The Faculty of Mathematics and Natural Sciences: Search
Now showing items 91-100 of 106
Irreversible Antagonists for the Adenosine A2B Receptor
(2022-06-13)
Blockade of the adenosine A2B receptor (A2BAR) represents a potential novel strategy for the immunotherapy of cancer. In the present study, we designed, synthesized, and characterized irreversible A2BAR antagonists based ...
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 ...
Carvedilol-mediated signal transduction at the β2 adrenergic receptor
(2022-07-14)
G protein-coupled receptors (GPCRs) comprise the most prominent family of membrane proteins in the mammalian genome. They are required to relay extracellular cues into a cellular response. The environmental interactions ...
The Role of Inosine in Adipose Tissue Metabolism
(2022-05-02)
During the last decades, obesity has become a pandemic disease, associated with severe comorbidities, and a major problem for health care systems. Obesity results from energy imbalance, when energy intake exceeds energy ......
Targeted therapeutics against cancer and infections Identification and characterization of human ecto-nucleotidase (CD39) and coronaviral protease (Mpro) inhibitors
(2022-09-28)
The main objectives of this thesis were the development, characterization and optimization of enzyme inhibitors (i) for the human ecto-nucleotidase CD39, and (ii) for the main protease of the human-pathogenic coronavirus ...
Computational studies on δ-branch G protein-coupled P2Y and related orphan receptors
(2023-06-26)
G protein-coupled receptors (GPCRs) represent an attractive target for drug development as the modulation of their activity can induce a desired physiological response to treat pathological conditions. Given the knowledge ...
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 ...
Targeted transport of active pharmaceutical ingredients into adipose tissue
(2023-02-21)
(noch nicht zugänglich / not yet accessible)
Functional characterization of Gαi/s proteins and modulation of their activity by linear and cyclic peptides
(2024-01-30)
Heterotrimeric Gαβγ (guanine nucleotide-binding) proteins serve as molecular switches to activate (“switch on”) or inactivate (“switch off”) diverse intracellular signaling cascades in response to stimulated G protein-coupled ...