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Design and Synthesis of Covalent Peptidomimetic Inhibitors for Human Cysteine Cathepsins
(2020-02-07)
The present thesis elucidates the development of (i) a series of small molecule inhibitors reacting in a covalent-irreversible manner with the targeted proteases and (ii) a fluorescently labeled activity-based probe as a ......
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 ...
Chemoinformatics-Driven Approaches for Kinase Drug Discovery
(2020-01-07)
Given their importance for the majority of cell physiology processes, protein kinases are among the most extensively studied protein targets in drug discovery. Inappropriate regulation of their basal levels results in ...
Mechanisms of epileptogenesis in animal models of developmental brain lesions
(2021-11-05)
Developmental brain lesions, including glioneuronal tumors (GNT) and malformations of cortical development (MCD), are among the most common causes for pharmaco-resistant epilepsy. Despite substantial differences, their ...
Evolution of the Activity Cliff Concept and Practical Implications for Compound Design
(2021-07-22)
Entering the “big data” era, a number of different research areas have witnessed an enormous increase in data at an exponential rate. For drug discovery, various publicly available protein structure and compound bioactivity ...
Characterization of cellular functions of the deubiquitinating enzyme OTUD4
(2020-08-10)
Post-translational modification of proteins with ubiquitin influences myriad of cellular processes by affecting protein stability, degradation, localization and protein-protein interactions. Ubiquitin gets transferred to ...
A role of Alzheimer’s disease-associated γ-secretase in lipid metabolism and lipid droplet formation via LXR activation
(2021-06-29)
The γ secretase is an intramembrane protease complex, essential for the processing of a wide variety of type-1 membrane proteins. Among these is the amyloid precursor protein (APP), a protein strongly linked to Alzheimer’s ...
Design, Entwicklung und Herstellung modifizierter gastroretentiver schwimmender Systeme auf Basis von schmelzextrudierten hohlen Zylindermatrices
(2020-04-15)
Die Entwicklung gastroretentiver Arzneiformen ist komplex, da neben der kontrollierten Freisetzung des Wirkstoffs zusätzlich die Verlängerung der Verweilzeit im Magen gewährleistet werden muss. Hierfür werden meist hydrophile ...
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 ...