In this report, we show that desensitization regulates ligand- independent, spontaneous activity of the human B2 bradykinin (BK) receptor, and the level of spontaneous receptor activity determines the action of the BK antagonists and partial receptor agonists NPC17731 and HOE140 as agonists or inverse agonists. Spontaneous receptor activity was monitored by measuring basal cellular phosphoinositid

Elevated formation of bradykinin (BK) and Lys-BK or kallidin (KD) and their carboxypeptidase metabolites desArg9BK and desArg10KD is evident at sites of inflammation. Moreover, B2 receptors (B2R) which mediate the action of BK and KD, participates in the acute stage of the inflammatory and pain response, whereas B1 receptors (B1R), through which desArg9BK and desArg10KD act, partake in the chronic

In order to identify agonist- and antagonist-binding epitopes in the human B1 and B2 bradykinin (BK) receptors, we exploited the ability of these receptors to discriminate between peptide ligands that differ only by the absence (B1) grid presence (B2) of a C-terminal Arg. This was done by constructing chimeric proteins in which specific domains were exchanged between these receptors as recently de

The B1 and B2 bradykinin (BK) receptor subtypes belong to the GPCR faro ily, and they discriminate between peptides that differ only by the absence and presence of a C-terminal Arg, To identify receptor residues conferring tigand spe.cificity, chimeric constructs in which TM-III were exchanged between the receptors were expressed and assayed by radioligand binding and fluorescence Ca2+ imaging in

Caveolae are small flask-like invaginations on the plasma membrane that contain both G-proteins aim G-protein coupled receptors. Consequently, these structures have been implicated to serve a role in transmembrane signaling. Bradykinin (BK) is a potent vasoactive peptide that acts through B2 BK receptors to stimulate both Gaq and Gai. DDT1 MF2 smooth muscle cells were used to show that eaveolae co

In order to investigate the molecular basis for the ability of the human B1 and B2 bradykinin (BK) receptor subtypes to discriminate between subtype- selective ligands, we constructed chimeric proteins in which the sixth transmembrane domains (TM-VI) of these receptors were exchanged. The pharmacological profiles of the constructs were analyzed by radioligand binding in particulate preparations of

In this report, we show that the vasoactive peptide agonist bradykinin (BK) when bound to B2 BK receptors on DDT1 MF-2 smooth muscle cells promotes the recruitment and sequestration of the occupied receptors and the receptor- coupled G-protein α subunits Gα(q) and Gα(i) in caveolae. Association of ligand receptor complexes and Gα subunits with caveolae was indicated by their co-enrichment on densi

Artificiell intelligens bryter med invanda sätt att tänka kring å ena sidan objekt, ting, teknologiska artefakter och, å andra sidan, handlande subjekt. Somliga tänker rent av på artificiell intelligens som en ny form av liv. En sfär där artificiell intelligens står inför ett genombrott är i krig. Av förklarliga skäl finns starka åsikter om detta. Utvecklingen förkastas som innebärandes slutet på

The objective of this study was to probe the molecular mechanisms underlying the increase in sensitivity of cells to bradykinin (BK) following expression of a transforming Ha-ras oncogene. We used native NIH3T3 fibroblast (3T3) cells and 3T3 cells transfected with a glucocorticoid-sensitive oncogenic Ha-ras construct (DT cells). DT cells incubated in the presence of 1 μM dexamethasone (DEX) for 24

Stimulation of B1 and B2 kinin receptors on cultured rabbit superior mesenteric artery smooth muscle cells with des-Arg9-bradykinin (DBK) and bradykinin (BK), respectively, results in significantly different patterns of intracellular Ca2+ mobilization. Single-cell fluorescence imaging of Fura- 2-loaded cells revealed that although both DBK and BK initially triggered similar rapid increases in cyto

Chemical cross-linking combined with site-directed mutagenesis was used to evaluate the role of extracellular cysteines and their positions relative to the binding site for the agonist bradykinin (BK) in the human BK B2 receptor. All extracellular cysteines, Cys20, Cys103, Cys184, and Cys277, in the receptor were mutated to serines, and single and double mutants were transfected into COS-7 cells.

This thesis is an exploration of leadership dimensions of academic organisational processes. It consists of four case studies, each presenting a leadership challenge. These studies of specific situations offer great opportunities to investigate the variety of leading that the academy contains. There is focus, not so much on the task but on the process in which the challenges are positioned, how th

The present paper investigates the ongoing validity of the notion of subordination as selection criteria to allocate the labour protections in the contemporary economic framework. The gig economy is deeply affecting the way of working, transforming the employee in a service provider. This phenomenon is partially due to the progressive shift from a firm-based production model towards a market trans

Causes of egg‐size variation between and within clutches were studied in clutches of the blue tit (Parus caeruleus L.). We measured the mass of each egg in the laying sequence in unmanipulated clutches, in clutches of parents experimentally supplied with extra food before egg‐laying, and in clutches of parents supplemented with extra food after the start of egg‐laying. Hatchlings were weighed at a

In altricial birds, the period of parental investment covers three distinctly separated phases: Incubation, feeding of nestlings, and feeding of fledglings in the family group. The transition between the latter two phases occurs when the brood fledges and leaves the nest. To investigate which party, parents or offspring, initiates nest leaving, different-aged broods were swopped between nestboxes

Although hoarding has been studied intensively for many decades, few studies have attempted to measure its actual fitness consequences. To fill this gap, we used ptilochronology, the growth of replacement feathers as a measure of nutritional status, and thus a reflection of starvation risk, of individual European nuthatches (Sitta europaea) during winter. We found that nuthatches are long-term hoa