The significance of G protein-coupled receptor crystallography for drug discovery

JA Salon, DT Lodowski, K Palczewski - Pharmacological reviews, 2011 - ASPET
Crucial as molecular sensors for many vital physiological processes, seven-transmembrane
domain G protein-coupled receptors (GPCRs) comprise the largest family of proteins …

[HTML][HTML] Protein interactors and trafficking pathways that regulate the cannabinoid type 1 receptor (CB1R)

A Fletcher-Jones, KL Hildick, AJ Evans… - Frontiers in molecular …, 2020 - frontiersin.org
The endocannabinoid system (ECS) acts as a negative feedback mechanism to suppress
synaptic transmission and plays a major role in a diverse range of brain functions including …

Structure of signaling-competent neurotensin receptor 1 obtained by directed evolution in Escherichia coli

P Egloff, M Hillenbrand, C Klenk… - Proceedings of the …, 2014 - National Acad Sciences
Crystallography has advanced our understanding of G protein–coupled receptors, but low
expression levels and instability in solution have limited structural insights to very few …

Structure–function relationship and physiological role of apelin and its G protein coupled receptor

S Murali, GK Aradhyam - Biophysical reviews, 2023 - Springer
Apelin receptor (APJR) is a class A peptide (apelin) binding G protein-coupled receptor
(GPCR) that plays a significant role in regulating blood pressure, cardiac output, and …

Role of helix 8 in G protein-coupled receptors based on structure–function studies on the type 1 angiotensin receptor

J Huynh, WG Thomas, MI Aguilar… - Molecular and cellular …, 2009 - Elsevier
G protein-coupled receptors (GPCRs) are transmembrane receptors that convert
extracellular stimuli to intracellular signals. The type 1 angiotensin II receptor is a widely …

[HTML][HTML] Characterization of the residues in helix 8 of the human β1-adrenergic receptor that are involved in coupling the receptor to G proteins

NMD Santos, LA Gardner, SW White… - Journal of Biological …, 2006 - ASBMB
Several key amino acids within amphipathic helix 8 of the human β 1-adrenergic receptor (β
1-AR) were mutagenized to characterize their role in signaling by G protein-coupled …

[HTML][HTML] Helix 8 plays a crucial role in bradykinin B2 receptor trafficking and signaling

J Feierler, M Wirth, B Welte, S Schüssler… - Journal of Biological …, 2011 - ASBMB
Upon activation the human bradykinin B 2 receptor (B 2 R) acts as guanine nucleotide
exchange factor for the G proteins G q/11 and G i. Thereafter, it gets phosphorylated by G …

[HTML][HTML] Direct addition of poly-lysine or poly-ethylenimine to the medium: A simple alternative to plate pre-coating

A Faussner, MM Deininger, C Weber, S Steffens - Plos one, 2022 - journals.plos.org
For most cell culture experiments, it is indispensable that the cells are firmly anchored to
culture plates, withstanding rinsing steps that can create shear forces and tolerating …

Extracellular aspartic protease SAP2 of Candida albicans yeast cleaves human kininogens and releases proinflammatory peptides, Met-Lys-bradykinin and des-Arg9 …

G Bras, O Bochenska, M Rapala-Kozik… - Biological …, 2012 - degruyter.com
Bradykinin-related peptides, universal mediators of inflammation collectively referred to as
the kinins, are often produced in excessive amounts during microbial infections. We have …

[HTML][HTML] Bradykinin B2 and dopamine D2 receptors form a functional dimer

A Niewiarowska-Sendo, A Polit, M Piwowar… - … et Biophysica Acta (BBA …, 2017 - Elsevier
In recent years a wide range of studies have shown that G protein-coupled receptors
modulate a variety of cell functions through the formation of dimers. For instance, there is …