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Structures of the CXCR4 Chemokine GPCR with Small-Molecule and Cyclic Peptide Antagonists
Regulating Migration The migration of cells around the body is an important factor in cancer development and the establishment of infection. Movement is induced by small proteins called chemokines,… Expand
High-resolution crystal structure of an engineered human beta2-adrenergic G protein-coupled receptor.
Heterotrimeric guanine nucleotide-binding protein (G protein)-coupled receptors constitute the largest family of eukaryotic signal transduction proteins that communicate across the membrane. We… Expand
Structure of the Human Dopamine D3 Receptor in Complex with a D2/D3 Selective Antagonist
Tweaking Dopamine Reception Dopamine modulates many cognitive and emotional functions of the human brain by activating G protein–coupled receptors. Antipsychotic drugs that block two of the receptor… Expand
Structure of an Agonist-Bound Human A2A Adenosine Receptor
Changes associated with conformationally selective agonist binding shed light on G protein–coupled receptor activation. Activation of G protein–coupled receptors upon agonist binding is a critical… Expand
Structural Basis for Allosteric Regulation of GPCRs by Sodium Ions
GPCR Close-Up Structures of G protein–coupled receptors (GPCRs) determined in the past few years, have provided insight into the function of this important family of membrane proteins. Liu et al. (p.… Expand
A specific cholesterol binding site is established by the 2.8 A structure of the human beta2-adrenergic receptor.
The role of cholesterol in eukaryotic membrane protein function has been attributed primarily to an influence on membrane fluidity and curvature. We present the 2.8 A resolution crystal structure of… Expand
Structure-function of the G protein-coupled receptor superfamily.
- V. Katritch, V. Cherezov, R. Stevens
- Biology, Medicine
- Annual review of pharmacology and toxicology
- 7 January 2013
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 receptors-9 of… Expand
GPCR Engineering Yields High-Resolution Structural Insights into β2-Adrenergic Receptor Function
The β2-adrenergic receptor (β2AR) is a well-studied prototype for heterotrimeric guanine nucleotide–binding protein (G protein)–coupled receptors (GPCRs) that respond to diffusible hormones and… Expand
Structure of the human smoothened receptor bound to an antitumour agent
The smoothened (SMO) receptor, a key signal transducer in the hedgehog signalling pathway, is responsible for the maintenance of normal embryonic development and is implicated in carcinogenesis. It… Expand
Structure of the human histamine H1 receptor complex with doxepin
The biogenic amine histamine is an important pharmacological mediator involved in pathophysiological processes such as allergies and inflammations. Histamine H1 receptor (H1R) antagonists are very… Expand