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With the dose at which its binding to plasma membrane PIP2 is nearly saturated (330 µM in injection pipette, i.e. 3.3 µM in cytoplasm), we have observed that the RFP-PH protein inhibits the sperm-induced Ca2+ signals, but only modestly (Fig. 6C).
To overcome this problem, we utilized a radiolabelled form of AR-C155858 to measure inhibitor binding to plasma membrane preparations from Xenopus oocytes expressing the different MCT1 mutants.
The mechanism of action of calcilytic drugs involves binding to plasma membrane CaSRs and diminishing receptor signaling responses in the presence of orthosteric agonist (20).
By binding to plasma membrane transporters, cocaine prevents the uptake of extracellular monoamines, consequently enhancing their extracellular levels, including norepinephrine and dopamine [ 2– 4].
Prior studies showed that TOM-1 inhibits SV priming, and that it does so by binding to plasma membrane SNAREs, forming inactive SNARE complexes (Gracheva et al., 2006; McEwen et al., 2006).
For example, clathrin heavy chain (CLTC) KD results in a large fraction of anti-CD8 antibody binding to plasma membrane localized CD8-CIMPR, indicative of a defect in the endocytic uptake of the CD8-CIMPR reporter.
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The effects of somatostatin are transduced by its binding to plasma membrane-localized somatostatin receptors (SSTRs).
The cellular effects of adiponectin are believed to be principally mediated through binding to plasma membrane-associated adiponectin receptors (AdipoRs -1 AdipoRs -1the progestin and AdipoQ receptor family, of which AdipoR1 is the more abundant isoform in muscle (13, 14).
Endogenous polyamine protects cells from damage by some fermentation inhibitors and ethanol by binding to plasma membranes, ribosomes, and DNA [ 39].
Specifically, disordered GluCer metabolism is postulated to interfere with α-syn binding to plasma membranes or to directly affect its fibrillisation, leading to an accumulation of toxic α-syn species.
Using a competitive displacement assay, specific 125I-tyrosine-11-somatostatin-14 binding to plasma membranes was assessed and and characterised in terms of receptor affinity (Kd) and maximum binding capacity (Bmax) as determined by Scatchard analysis.
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