Hot topics in pharmacology

Recent publications of interest recommended by NC-IUPHAR

2018: Jan | Feb

February 2018

Selective Photoaffinity Probe That Enables Assessment of Cannabinoid CB2 Receptor Expression and Ligand Engagement in Human Cells
(1) Soethoudt M et al. (2018). Selective Photoaffinity Probe That Enables Assessment of Cannabinoid CB2 Receptor Expression and Ligand Engagement in Human Cells. J Am Chem Soc., doi: 10.1021/jacs.7b11281. [Epub ahead of print] [PMID:29420021]


Caveat usor: assessing differences between major chemistry databases
(1) Southan C. (2018). Caveat usor: assessing differences between major chemistry databases. ChemMedChem., doi: 10.1002/cmdc.201700724. [Epub ahead of print] [PMID:29451740]


£54 million funding to transform UK health through data science
Health Data Research UK is awarding £30 million funding to six sites across the UK to address challenging healthcare issues through use of data science. Each site has world-class expertise; a track record in using health data to derive new knowledge, scientific discovery and insight; and works in close partnership with NHS bodies and the public to translate research findings into benefits for patients and populations. [Read more at Health Data Research UK]


The 100,000 Genomes Project
The project will sequence 100,000 genomes from around 70,000 people. Participants are NHS patients with a rare disease, plus their families, and patients with cancer. [Read more at Genomics England]


BACE1 inhibition more effectively suppresses initiation than progression of β-amyloid pathology
(1) Peters F et al. (2018). BACE1 inhibition more effectively suppresses initiation than progression of β-amyloid pathology. Acta Neuropathol., doi: 10.1007/s00401-017-1804-9. [Epub ahead of print] [PMID:29327084]


5-HT2C Receptor Structures Reveal the Structural Basis of GPCR Polypharmacology
(1) Peng Y et al. (2018). 5-HT2C Receptor Structures Reveal the Structural Basis of GPCR Polypharmacology. Cell, 172(4):719-730.e14. doi: 10.1016/j.cell.2018.01.001. [PMID:29398112]


Deubiquitylating enzymes and drug discovery: emerging opportunities
(1) Harrigan JA et al. (2018). Deubiquitylating enzymes and drug discovery: emerging opportunities. Nat Rev Drug Discov., 17(1):57-78. doi: 10.1038/nrd.2017.152. [PMID:28959952]


January 2018

Structure of the D2 dopamine receptor bound to the atypical antipsychotic drug risperidone
(1) Wang S et al. (2018). Structure of the D2 dopamine receptor bound to the atypical antipsychotic drug risperidone. Nature, doi:10.1038/nature25758. [Epub ahead of print]. [Abstract]


The Enduring Legacy of 250 Years of Pharmacology in Edinburgh
(1) Kelly JS, Mackay AVP. (2018). The Enduring Legacy of 250 Years of Pharmacology in Edinburgh. Annu Rev Pharmacol Toxicol., 58:293-307. doi: 10.1146/annurev-pharmtox-010617-052901 [PMID:28934562]


A Serendipitous Scientist
(1) Lefkowitz RJ. (2018). A Serendipitous Scientist. Annu Rev Pharmacol Toxicol., 58:17-32. doi: 10.1146/annurev-pharmtox-010617-053149. [PMID:28715979]


Pharmacogenomics of GPCR Drug Targets

Comments by Alexander Hauser, University of Copenhagen and GPCRdb

A collaboration between the MRC Laboratory of Molecular Biology, Cambridge (UK), the Scripps Research Institute in Florida and the Department of Drug Design and Pharmacology, University of Copenhagen (home of the GPCRdb team) has now published a new detailed study on the effects of genetic variation in G protein-coupled receptors on responses to FDA-approved drugs [1]. The authors address the following main questions: How variable are GPCR drug targets in the human population? Are individuals with variant receptors likely to respond differently to drugs? What is the estimated economic burden associated with variation in GPCR drug targets? Read the full article on our blog

(1) Hauser AS et al. (2017). Pharmacogenomics of GPCR Drug Targets. Cell, 172(1-2):41-54.e19. doi:10.1016/j.cell.2017.11.033. [PMID:29249361]


