Mechanisms of signalling and biased agonism in G protein-coupled receptors
G protein-coupled receptors (GPCRs) are the largest group of cell surface receptors in
humans that signal in response to diverse inputs and regulate a plethora of cellular …
humans that signal in response to diverse inputs and regulate a plethora of cellular …
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 …
Common activation mechanism of class A GPCRs
Class A G-protein-coupled receptors (GPCRs) influence virtually every aspect of human
physiology. Understanding receptor activation mechanism is critical for discovering novel …
physiology. Understanding receptor activation mechanism is critical for discovering novel …
Into the tissues: Extracellular matrix and its artificial substitutes: Cell signalling mechanisms
The existence of orderly structures, such as tissues and organs is made possible by cell
adhesion, ie, the process by which cells attach to neighbouring cells and a supporting …
adhesion, ie, the process by which cells attach to neighbouring cells and a supporting …
Microbial and animal rhodopsins: structures, functions, and molecular mechanisms
Organisms of all domains of life use photoreceptor proteins to sense and respond to light.
The light-sensitivity of photoreceptor proteins arises from bound chromophores such as …
The light-sensitivity of photoreceptor proteins arises from bound chromophores such as …
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 …
PRESTO-Tango as an open-source resource for interrogation of the druggable human GPCRome
G protein–coupled receptors (GPCRs) are essential mediators of cellular signaling and are
important targets of drug action. Of the approximately 350 nonolfactory human GPCRs, more …
important targets of drug action. Of the approximately 350 nonolfactory human GPCRs, more …
Roles of Mas-related G protein–coupled receptor X2 on mast cell–mediated host defense, pseudoallergic drug reactions, and chronic inflammatory diseases
Mast cells (MCs), which are granulated tissue-resident cells of hematopoietic lineage,
contribute to vascular homeostasis, innate/adaptive immunity, and wound healing. However …
contribute to vascular homeostasis, innate/adaptive immunity, and wound healing. However …
Adenosine receptors as drug targets—what are the challenges?
Adenosine signalling has long been a target for drug development, with adenosine itself or
its derivatives being used clinically since the 1940s. In addition, methylxanthines such as …
its derivatives being used clinically since the 1940s. In addition, methylxanthines such as …
Structure-function of the G protein–coupled receptor superfamily
During the past few years, crystallography of G protein–coupled receptors (GPCRs) has
experienced exponential growth, resulting in the determination of the structures of 16 distinct …
experienced exponential growth, resulting in the determination of the structures of 16 distinct …