G protein-coupled receptors: structure-and function-based drug discovery
D Yang, Q Zhou, V Labroska, S Qin… - Signal transduction and …, 2021 - nature.com
As one of the most successful therapeutic target families, G protein-coupled receptors
(GPCRs) have experienced a transformation from random ligand screening to knowledge …
(GPCRs) have experienced a transformation from random ligand screening to knowledge …
Glutamatergic signaling in the central nervous system: ionotropic and metabotropic receptors in concert
A Reiner, J Levitz - Neuron, 2018 - cell.com
Glutamate serves as both the mammalian brain's primary excitatory neurotransmitter and as
a key neuromodulator to control synapse and circuit function over a wide range of spatial …
a key neuromodulator to control synapse and circuit function over a wide range of spatial …
GPCR activation mechanisms across classes and macro/microscales
Two-thirds of human hormones and one-third of clinical drugs activate~ 350 G-protein-
coupled receptors (GPCR) belonging to four classes: A, B1, C and F. Whereas a model of …
coupled receptors (GPCR) belonging to four classes: A, B1, C and F. Whereas a model of …
Multiscale simulations of biological membranes: the challenge to understand biological phenomena in a living substance
Biological membranes are tricky to investigate. They are complex in terms of molecular
composition and structure, functional over a wide range of time scales, and characterized by …
composition and structure, functional over a wide range of time scales, and characterized by …
Structural insights into the activation of metabotropic glutamate receptors
Metabotropic glutamate receptors are family C G-protein-coupled receptors. They form
obligate dimers and possess extracellular ligand-binding Venus flytrap domains, which are …
obligate dimers and possess extracellular ligand-binding Venus flytrap domains, which are …
Structural insights into G-protein-coupled receptor allostery
G-protein-coupled receptors (GPCRs) are key cell-surface proteins that transduce external
environmental cues into biochemical signals across the membrane. GPCRs are intrinsically …
environmental cues into biochemical signals across the membrane. GPCRs are intrinsically …
The role of interfacial lipids in stabilizing membrane protein oligomers
K Gupta, JAC Donlan, JTS Hopper, P Uzdavinys… - Nature, 2017 - nature.com
Oligomerization of membrane proteins in response to lipid binding has a critical role in many
cell-signalling pathways but is often difficult to define or predict. Here we report the …
cell-signalling pathways but is often difficult to define or predict. Here we report the …
Asymmetric activation of the calcium-sensing receptor homodimer
The calcium-sensing receptor (CaSR), a cell-surface sensor for Ca2+, is the master
regulator of calcium homeostasis in humans and is the target of calcimimetic drugs for the …
regulator of calcium homeostasis in humans and is the target of calcimimetic drugs for the …
Structures of Gi-bound metabotropic glutamate receptors mGlu2 and mGlu4
S Lin, S Han, X Cai, Q Tan, K Zhou, D Wang, X Wang… - Nature, 2021 - nature.com
The metabotropic glutamate receptors (mGlus) have key roles in modulating cell excitability
and synaptic transmission in response to glutamate (the main excitatory neurotransmitter in …
and synaptic transmission in response to glutamate (the main excitatory neurotransmitter in …
Generic GPCR residue numbers–aligning topology maps while minding the gaps
Generic residue numbers facilitate comparisons of, for example, mutational effects, ligand
interactions, and structural motifs. The numbering scheme by Ballesteros and Weinstein for …
interactions, and structural motifs. The numbering scheme by Ballesteros and Weinstein for …