IUPHAR Database of Receptors and Ion Channels

Hot topic: Crystal structures of the mu and kappa opioid receptors

The structures of the mu and kappa opioid receptors have been reported in the journal Nature by Manglik et al. and Wu et al. respectively, showing several interesting features. See the IUPHAR-DB Hot Topics page for further details and commentary by NC-IUPHAR: http://www.iuphar-db.org/hotTopics.jsp

Hot topic: Crystal structure of the S1P1 receptor

The structure of the S1P1 receptor fused with T4 lysozyme, in complex with a selective antagonist sphingolipid mimic (ML056), has been reported in the journal Science by Hanson and colleagues. See the IUPHAR-DB Hot Topics page for further details and commentary by NC-IUPHAR: http://www.iuphar-db.org/hotTopics.jsp

Hot topic: Structures of M2 and M3 muscarinic acetylcholine receptors

The structures of the human M2 receptor and the rat M3 receptor, each in a complex with an inverse agonist (3-quinuclidinyl-benzilate and tiotropium, respectively) have been reported in two papers published in Nature by Haga et al. and Kruse et al. See the IUPHAR-DB Hot Topics page for further details and commentary by NC-IUPHAR: http://www.iuphar-db.org/hotTopics.jsp

Database update: new version of IUPHAR-DB released February 2012 with new features and several receptor updates

The latest release of the IUPHAR database includes new annotation for the GABAA subunits alpha 3, 4 and 5, beta 2 and 3 and gamma 1, 2 and 3, as well as updates to several GPCR pages including beta-Adrenoceptors and Adrenoceptor introduction, Calcitonin receptors, Cannabinoid receptor introduction and Orexin receptors. Furthermore, the database team has completed the curation of sequence, structure and precursor data for all the endogenous peptide ligands of human, rat and mouse GPCRs and added links from receptor pages. New database links include links from ligand pages to BindingDB, a public database of measured binding affinities for drug-targets and small molecules, and links from receptor pages to Orphanet, the Portal for Rare Diseases and Orphan Drugs (see below).

Database update: new pilot Enzyme database released featuring the enzymes of the Lanosterol Biosynthesis Pathway

A pilot project to investigate the inclusion of enzymes in the IUPHAR database has been completed by database curators, covering the enzymes of the lanosterol biosynthesis pathway, including the target of the statin drugs, HMG CoA reductase. Enzyme pages include data on substrates, cofactors, reaction mechanisms, enzyme kinetics and potent inhibitors from literature with their binding affinities, plus links to BRENDA, the Comprehensive Enzyme Information System, KEGG, the Kyoto Encyclopedia of Genes and Genomes, which contains pathway, gene and chemical information, and the IUBMB Enzyme Nomenclature database. Enzyme database pages can be accessed at http://www.iuphar-db.org/DATABASE/ReceptorFamiliesForward?type=ENZYME

Database update: IUPHAR-DB and Orphanet collaborate to share information on the molecular basis of rare diseases

IUPHAR-DB and Orphanet, the Portal for Rare Diseases and Orphan Drugs, have begun a collaboration to share knowledge and links on the genetic and molecular bases of rare diseases and the actions of orphan drugs. Database links have been established between GPCRs, ion channels and NHRs in IUPHAR-DB and Orphanet gene pages. Information about the rare diseases to which they are linked will be added to the database over the coming weeks and linked up to expert-curated disease information available in Orphanet. Data on Ion channel-linked diseases (channelopathies) has already been added in a pilot project.

NC-IUPHAR and BPS announce the launch of a new online portal, the Guide to Pharmacology

NC-IUPHAR and the British Pharmacological Society (BPS) announce the launch of a new web site, the Guide to Pharmacology (http://www.guidetopharmacology.org), developed as a joint initiative to provide a one-stop shop for quantitative information on drug targets and the prescription medicines and experimental dugs that act on them. It provides a single entry point to IUPHAR-DB and an online database of information from the Guide to Receptors and Channels (GRAC) 5th (2011) edition. GRAC provides a succinct overview of the key properties of over 1600 established or potential pharmacological targets. This resource should be of interest to researchers and students in pharmacology and drug discovery as well as the interested public. IUPHAR-DB and GRAC data may be searched on either web site and receptor and ligand pages have reciprocal database links.

