Isoform Selectivity of Adenylyl Cyclase Inhibitors and Identification of Novel Compounds
Nine membrane‐bound adenylyl cyclase (AC) isoforms produce the 2nd messenger cyclic AMP (cAMP) in response to a wide‐range of stimuli. Reduction of AC activity has well documented benefits, including for heart disease and pain. These roles have inspired development of isoform selective AC inhibitors, a lack of which currently limits exploration and/or ...
Cameron S. Brand +4 more
openaire +1 more source
Corticotropin-releasing factor facilitates epileptiform activity in the entorhinal cortex: roles of CRF2 receptors and PKA pathway. [PDF]
Whereas corticotropin-releasing factor (CRF) has been considered as the most potent epileptogenic neuropeptide in the brain, its action site and underlying mechanisms in epilepsy have not been determined.
Lalitha Kurada, Chuanxiu Yang, Saobo Lei
doaj +1 more source
Both Ligand- and Cell-Specific Parameters Control Ligand Agonism in a Kinetic Model of G Protein–Coupled Receptor Signaling [PDF]
G protein–coupled receptors (GPCRs) exist in multiple dynamic states (e.g., ligand-bound, inactive, G protein–coupled) that influence G protein activation and ultimately response generation. In quantitative models of GPCR signaling that incorporate these
Kinzer-Ursem, Tamara L. +1 more
core +3 more sources
Antiplatelet therapies: An overview
The role of blood components including platelets, in initiating inflammation, endothelial dysfunction, atherosclerosis, thrombus formation, thrombus growth, and acute vascular ischemic events, is well established.
Gundu H R Rao
doaj +1 more source
PACAP induces FSHβ gene expression via EPAC. [PDF]
Gonadotropins, luteinizing hormone (LH) and follicle-stimulating hormone (FSH), are heterodimers of a common α subunit and unique β subunits. Regulation of their levels, primarily by GnRH, is critical for reproductive function.
Coss, Djurdjica, Yeh, Debra M
core
Identification of novel molecular signatures of IgA nephropathy through an integrative -omics analysis [PDF]
IgA nephropathy (IgAN) is the most prevalent among primary glomerular diseases worldwide. Although our understanding of IgAN has advanced significantly, its underlying biology and potential drug targets are still unexplored.
Cisek, Katryna +11 more
core +2 more sources
Identification of a selective small-molecule inhibitor of type 1 adenylyl cyclase activity with analgesic properties [PDF]
ST034307 is a selective AC1 inhibitor with analgesic activity.
Tarsis F. Brust +8 more
openaire +2 more sources
No evidence for oncogenic mutations in guanine nucleotide-binding proteins of human adrenocortical neoplasms [PDF]
G-Proteins are membrane-bound heterotrimeric polypeptides that couple receptor signals to second messenger systems such as cAMP. Recently, point mutations at 2 codons of the highly preserved alpha-chain of Gs, the adenyl cyclase-stimulating G-protein ...
Chrousos, G. P. +3 more
core
Amino-terminal cysteine residues of RGS16 are required for palmitoylation and modulation of G(i)- and G(q)-mediated signaling [PDF]
RGS proteins (Regulators of G protein Signaling) are a recently discovered family of proteins that accelerate the GTPase activity of heterotrimeric G protein α subunits of the i, q, and 12 classes.
Backlund, Peter S. +5 more
core +1 more source
HD Physiology Project-Japanese efforts to promote multilevel integrative systems biology and physiome research. [PDF]
The HD Physiology Project is a Japanese research consortium that aimed to develop methods and a computational platform in which physiological and pathological information can be described in high-level definitions across multiple scales of time and size.
for HD physiology project investigators +3 more
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