Blog Archives

Hot topic: (but in this case, stale beer) the long overdue primary pharmacological characterisation of BIA 10-2747

The unfortunate French clinical trial disaster in which the FAAH inhibitor BIA 10-2747 (ligand ID 9001)  left one participant dead and several others with serious neurological adverse events, occurred back in January 2016.  However, the primary publication that describes the properties

Posted in Hot Topics

Hot topic: Cryo-EM structure of the active, Gs-protein complexed, human CGRP receptor

In this multi-author, multi-centre publication [1] lead by Denise Wootten and Patrick Sexton from the Monash Institute of Pharmacological Sciences, there is reported a 3.3 Angstrom structure of one of the more unusual G protein-coupled receptors. The CGRP receptor is

Posted in Hot Topics

Hot Topic: β-Subunit of the voltage-gated Ca2+ channel Cav1.2 drives signaling to the nucleus via H-Ras

This paper [1] extends previous studies demonstrating a key role of voltage-gated L-type Ca2+ channels in the modulation of activity-dependent gene transcription. Earlier work in cultured neurons had already shown that L-type channel activity is required to activate gene expression

Posted in Hot Topics

July 2018 News, Updates and Hot Topics

July 2018 News, Updates and Hot Topics Database release 2018.3: Our third database release of the year, 2018.3, is now available. This update contains the following new features and content changes: Updates across several target classes. The existing Antimalarial targets

Tagged with: ,
Posted in Hot Topics

Hot topic: Direct activation of neuronal KV7 channels by GABA and gabapentin – a novel mechanism for reducing neuronal excitability

The potassium channels KV7.2-KV7.5 (KCNQ2-5; GtoPdb target IDs 561-564) regulate neuronal excitability in the mammalian nervous system. The best characterised neuronal KV7 channels give rise to the M current (1) and are mediated predominantly by hetero-tetramers of KV7.2 and KV7.3

Posted in Hot Topics

Hot topic: New pharmacological tools reiterate lack of direct connection between Angiotensin 1–7 and the MAS1 GPCR

A new type of deorphanization conundrum confronted in pairing the GPCR, MAS1 with the hormonal peptide angiotensin 1–7 (Ang1-7) was emphasised in recent IUPHAR reviews (1, 2). More evidence for disconnection between Ang1-7 and MAS1 is presented in the recent

Posted in Hot Topics

Hot Topic: Structural details for coupling of the agonist-occupied µ opioid receptor (amongst others) to the Gi protein

Every few years in the field of receptor pharmacology, a technological advance occurs that drives the field forward in terms of insight and understanding. Over the past couple of years, the cryo-EM technique (the development of which won the 2017

Tagged with: ,
Posted in Hot Topics