This post on SID tagging has been reproduced, with permission, from Dr. Chris Southan’s original post in his blog – Bio <-> Chem. It is intended to be user-orientated, those interested in the technicalities are welcome to contact the Guide…
Blog Archives
Database Release 2022.4
The latest release of the IUPHAR/BPS Guide to Pharmacology database was made on 13th December 2022. This database release is version 2022.4, and is the fourth release this year. GtoPdb now contains: 3,013 human targets, 1,633 of which have curated…
Hot Topics: FXR inhibition may protect from SARS-CoV-2 infection by reducing ACE2
FXR inhibition may protect from SARS-CoV-2 infection by reducing ACE2 This manuscript (1) reports on extensive and compelling experimental evidence and translational data from retrospective review of clinical registries, which show that pharmacological inhibition of the farnesoid X receptor (FXR)…
Database Release 2022.3
The latest release of the IUPHAR/BPS Guide to Pharmacology database was made on 13th October 2022. This database release is version 2022.3, and is the third release this year. The following blog post gives details of the key content updates…
Database Release 2022.2
A new database release (version 2022.2) of the IUPHAR/BPS Guide to Pharmacology was made on 9th June 2022. This blog post gives details of the key content updates and website changes. GtoPdb now contains: 3,002 human targets, 1,611 of which…
Prof. Jamie Davies – RSE Fellow
Congratulations to Professor Jamie Davies, Professor of Experimental Anatomy, University of Edinburgh, who has been elected to a Fellowship by The Royal Society of Edinburgh, Scotland’s National Academy. Fellowships are awarded to individuals in academia, business and public service who…
Hot Topics: A new study shows that human ageing is absolutely precise, when disease is eliminated, and accompanied by a disintegration of metabolic efficiency
Human ageing is just disintegration, but absolutely precise, linked to loss of VO2 max, which is why COVID is age-related. A new study (1) shows that the decline in human performance with age at 5000 m, an athletic event requiring…
Hot Topics: Endothelin-1 pathway, a new therapeutic target for COVID-19
SARS-CoV-2 gains entry into the body mainly via the lungs. After entering the blood, the virus rapidly multiplies to infect nearby cells. Endothelial cells line every blood vessel and have a surface area similar to a tennis court. These cells…
Database Release 2022.1
We are pleased to announce that the first IUPHAR/BPS Guide to Pharmacology of 2022 was made on 31st March 2022. database. This release is version 2022.1 and this blog post gives details of the key content updates and website changes.…
Hot Topics: SARS-CoV-2 and the truncated ACE-2 variant
ACE2 (Guide to Pharmacology Target id: 1614) normally functions as an enzyme metabolising peptides that regulate the cardiovascular system. As is well known though, it has recently gained additional scientific fame by also acting as a receptor for SARS-CoV-2. This study [1] compared…
Database Release 2021.4
The 2021.4 release of the IUPHAR Guide to Pharmacology was made on 14th December 2021. This blog post gives details of the key content updates and website change The 2021.4 release contains: 3,000 human targets with curated quantitative ligand interactions.…
Posted in Database updates, Guide to Malaria Pharmacology
Hidden REF award to Guide to Pharmacology
It is with great pleasure that we can announce that the IUPHAR/BPS Guide to PHARMACOLOGY has been given a hidden REF award in the category ‘applications of research’. The hidden Ref (https://hidden-ref.org) is a national ‘competition’, supported by publishers, learned…
Database Release 2021.3
Database release details for the first release in 2021 of the Guide to PHARMACOLOGY database, version 2021.1
Hot Topics: Trends in kinase drug discovery: twenty years of successfully targeting the kinome
The FDA approval of imatinib in 2001 was a breakthrough in molecularly targeted cancer therapy and heralded the emergence of kinase inhibitors as a key drug class in the oncology area and beyond. Continued advances in the molecular understanding of…
Database Release 2021.2
Database release details for the first release in 2021 of the Guide to PHARMACOLOGY database, version 2021.1
Database Release 2021.1
Database release details for the first release in 2021 of the Guide to PHARMACOLOGY database, version 2021.1
GtoPdb pre-release ligands (2021.1)
These are some of the ligands under curation (pre-release) in the Guide to Pharmacology. We expect them to be available on the website at the next database release (2021.1). Ligand ID: 11395Names: MK-7110Comment: MK-7110 (originally OncoImmune’s CD24Fc) is a synthetic…
Hot Topics: Gene Symbol usage and the need to do better
The GtoPdb team need no convincing about the importance of eliminating equivocality in gene and gene product names, as they are used in the pharmacology, chemical biology and drug discovery literature. Crucially, this also applies to their inclusion in curated…
Posted in Hot Topics
GtoPdb at Pharmacology 2020
The BPS Pharmacology 2020 Meeting is being held virtually this year, but this hasn’t diminished Guide to Pharmacology presence. On Monday 14th, Dr. Simon Harding presented our poster on ‘Expansion for anti-malarial, antibiotics and COVID-19’. Click to view poster. On…