Hot topic: IUPHAR review article published on the Calcium-Activated Chloride Channels.

An IUPHAR review article on the Calcium-Activated Chloride Channels has been published online in Pharmacological Reviews.

Latest pairings: NC-IUPHAR provide details of recent pairings between orphan GPCRs and putative endogenous ligands reported in the literature

NC-IUPHAR provide details of several recent pairings between orphan GPCRs and putative endogenous ligands reported in the literature. Pairings have been reported between GPR31 and 12-(S)-Hydroxyeicosatetraenoic acid, GPR56 and collagen, type III, alpha-1, GPR35 and kynurenic acid/2-acyl lysophosphatidic acid and GPR183 (EBI2) and oxysterols. Visit the IUPHAR-DB latest pairings page for further information: http://www.iuphar-db.org/latestPairings.jsp

NC-IUPHAR and DiscoveRx announce that they will form an alliance to accelerate GPCR deorphanization efforts

NC-IUPHAR and DiscoveRx have announced that they will form an alliance to accelerate progress on understanding the functions of orphan G Protein-coupled receptors (GPCRs) and their signalling mechanisms, which will be communicated through the IUPHAR Database. Reciprocal links between IUPHAR-DB and the DiscoveRx websites have been established, enabling users of DiscoveRx products to access cutting-edge information on orphan GPCRs in the IUPHAR-DB and to provide a portal for IUHPAR-DB users to access information on DiscoveRx products. Read more about the goals of this unprecedented industry-academia alliance here: http://www.discoverx.com/about/about-press_090611.php

Database updates: recent updates to IUPHAR-DB include the addition of detailed annotation for the Nicotinic Acetylcholine receptor subunits, the Frizzled receptor FZD6 and updates to the database pages for VIP and PACAP receptors.

Recent updates to information in IUPHAR-DB include the addition of detailed annotation for the Nicotinic Acetylcholine receptor subunits, the Frizzled receptor FZD6 and updates to the introduction and receptor pages for VIP and PACAP receptors.

Hot topic: The 7-transmembrane receptor LGR5: A GPCR no more?

Two recent papers have now identified secreted R-spondin (RSPO) proteins as ligands for LGR5 and its homologues and have demonstrated that RSPO binding of LGR4/5/6 potentiates canonical Wnt-beta catenin signaling. See the IUPHAR-DB Hot Topics page for further details: http://www.iuphar-db.org/hotTopics.jsp

Hot topic: IUPHAR review article published on the nomenclature, distribution and pathophysiological functions of Leukotriene receptors.

An IUPHAR review article on the nomenclature, distribution and pathophysiological functions of Leukotriene receptors has been published online in Pharmacological Reviews.

Hot topic: An IUPHAR review article updating the classification of Prostanoid receptors has been published online ahead of print.

An update on the classification of Prostanoid receptors has been published online ahead of print in Pharmacological Reviews.

Website update: The NC-IUPHAR and IUPHAR-DB annual report is now online.

NC-IUPHAR and IUPHAR-DB curators publish their annual progress report. An online PDF document is available at http://www.iuphar-db.org/AboutNC-IUPHAR.pdf.

Database update: revised introductory chapter for 5-HT receptors.

The database introductory chapter for 5-HT G protein-coupled receptors has been updated.

Hot topic: Official IUPHAR nomenclature articles published on Adenosine and Hydroxy-carboxylic Acid receptors.

An update on the nomenclature and classification of Adenosine receptors has been published in the latest issue of Pharmacological Reviews. An article published online ahead of print introduces the IUPHAR-recommended nomenclature and classification of Hydroxy-carboxylic Acid receptors (GPR81, GPR109A, and GPR109B).