Targeting PI3Kδ and PI3Kγ signalling disrupts human AML survival and bone marrow stromal cell mediated protection [PDF]
Phosphoinositide-3-kinase (PI3K) is an enzyme group, known to regulate key survival pathways in acute myeloid leukaemia (AML). It generates phosphatidylinositol-3,4,5-triphosphate, which provides a membrane docking site for protein kinaseB activation ...
Alves +37 more
core +1 more source
Threonine 180 Is Required for G-protein-coupled Receptor Kinase 3- and β-Arrestin 2-mediated Desensitization of the µ-Opioid Receptor in Xenopus Oocytes [PDF]
To determine the sites in the µ-opioid receptor (MOR) critical for agonist-dependent desensitization, we constructed and coexpressed MORs lacking potential phosphorylation sites along with G-protein activated inwardly rectifying potassium channels ...
Celvert, Jeremy P. +4 more
core
Skap2 is required for β2 integrin-mediated neutrophil recruitment and functions. [PDF]
Integrin activation is required for neutrophil functions. Impaired integrin activation on neutrophils is the hallmark of leukocyte adhesion deficiency (LAD) syndrome in humans, characterized by impaired leukocyte recruitment and recurrent infections. The
Bardel, Bernadette +11 more
core +2 more sources
Regulation of CXCR4 function by S1P1 through heteromerization
Background The trafficking of immune cells between lymphoid organs and circulation depends on gradients of CXCL12 and sphingosine-1-phosphate (S1P), mediated through their cognate receptors C-X-C chemokine receptor type 4 (CXCR4) and S1P receptor type 1 (
Hyun-Tae Kim, Jae-Yeon Jeong, Won-Ki Huh
doaj +1 more source
Identification of novel post-transcriptional features in olfactory receptor family mRNAs. [PDF]
Olfactory receptor (Olfr) genes comprise the largest gene family in mice. Despite their importance in olfaction, how most Olfr mRNAs are regulated remains unexplored.
Espinoza, Josh L +3 more
core +1 more source
An Alternative Mode of GPCR Transactivation: Activation of GPCRs by Adhesion GPCRs
G protein-coupled receptors (GPCRs), critical for cellular communication and signaling, represent the largest cell surface protein family and play important roles in numerous pathophysiological processes. Consequently, GPCRs have become a primary focus in drug discovery efforts. Beyond their traditional G protein-dependent signaling pathways, GPCRs are
openaire +2 more sources
Cardiac GPCRs: GPCR signaling in healthy and failing hearts
G protein-coupled receptors (GPCRs) are widely implicated in human heart disease, making them an important target for cardiac drug therapy. The most commonly studied and clinically targeted cardiac GPCRs include the adrenergic, angiotensin, endothelin, and adenosine receptors.
Salazar, Natasha C. +2 more
openaire +2 more sources
Computerized molecular docking methodologies are pivotal in in-silico screening, a crucial facet of modern drug design. ChooseLD, a docking simulation software, combines structure- and ligand-based drug design methods with empirical scoring.
Akihiro Masuda +2 more
doaj +1 more source
Crystal structure of rhodopsin bound to arrestin by femtosecond X-ray laser. [PDF]
G-protein-coupled receptors (GPCRs) signal primarily through G proteins or arrestins. Arrestin binding to GPCRs blocks G protein interaction and redirects signalling to numerous G-protein-independent pathways.
Barty, Anton +71 more
core +1 more source

