Adenosine receptors as drug targets—what are the challenges?
JF Chen, HK Eltzschig, BB Fredholm - Nature reviews Drug discovery, 2013 - nature.com
Adenosine signalling has long been a target for drug development, with adenosine itself or
its derivatives being used clinically since the 1940s. In addition, methylxanthines such as …
its derivatives being used clinically since the 1940s. In addition, methylxanthines such as …
Endothelin
The endothelins comprise three structurally similar 21-amino acid peptides. Endothelin-1
and-2 activate two G-protein coupled receptors, ETA and ETB, with equal affinity, whereas …
and-2 activate two G-protein coupled receptors, ETA and ETB, with equal affinity, whereas …
G protein–coupled receptor oligomerization revisited: functional and pharmacological perspectives
Most evidence indicates that, as for family CG protein–coupled receptors (GPCRs), family A
GPCRs form homo-and heteromers. Homodimers seem to be a predominant species, with …
GPCRs form homo-and heteromers. Homodimers seem to be a predominant species, with …
The IUPHAR/BPS Guide to PHARMACOLOGY: an expert-driven knowledgebase of drug targets and their ligands
AJ Pawson, JL Sharman, HE Benson… - Nucleic acids …, 2014 - academic.oup.com
Abstract The International Union of Basic and Clinical Pharmacology/British
Pharmacological Society (IUPHAR/BPS) Guide to PHARMACOLOGY (http://www …
Pharmacological Society (IUPHAR/BPS) Guide to PHARMACOLOGY (http://www …
International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and classification of adenosine receptors—an update
BB Fredholm, AP IJzerman, KA Jacobson… - Pharmacological …, 2011 - ASPET
In the 10 years since our previous International Union of Basic and Clinical Pharmacology
report on the nomenclature and classification of adenosine receptors, no developments …
report on the nomenclature and classification of adenosine receptors, no developments …
The Concise Guide to PHARMACOLOGY 2013/14: G protein‐coupled receptors
SPH Alexander, HE Benson… - British journal of …, 2013 - Wiley Online Library
Abstract The Concise Guide to PHARMACOLOGY 2013/14 provides concise overviews of
the key properties of over 2000 human drug targets with their pharmacology, plus links to an …
the key properties of over 2000 human drug targets with their pharmacology, plus links to an …
Single-molecule analysis of fluorescently labeled G-protein–coupled receptors reveals complexes with distinct dynamics and organization
D Calebiro, F Rieken, J Wagner… - Proceedings of the …, 2013 - National Acad Sciences
G-protein–coupled receptors (GPCRs) constitute the largest family of receptors and major
pharmacological targets. Whereas many GPCRs have been shown to form di-/oligomers, the …
pharmacological targets. Whereas many GPCRs have been shown to form di-/oligomers, the …
International Union of Pharmacology. LXX. Subtypes of γ-aminobutyric acidA receptors: classification on the basis of subunit composition, pharmacology, and function …
RW Olsen, W Sieghart - Pharmacological reviews, 2008 - ASPET
In this review we attempt to summarize experimental evidence on the existence of defined
native GABAA receptor subtypes and to produce a list of receptors that actually seem to exist …
native GABAA receptor subtypes and to produce a list of receptors that actually seem to exist …
Fluorescence/bioluminescence resonance energy transfer techniques to study G-protein-coupled receptor activation and signaling
MJ Lohse, S Nuber, C Hoffmann - Pharmacological reviews, 2012 - ASPET
Fluorescence and bioluminescence resonance energy transfer (FRET and BRET)
techniques allow the sensitive monitoring of distances between two labels at the nanometer …
techniques allow the sensitive monitoring of distances between two labels at the nanometer …
G protein–coupled receptor heteromers
G protein–coupled receptors (GPCRs) compose one of the largest families of membrane
proteins involved in intracellular signaling. They are involved in numerous physiological and …
proteins involved in intracellular signaling. They are involved in numerous physiological and …