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GPCR & Company: Databases and Servers for GPCRs and Interacting Partners
2013G-protein-coupled receptors (GPCRs) are a large superfamily of membrane receptors that are involved in a wide range of signaling pathways. To fulfill their tasks, GPCRs interact with a variety of partners, including small molecules, lipids and proteins. They are accompanied by different proteins during all phases of their life cycle.
Noga, Kowalsman, Masha Y, Niv
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2010
There are a total of 33 members of adhesion G protein-coupled receptors (GPCRs) in humans and 30 members in mice and rats. More than half of these receptors are expressed in the central nervous system (CNS), indicating their possible roles in the development and function of the CNS.
Natalie, Strokes, Xianhua, Piao
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There are a total of 33 members of adhesion G protein-coupled receptors (GPCRs) in humans and 30 members in mice and rats. More than half of these receptors are expressed in the central nervous system (CNS), indicating their possible roles in the development and function of the CNS.
Natalie, Strokes, Xianhua, Piao
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Orphan GPCRs and their ligands
Pharmacology & Therapeutics, 2006Due to their diversity, G-protein-coupled receptors (GPCRs) are major regulators of intercellular interactions. They exert their actions by being activated by a vast array of natural ligands, referred to in this article as "transmitters". Yet each GPCR is highly selective in its ligand recognition.
Olivier, Civelli +4 more
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Current Opinion in Structural Biology, 2019
Molecular switches in GPCRs enable passing the signal from the agonist binding site, usually located close to the extracellular surface, to the intracellular part of the receptor. The switches are usually associated with conserved structural motifs on transmembrane helices (TMs), and they are accompanied by adjacent residues which provide the signal to
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Molecular switches in GPCRs enable passing the signal from the agonist binding site, usually located close to the extracellular surface, to the intracellular part of the receptor. The switches are usually associated with conserved structural motifs on transmembrane helices (TMs), and they are accompanied by adjacent residues which provide the signal to
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Privileged Structures in GPCRs
2007Certain kinds of ligand substructures recur frequently in pharmacologically successful synthetic compounds. For this reason they are called privileged structures. In seeking an explanation for this phenomenon, it is observed that the privileged structure represents a generic substructure that matches commonly recurring conserved structural motifs in ...
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Trends in Biotechnology, 2005
G protein-coupled receptors (GPCRs) are targets for 60-70% of drugs in development today. Traditionally, the drug discovery process has relied on screening of chemical compounds to identify novel and more-efficient drug molecules. Structure-based drug design, however, provides a targeted approach but has been severely hampered by limited knowledge of ...
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G protein-coupled receptors (GPCRs) are targets for 60-70% of drugs in development today. Traditionally, the drug discovery process has relied on screening of chemical compounds to identify novel and more-efficient drug molecules. Structure-based drug design, however, provides a targeted approach but has been severely hampered by limited knowledge of ...
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Structural snapshots uncover a key phosphorylation motif in GPCRs driving β-arrestin activation
Molecular Cell, 2023Shirsha Saha +2 more
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