Biased signalling: from simple switches to allosteric microprocessors
G protein-coupled receptors (GPCRs) are the largest class of receptors in the human
genome and some of the most common drug targets. It is now well established that GPCRs …
genome and some of the most common drug targets. It is now well established that GPCRs …
[HTML][HTML] DREADDs for neuroscientists
BL Roth - Neuron, 2016 - cell.com
To understand brain function, it is essential that we discover how cellular signaling specifies
normal and pathological brain function. In this regard, chemogenetic technologies represent …
normal and pathological brain function. In this regard, chemogenetic technologies represent …
[HTML][HTML] How ligands illuminate GPCR molecular pharmacology
G protein-coupled receptors (GPCRs), which are modulated by a variety of endogenous and
synthetic ligands, represent the largest family of druggable targets in the human genome …
synthetic ligands, represent the largest family of druggable targets in the human genome …
[HTML][HTML] Structure of the nanobody-stabilized active state of the kappa opioid receptor
The κ-opioid receptor (KOP) mediates the actions of opioids with hallucinogenic, dysphoric,
and analgesic activities. The design of KOP analgesics devoid of hallucinatory and …
and analgesic activities. The design of KOP analgesics devoid of hallucinatory and …
The diverse roles of arrestin scaffolds in G protein–coupled receptor signaling
YK Peterson, LM Luttrell - Pharmacological reviews, 2017 - ASPET
The visual/β-arrestins, a small family of proteins originally described for their role in the
desensitization and intracellular trafficking of G protein–coupled receptors (GPCRs), have …
desensitization and intracellular trafficking of G protein–coupled receptors (GPCRs), have …
[HTML][HTML] CXCR3 ligands in cancer and autoimmunity, chemoattraction of effector T cells, and beyond
N Karin - Frontiers in immunology, 2020 - frontiersin.org
CXCR3 is a chemokine receptor with three ligands; CXCL9, CXCL10, and CXCL11.
CXCL11 binds CXCR3 with a higher affinity than the other ligands leading to receptor …
CXCL11 binds CXCR3 with a higher affinity than the other ligands leading to receptor …
Molecular signatures of G-protein-coupled receptors
G-protein-coupled receptors (GPCRs) are physiologically important membrane proteins that
sense signalling molecules such as hormones and neurotransmitters, and are the targets of …
sense signalling molecules such as hormones and neurotransmitters, and are the targets of …
[HTML][HTML] The dynamic process of β2-adrenergic receptor activation
G-protein-coupled receptors (GPCRs) can modulate diverse signaling pathways, often in a
ligand-specific manner. The full range of functionally relevant GPCR conformations is poorly …
ligand-specific manner. The full range of functionally relevant GPCR conformations is poorly …
Allosteric nanobodies reveal the dynamic range and diverse mechanisms of G-protein-coupled receptor activation
G-protein-coupled receptors (GPCRs) modulate many physiological processes by
transducing a variety of extracellular cues into intracellular responses. Ligand binding to an …
transducing a variety of extracellular cues into intracellular responses. Ligand binding to an …
[HTML][HTML] Ligand and G-protein selectivity in the κ-opioid receptor
The κ-opioid receptor (KOR) represents a highly desirable therapeutic target for treating not
only pain but also addiction and affective disorders. However, the development of KOR …
only pain but also addiction and affective disorders. However, the development of KOR …