Blog Archives

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: , , , , ,
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

Tagged with: , , ,
Posted in Hot Topics

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

Tagged with: , ,
Posted in Hot Topics

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

Tagged with: , , ,
Posted in Hot Topics

Hot Topic: Unexplored therapeutic opportunities in the human genome

Contemporary drug discovery is dominated by two related  themes. The first of these is target validation upon which the sustainability of pharmaceutical R&D (in both the commercial and academic sectors) crucially depends.  The second is the size of the pool of human

Tagged with: ,
Posted in Hot Topics

Hot topic: The G Protein-Coupled Receptors deorphanization landscape.

Within the vast GPCR superfamily, orphans are described as receptors devoid of known endogenous ligands. They have been labeled as 7 transmembrane proteins by sequence homology and dispatched accordingly in the different GPCR subfamilies. They have attracted much attention given

Tagged with: ,
Posted in Hot Topics

GtoPdb at Pharmacology 2017

The GtoPdb team will be at the British Pharmacological Society’s flagship meeting, Pharmacology 2017, in London, December 11-13th 2017. We are pleased to have our own stand at this meeting and will be present during the refreshment breaks and poster

Tagged with: ,
Posted in Concise Guide to Pharmacology, Events