Database Release 2020.5
We are pleased to announce the latest release of the Guide to PHARMACOLOGY database, version 2020.5. This is the last planned release for 2020. The 2020.5 release contains: 1,567 human targets with curated quantitative ligand interactions. 10,659 ligands, 7,884 of…
Database Release 2020.4
The latest release of the Guide to PHARMACOLOGY database, version 2020.4, has now been made. Coronavirus The Guide to Pharmacology coronavirus information page continues to be updated on a regular basis to capture the latest pharmacological strategies under investigation to mitigate against…
Tagged with: 2020.4, database release, oncology targets, WHO essential medicines
Posted in Database updates
Posted in Database updates
Hot Topics: Soluble ligands as drug targets
Historically, the main classes of drug targets have been receptors, enzymes, ion channels and transporters which are primarily targeted by small molecules. However, advances in molecular biology, genomics, and pharmacology have facilitated the development of different therapeutic modalities which in…
GtoPdb pre-release ligands (2020.4)
These are some of the ligands under curation (pre-release) in the Guide to Pharmacology. We expect them to be available on the website at the next database release (2020.4). Ligand ID: 11132 Name: otilimabComment: Otilimab (MOR103, GSK3196165) is a clinical…
Hot Topics: TMEM163 regulates ATP-gated P2X receptor and behaviour
It is now clear that ligand-gated ion channels (LGICs) are not “stand alone” functional units, but form complexes with other components, including scaffolding proteins, regulatory proteins and enzymes. Besides their important physiological roles, these modulating proteins are also potential targets…
Accessing WHO Essential Medicines in GtoPdb
The Guide to Pharmacology (GtoPdb) currently contains data on over 10,000 different ligands which are categorised into an number of different groups or classifications. The ligand list page (https://www.guidetopharmacology.org/GRAC/LigandListForward?type=WHO-essential&database=all) provides a directory of all the ligands described in the database,…
Database Release 2020.3
The latest release of the Guide to PHARMACOLOGY database, version 2020.3, has now been made. A large focus of our curation over the last couple of month since our 2020.2 release We are pleased to have been able to make…
Hot Topics: A trio of GPCR peptide publications
This post covers three recent publications with a common theme and whose authors are collaborators with GtoPdb, thus making them as a trio particularly suitable for combined review. These are; Discovery of Human Signaling Systems: Pairing Peptides to G Protein-Coupled…
GtoPdb pre-release ligands (2020.3)
These are some of the ligands under curation (pre-release) in the Guide to Pharmacology. We expect them to be available on the website at the next database release (2020.3). Ligand ID: 10891 Name: aviptadil Comment: Aviptadil is a vasoactive intestinal…
Database Release 2020.2
We are pleased to have been able to make an expeditious database release (version 2020.2), following on from our last update in March 2020 in order to make public new curation specifically related to SARS-CoV-2. Content Updates GtoPdb now includes…
Posted in Database updates, Technical
GtoPdb pre-release ligands (2020.2)
These are some of the ligands under curation (pre-release) in the Guide to Pharmacology. We expect them to be available on the website at the next database release (2020.2 – no earlier than April 2020). Ligand ID: 10716 Name: PRD_002214…
Database Release 2020.1
We are pleased to announce our first database release of 2020 – version 2020.1. Coronavirus (Covid-19) We have added a new coronavirus page to the Guide to Pharmacology which aims to consolidate key pharmacological information and resources related to coronavirus.…
Hot Topics: Virtual screening on the crystal structure of the G protein-coupled melatonin MT1 receptor reveals several new chemical scaffolds with biological activity
Melatonin targets two high-affinity receptors, MT1 and MT2, that belong to the G protein-coupled receptor (GPCR) superfamily (1,2). Drugs acting on melatonin receptors are subscribed for circadian disorders (jet lag, shift work, etc.), insomnia and major depression (3). All marketed…
Hot Topics: Cardiac Ca2+ Channel Regulation in the Fight-or-Flight Response: the monomeric small G-protein as another piece in the puzzle
Thirty eight years after the discovery that injection of the catalytic subunits of cyclic AMP-dependent protein kinase A (PKA) into isolated pig ventricular cardiac myocytes (1) increases the amplitude of L-type Ca2+ current (today known to be formed by Cav1.2…
Hot topics: Cannabinoid receptor stuctures
Two new reports cover further aspects of cannabinoid receptor binding as defined using cryo-EM. These expand on previous reports of the structure of the human CB1 cannabinoid receptor with the antagonists taranabant and AM6538 bound, and with the agonists MDMB-FUBINACA,…
Hot Topics: A brief update on coronaviruses
The new respiratory coronavirus from Wuhan in China is causing intense research activity in the world. Viruses are evidently associated with respiratory infections ranging in severity from the common cold to pneumonia and death
