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Influence of High-Pressure Compaction of Binary Mixtures on Solubility, Dissolution and Wettability of Borderline Poorly Soluble Drugs Employing Standard Excipients
(2021-12-14)
Many of new drug candidates are impaired by low aqueous solubility and slow dissolution rates, which may hinder their pharmacological response. Therefore, there is an increasing need to investigate and implement new ...
Influence of disulfide-bonds on structural and functional properties of peptides and proteins - Case studies on FXIIIa inhibitor tridegin and µ-conotoxin PIIIA
(2021-05-28)
Disulfide-bonded peptides have been studied for many decades serving as tools to investigate various biochemical pathways as well as lead structures for drug development for numerous diseases. Among these, the most fatal ...
Role of Endothelin-1 in the Brown Adipose Tissue
(2021-06-22)
ET-1 was shown to inhibit adipogenesis in murine mesenchymal stem cells derived from new-born brown adipose tissue in vitro and antagonism of Endothelin-1 (ET-1) signaling at the respective level of the Endothelin-1 receptor ...
The role of YAP signaling in thermogenic adiposetissues
(2021-01-02)
One of major metabolic organs, brown adipose tissue (BAT), is responsible for energy expenditure through uncoupling protein 1 (UCP1) mediated non-shivering thermogenesis, which has been considered a promising pharmacological ...
The role of Sphingosine-1-phosphate receptors in adipocytes and adipose tissues
(2021-01-19)
Obesity is a worldwide health issue with increasing numbers of patients every year. Moreover, the prevalence of obesity gives rise to related cardiovascular diseases and various other comorbidities influencing quality of ...
G protein coupled receptors require active Gαq to mobilize Gi-Gβγ-dependent calcium
(2021-06-23)
The mechanisms by which GPCRs drive calcium mobilization in living cells have been a topic of intense research interest for many years. One such mechanism is the paradigmatic Gi-calcium pathway, which describes how Gβγ ...
Bindung, Funktion und Signalwegbevorzugung von orthosterischen, allosterischen und Hybridliganden vermittelt durch Wildtyp und punktmutierte muskarinische hM1-hM5-Rezeptoren
(2021-12-16)
Bislang war ungeklärt, ob der Arzneistoff Methantheliniumbromid (MB) (Vagantin®) mit muskarinischen Acetylcholinrezeptoren (hM-Rezeptoren) interagiert (Teilprojekt 1). In umfassenden Untersuchungen konnte erstmalig ......
The role of beta arrestin 1 in vascular tone regulation of pulmonary arteries
(2021-09-07)
Vascular tone regulation is facilitated by a complex interplay of various constricting and relaxing mechanisms. Excessive vasoconstriction is a prominent symptom of multiple vascular diseases and target of numerous ...
Die biologische Funktion der N1-2´O-Methylierung eukaryotischer mRNA durch die Methyltransferase CMTr1
(2021-05-14)
Eukaryoten modifizieren das 5´-Ende ihrer mRNA mit einem invertierten N7-methyliertem Guanosin (m7G). Diese Cap0 genannte Struktur wird in höheren Eukaryoten durch die Methyltransferase CMTr1 weiter modifiziert: CMTr1 ...
Beeinflussung (steriler) entzündlicher Prozesse in Makrophagen durch lysosomotrope Arzneistoffe
(2021-05-14)
Inflammatorische Reaktionen und chronische Entzündungen sind mitunter die Hauptfaktoren für das Auftreten von Erkrankungen wie Psoriasis, rheumatoider Arthritis oder Morbus Crohn, wobei zahlreiche Komponenten des Immunsystems ......