Structure of the Nanobody-Stabilized Active State of the Kappa Opioid Receptor
(1) Che T et al. (2018). Structure of the Nanobody-Stabilized Active State of the Kappa Opioid Receptor. Drug Discov Today, 172(1-2):55-67.e15. doi: 10.1016/j.cell.2017.12.011. [PMID:29307491]


Drug target residence time: a misleading concept
(1) Folmer RHA. (2017). Drug target residence time: a misleading concept. Drug Discov Today, S1359-6446(17)30241-6. doi: 10.1016/j.drudis.2017.07.016. [PMID:28782685]


GPCRs as targets for approved drugs: How many targets and how many drugs?
(1) Sriram K & Insel PA. (2018). GPCRs as targets for approved drugs: How many targets and how many drugs? Mol Pharmacol., doi: 10.1124/mol.117.111062. [Epub ahead of print]. [PMID:29298813]


International Union of Basic and Clinical Pharmacology CIII
(1) Kennedy AJ & Davenport AP. (2018). International Union of Basic and Clinical Pharmacology CIII: Chemerin Receptors CMKLR1 (Chemerin1) and GPR1 (Chemerin2) Nomenclature, Pharmacology, and Function. Pharmacol Rev., 70(1):174-196. doi: 10.1124/pr.116.013177. [PMID:29279348]


Structure of the complement C5a receptor bound to the extra-helical antagonist NDT9513727
(1) Roberston N et al. (2018). Structure of the complement C5a receptor bound to the extra-helical antagonist NDT9513727. Nature, 553(7686):111-114 doi: 10.1038/nature25025. [PMID:29300009]


Structure of the glucagon receptor in complex with a glucagon analogue
(1) Zhang H et al. (2018). Structure of the glucagon receptor in complex with a glucagon analogue. Nature, 553(7686):106-110. doi: 10.1038/nature25153. [PMID:29300013]


Allosteric Coupling of Drug Binding and Intracellular Signaling in the A2A Adenosine Receptor
(1) Eddy MT et al. (2017). Allosteric Coupling of Drug Binding and Intracellular Signaling in the A2A Adenosine Receptor. Cell Chem Biol., 172(1-2):68-80.e12. doi: 10.1016/j.cell.2017.12.004. [PMID:29290469]


Drug Target Commons: A Community Effort to Build a Consensus Knowledge Base for Drug-Target Interactions
(1) Tang J et al. (2017). Drug Target Commons: A Community Effort to Build a Consensus Knowledge Base for Drug-Target Interactions. Cell Chem Biol., S2451-9456(17)30426-9. doi: 10.1016/j.chembiol.2017.11.009. [PMID:29276046]


A dynamic map for learning, communicating, navigating and improving therapeutic development
(1) Wagner J et al. (2017). A dynamic map for learning, communicating, navigating and improving therapeutic development. Nat Rev Drug Discov., [EPub ahead of print]. doi: 10.1038/nrd.2017.217. [PMID:29269942]


Residue-Specific Peptide Modification: A Chemist's Guide
(1) deGruyter JN et al. (2017). Residue-Specific Peptide Modification: A Chemist's Guide. Biochemistry., 56(30):3863-3873. doi: 10.1021/acs.biochem.7b00536. [PMID:28653834]


Phenome-wide association studies (PheWAS) across large "real-world data" population cohorts support drug target validation
(1) Diogo D et al. (2017). Phenome-wide association studies (PheWAS) across large "real-world data" population cohorts support drug target validation BioRxiv., doi: https://doi.org/10.1101/218875. [Full text]


The spectrum of T cell metabolism in health and disease.
(1) Bantug GR et al. (2017). The spectrum of T cell metabolism in health and disease. Nat Rev Immunol., 18(1):19-34. doi: 10.1038/nri.2017.99. [PMID:28944771]


Genetic variation in human drug-related genes
(1) Schärfe CPI et al. (2017). Genetic variation in human drug-related genes. Genome Med., 9(1):117. doi: 10.1186/s13073-017-0502-5. [PMID:29273096]


Complex Portal - A Unifying Protein Complex Database
(1) Meldal, B et al. (2017). Complex Portal - A Unifying Protein Complex Database. Genomics and Computational Biology, [S.l.], v. 4, n. 1, p. e100052, dec. 2017. ISSN 2365-7154. [Full text]


Archive of previous years