Skip to main content

DEtermination of Orphan Receptor PHysiological Agonists and sigNals

Searching for OpenAIRE data...

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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
DOI: 10.1101/839597