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Compartmentalisation of cAMP in Brown Adipocytes
(2022-02-14)
The second messenger, 3',5'-cyclic adenosine monophosphate (cAMP) plays an important role in governing the function and differentiation of brown adipocytes. Upon the stimulation of Gs-coupled G protein-coupled ...
Evaluating onco-geriatric scores and medication risks to improve cancer care for older patients
(2020-03-19)
The cancer therapy of older patients is challenging, being more complex than the therapy of younger patients. Older cancer patients show a higher toxicity risk during therapy and drug-related problems are common. In order ...
Pharmacological reprogramming of macrophages through aptamiRs
(2020-03-05)
Nucleic acid-based molecules have certain advantages over conventional drugs or protein-based target approaches. Chemically synthetized nucleic acids-based molecules are known as aptamers. They are selected from a combinatorial ...
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. ...
Protein and epigenetic biomarkers for variability in epidermal growth factor receptor inhibition in cancer treatment and characterization of the inhibitor-induced skin toxicity in an in vitro model
(2019-01-31)
Epidermal growth factor receptor (EGFR) is often over-expressed or over-activated in cells of solid tumors and can be targeted by specific inhibitors (EGFRIs), like erlotinib, gefitinib, cetuximab and panitumumab. ...
Formulierung von therapeutischen Oligonukleotiden mit PAMAM-Dendrimeren zur Aktivierung von Pattern Recognition Rezeptoren des angeborenen Immunsystems
(2019-05-03)
Der ubiquitär exprimierte Immunrezeptor Retinoic Acid inducible Gene-I, kurz RIG-I, ist eine zytosolisch lokalisierte Helikase, die zur Detektion von pathogenen RNA-Viren befähigt ist. Als synthetischer Ligand konnte eine ......
Dualsterische Liganden, allosterische Agonisten und ein allosterischer Förderer der Agonist-Bindung und -Funktion: Modellgestützte Analysen ihrer Rezeptorinteraktionen, Signalweg-Aktivierungen und -Selektivitäten an Wildtyp und punktmutierten hM1-Rezeptoren in CHO-Zellen
(2018-05-24)
Dualsterische Hybridliganden, bestehend aus einem allosterischen und einem orthosterischen Baustein, die über eine Zwischenkette verbundenen sind, gelten als ideale Werkzeuge zur Entwicklung subtyp- und signalwegselektiver ...
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 ...
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 ...