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Concept

Partial agonist

Related publications (6)

Structural basis of the activation of the CC chemokine receptor 5 by a chemokine agonist

Henning Paul-Julius Stahlberg

The human CC chemokine receptor 5 (CCR5) is a G protein-coupled receptor (GPCR) that plays a major role in inflammation and is involved in cancer, HIV, and COVID-19. Despite its importance as a drug target, the molecular activation mechanism of CCR5, i.e., ...

AMER ASSOC ADVANCEMENT SCIENCE2021

Drug-induced increase in lysobisphosphatidic acid reduces the cholesterol overload in Niemann-Pick type C cells and mice

Marc Moniatte, Jonathan Paz Montoya

Most cells acquire cholesterol by endocytosis of circulating low-density lipoproteins (LDLs). After cholesteryl ester de-esterification in endosomes, free cholesterol is redistributed to intracellular membranes via unclear mechanisms. Our previous work sug ...

2019

The Principles of Ligand Specificity on beta-2-adrenergic receptor

Shuguang Yuan

G protein-coupled receptors are recognized as one of the largest families of membrane proteins. Despite sharing a characteristic seven-transmembrane topology, G protein-coupled receptors regulate a wide range of cellular signaling pathways in response to v ...

Nature Research2016

New conjugate of agonist ligand directed to ligand-gated ion channels of cysteine loop-family with chromophore, useful, e.g. in receptor proteins/their interaction with agonistic ligand and to study the effect of unlabelled ligands

Horst Arthur Vogel, Rudolf Hovius, Jörg Grandl

NOVELTY - Conjugate (I) of an agonist ligand directed to ligand-gated ion channels (LGICs) of the Cys loop-family with a chromophore, is new. USE - (I) is useful in the receptor proteins and/or their interaction with the agonistic ligand, where the interac ...

2007

Using X-ray absorption spectra to monitor specific radiation damage to anomalously scattering atoms in macromolecular crystallography

Philip Pattison, Marc Fleurant

Radiation damage in macromolecular crystals is not suppressed even at 90 K. This is particularly true for covalent bonds involving an anomalous scatterer (such as bromine) at the `peak wavelength'. It is shown that a series of absorption spectra recorded o ...

2007

Structure and function of the nicotinic acetylcholine receptor

Jörg Grandl

The subject of this thesis is the study of the structure and function of the human muscle nicotinic acetylcholine receptor (nAChR), which is a typical member of the large class of ligand-gated ion channels. Appropriate techniques, like site-directed mutage ...

EPFL2005