Receptor pharmacology articles from across Nature Portfolio

Cryo-electron microscopy structures of the type 2 taste receptor TAS2R14 in complex with Ggust and Gi1 identify cholesterol as an orthosteric agonist and the bitter tastant cmpd28.1 as a positive allosteric modulator and agonist.

Use of a cAMP biosensor to study real-time mechano-sensitive enhancement of β2-adrenoceptor constitutive activity and its inhibition by β2-inverse agonists in HEK 293 cells.

G protein responses mediated by GPCRs may differ depending on their environment. Here, using highly sensitive Gi/o sensors, the authors reveal the specific pharmacological and Gi/o protein responses of some native GPCRs in neurons, and the influence of G protein composition.

The serotonin transporter, targeted by several medications, terminates neurotransmission by clearing serotonin from the synaptic cleft. Combining biochemical results with in silico data, the authors show the key interactions that initiate substrate transport.

New research shows that a drug conjugate that links the dual PPAR𝛼/𝛾 agonist tesaglitazar to a GLP-1 receptor agonist has superior effects on weight loss and glucose metabolism compared with monotherapy in mice. The conjugate has actions in the hypothalamus that may contribute to its benefits.

Kv3 channels enable neurons to fire at very high frequencies (>100 Hz) which is fundamental to brain development and our ability to make sense of the world at large. Cryo-EM and structure-function studies by Chi et al. now uncover Kv3 channel gating mechanisms and support new precision medicine approaches for CNS diseases.