The Faculty of Mathematics and Natural Sciences: Search
Now showing items 21-27 of 27
Molecular pharmacological analysis of the human MrgD receptor: New insights into signaling
(2021-08-09)
Introduction: MrgD is a member of the MAS-related GPCRs family. It has been proposed to play roles in nociception and cardiovascular control. MrgD has been shown to couple to Gq, Gi, and Gs proteins. The ...
Investigations into side chain assembly and attachment during biosynthesis of the G protein inhibitor FR900359
(2021-06-07)
The natural product FR900359 (FR) selectively inhibits Gaq proteins and thus intracellular signalling of many G protein-coupled receptors. This unique mechanism of action makes FR an indispensable pharmacological tool to ......
Application of population, physiologically based, and semi-physiological pharmacokinetic modeling to assess sources of pharmacokinetic variability in individual drugs
(2020-06-05)
Large inter- and intra-individual variability in the response of drugs causes difficulties for clinicians to choose appropriate dosing regimens to target their therapeutic range. While underexposure might cause sub-therapeutic ...
Funktionelle Untersuchungen des ABC-Transporters ABCG2
(2021-10-15)
Das Phänomen der Multidrug Resistance (MDR) stellt ein bedeutsames Problem bei der Behandlung von Tumoren mit Chemotherapeutika dar. Die ABC-Transporter ABCB1, ABCC1 und ABCG2 sind an der Entstehung der MDR beteiligt. ...
Synthesis, optimization, and characterization of chromen-4-one and 1,7-phenanthroline derivatives as ligands for the orphan G protein-coupled receptors 35 and 84
(2021-06-21)
G protein-coupled receptors (GPCRs) are ideal drug targets. Their characteristic tissue distribution, marked ligand specificity, and their roles in countless (patho)physiological processes are being exploited by more than ...
Design and Synthesis of A2B- and Dual-Acting A2A/A2B Adenosine Receptor Antagonists
(2020-10-27)
A2A and A2B adenosine receptors (ARs) are novel drug targets in cancer (immuno)therapy. Activation of A2AARs expressed on the surface of many immune cells such as T-lymphocytes and natural ...
Supersaturation and solubilization to enhance the oral bioavailability of poorly soluble drug molecules: A mechanistic understanding of their potential and limitations
(2021-07-28)
The stabilization of the supersaturated state in solution was in the last few decades identified as a suitable strategy to enhance the oral bioavailability of poorly soluble drug molecules. From this point of view, drug ...