Chlorobisphenol A (ClxBPA) is a kind of novel estrogenic compounds. The present study aims to investigate the effects of three ClxBPA compounds on the kisspeptin/G protein-coupled receptor 54 (GPR54, also named KissR1)-gonadotropin-releasing hormone ...
Bingli Lei+5 more
doaj
Identification and Characterization of Amlexanox as a G Protein-Coupled Receptor Kinase 5 Inhibitor
G protein-coupled receptor kinases (GRKs) have been implicated in human diseases ranging from heart failure to diabetes. Previous studies have identified several compounds that selectively inhibit GRK2, such as paroxetine and balanol. Far fewer selective
Kristoff T. Homan+4 more
doaj +1 more source
Concomitant activation of Gi protein-coupled receptor and protein kinase C or phospholipase C is required for platelet aggregation [PDF]
It has recently been suggested that the concomitant activation of two distinct G protein-coupled receptors (Gi and Gq) is essential for platelet aggregation: in fact, the thromboxane A2 synthetic agonist, U46619, which causes the selective activation of ...
Ciampa, Maria Teresa+5 more
core +1 more source
This study used longitudinal transcriptomics and gene‐pattern classification to uncover patient‐specific mechanisms of chemotherapy resistance in breast cancer. Findings reveal preexisting drug‐tolerant states in primary tumors and diverse gene rewiring patterns across patients, converging on a few dysregulated functional modules. Despite receiving the
Maya Dadiani+14 more
wiley +1 more source
The basal subcellular distribution of β-adrenergic receptor kinase is independent of G-protein βγ subunits [PDF]
β-adrenergic receptor kinase (βARK-1 or GRK2) is a key regulatory protein involved in the regulation of G-protein-coupled receptors which associates with microsomal and plasma membranes.
Esteban, Nuria+3 more
core +1 more source
B‐cell chronic lymphocytic leukemia (B‐CLL) and monoclonal B‐cell lymphocytosis (MBL) show altered proteomes and phosphoproteomes, analyzed using mass spectrometry, protein microarrays, and western blotting. Identifying 2970 proteins and 316 phosphoproteins, including 55 novel phosphopeptides, we reveal BCR and NF‐kβ/STAT3 signaling in disease ...
Paula Díez+17 more
wiley +1 more source
Targeting cardiac beta-adrenergic signaling via GRK2 inhibition for heart failure therapy
Cardiac cells, like those of the other tissues, undergo regulation through membrane-bound proteins known as G protein-coupled receptors (GPCRs). β-adrenergic receptors (βARs) are key GPCRs expressed on cardiomyocytes and their role is crucial in cardiac
Alessandro eCannavo+2 more
doaj +1 more source
Molecular Mechanism for Inhibition of G Protein-Coupled Receptor Kinase 2 by a Selective RNA Aptamer [PDF]
SummaryCardiovascular homeostasis is maintained in part by the rapid desensitization of activated heptahelical receptors that have been phosphorylated by G protein-coupled receptor kinase 2 (GRK2).
Lennarz, Sabine+3 more
core +1 more source
Determination of ADP/ATP translocase isoform ratios in malignancy and cellular senescence
The individual functions of three isoforms exchanging ADP and ATP (ADP/ATP translocases; ANTs) on the mitochondrial membrane remain unclear. We developed a method for quantitatively differentiating highly similar human ANT1, ANT2, and ANT3 using parallel reaction monitoring. This method allowed us to assess changes in translocase levels during cellular
Zuzana Liblova+18 more
wiley +1 more source
Proteomic analysis reveals GIT1 as a novel mTOR complex component critical for mediating astrocyte survival [PDF]
As a critical regulator of cell growth, the mechanistic target of rapamycin (mTOR) protein operates as part of two molecularly and functionally distinct complexes. Herein, we demonstrate that mTOR complex molecular composition varies in different somatic
Gutmann, David H, Smithson, Laura J
core +2 more sources