Tagged with: ACE2, coronavirus, dendritic cells, HcoV-229E, immunopharmacology, pharmacology
Posted in Hot Topics
Posted in Hot Topics
Hot Topics: Cryo-EM structure of a selective T-type calcium channel blocker bound to the Cav3.1 voltage-gated calcium channel
Nieng Yan’s group has now published the cryo-EM structure of the selective T-type Ca2+ channel blocker Z944 bound to the pore-forming α1-subunit of Cav3.1 T-type Ca2+ channels (1). This nicely adds to recent publications reporting of the high-resolution structures of…
Tagged with: calcium channel, hot topic, pharmacology, protein structure, VGICs, voltage-gated
Posted in Hot Topics
Posted in Hot Topics
Hot Topics: Deciphering the crystal structure of the leukotriene receptor CysLT2 opens up for improved therapeutics
Leukotrienes are lipid mediators of inflammation, initially recognized for their role in asthma, but also having potent effects in for example cardiovascular and neurological diseases as well as in cancer. The initial pharmacological classification of leukotriene receptors based on antagonist…
Hot Topics: New crystal structure of the muscarinic M5 receptor completes the set
Muscarinic receptors consist of 5 G protein-coupled receptors which along with nicotinic ion channels mediate the effects of acetylcholine. Despite years of research on the role of muscarinic receptors in the brain and periphery the Muscarinic M5 receptor has stood…
Database Release 2019.5
Our fifth and final database release of 2019 has been made and includes a number of minor content and website updates. Crucially, it comes at a time when we have just published our most recent database update in Nucleic Acids…
Posted in Database updates, Technical
Hot Topics: 3D structure of the full-length P2X7 receptor provides insight into factors controlling agonist potency and receptor desensitisation
P2X receptors are ligand-gated cation channels for which ATP is the endogenous orthosteric agonist. Seven P2X subunits have been identified and they form trimers to produce at least twelve different receptor subtypes. The tertiary structure of several subtypes have been…
Official Launch of the Guide to MALARIA PHARMACOLOGY
We are delighted to announce the first full public release of the IUPHAR/MMV Guide to MALARIA PHARMACOLOGY (abbreviated to GtoMPdb). This new web resource, designed specifically for malaria pharmacology, has been developed as a joint initiative between the International Union…
Database Release 2019.4
We are very pleased to announce our a new release of the IUPHAR/BPS Guide to Pharmacology. This version (2019.4) is the fourth this year and includes the first full-release of the IUPHAR/MMV Guide to Malaria Pharmacology. Content Updates GtoPdb now…
Hot Topics: GPR139 as a potential target for increasing opioid safety
The cross-talk between different G protein-coupled receptor signal-transduction pathways is an intriguing concept with important physiological implications [1]. A recent study by Wang et al. [2] has discovered that the actions of opioid drugs on the μ-opioid receptor (MOR) are…
Hot Topics: Resting-State Structure and Gating Mechanism of a Voltage-Gated Sodium Channel
In this report the Catterall laboratory succeeded in solving the high resolution structure of a voltage-gated Na+-channel (Nav) in its resting state (1). Why is this difficult and why is this important? It is difficult because Navs exist in the…
Hot Topics: The atlas of aminergic GPCR mutagenesis
G protein-coupled receptors (GPCRs) are an important family of signal-transducing membrane proteins capable of binding various types of ligands from the extracellular space and activating various signalling pathways inside the cell, rendering them one of the largest protein target families…
Posted in Hot Topics
Database Release 2019.3
We have now made the third IUPHAR/BPS Guide to Pharmacology database release of 2019 (2019.3). It includes updates focussed on preparation for the next edition of The Concise Guide to PHARMACOLOGY (2019/20), due out later this year. Content Updates GtoPdb…
Hot Topics: Time to FRET about GPCR activation dynamics?
G protein coupled receptors (GPCRs) are crucial for the transduction of extracellular stimuli to the intracellular space. Upon activation, GPCRs undergo large conformational changes to engage transducers and stimulate intracellular responses. However, the kinetics of agonist induced GPCR conformational changes…
World Malaria Day 2019: A New Guide to Malaria Pharmacology
Thursday 25th 2019 is World Malaria Day and we’d like to highlight our new resource, currently under development, called The IUPHAR/MMV Guide to Malaria Pharmacology (GtoMPdb). Based in Edinburgh, this new resource is directed by Professor Jamie Davies and his team and…
Hot Topics: Rise up against statistical significance, probably.
A recent commentary in Nature has the provocative title “Retire Statistical Significance” (1, with a list of more than 800 signatories) and has been widely interpreted as a call for the entire concept of statistical significance to be abandoned. Closer…
Database Release 2019.2
We are pleased to announce a new IUPHAR/BPS Guide to Pharmacology database release! This release, 2019.2, is the second of the year and includes updates focussed on preparation for the next edition of The Concise Guide to PHARMACOLOGY (2019/20), due…
Posted in Database updates
guidetopharmacology blog 