Anne Cathrine Nøhr, David E. Gloriam, Hans Bräuner‐Osborne
Published in: Basic & Clinical Pharmacology & Toxicology, 2019, ISSN 1742-7835
Publisher: Nordic Pharmacological Society
DOI: 10.1111/bcpt.13263

An online resource for GPCR structure determination and analysis

Author(s): Christian Munk, Eshita Mutt, Vignir Isberg, Louise F. Nikolajsen, Janne M. Bibbe, Tilman Flock, Michael A. Hanson, Raymond C. Stevens, Xavier Deupi, David E. Gloriam
Published in: Nature Methods, Issue 16/2, 2019, Page(s) 151-162, ISSN 1548-7091
Publisher: Nature Publishing Group
DOI: 10.1038/s41592-018-0302-x

Novel approaches leading towards peptide GPCR de‐orphanisation

Author(s): Alexander S. Hauser, David E. Gloriam, Hans Bräuner‐Osborne, Simon R. Foster
Published in: British Journal of Pharmacology, Issue 177/5, 2020, Page(s) 961-968, ISSN 0007-1188
Publisher: Wiley-Blackwell
DOI: 10.1111/bph.14950

Discovery of a new class of orthosteric antagonists with nanomolar potency at extrasynaptic GABAA receptors

Author(s): Christina Birkedahl Falk-Petersen, Tsonko M. Tsonkov, Malene Sofie Nielsen, Kasper Harpsøe, Christoffer Bundgaard, Bente Frølund, Uffe Kristiansen, David E. Gloriam, Petrine Wellendorph
Published in: Scientific Reports, Issue 10/1, 2020, ISSN 2045-2322
Publisher: Nature Publishing Group
DOI: 10.1038/s41598-020-66821-0

GPCRmd uncovers the dynamics of the 3D-GPCRome

Author(s): Rodríguez-Espigares I, Torrens-Fontanals M, Tiemann JK, Aranda-García D, Ramírez-Anguita JM, Stepniewski TM, Worp N, Varela-Rial A, Morales-Pastor A, Lacruz BM, Gaspar Pándy-Szekeres, Mayol E, Giorgino T, Carlsson J, Deupi X, Filipek S, Filizola M, Gómez-Tamayo JC, Gonzalez A, Gutierrez-de-Teran H, Jimenez M, Jespers W, Kapla J, Khelashvili G, Kolb P, Latek D, Marti-Solano M, Matricon P, Mats
Published in: Nature Methods, 2020, ISSN 1548-7091
Publisher: Nature Publishing Group
DOI: 10.1101/839597

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