Mathematisch-Naturwissenschaftliche Fakultät: Suche
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A new molecular mechanism to promote protean agonism at a G protein-coupled receptorl
(2017-07-24)
Protean agonists are of great pharmacological interest as their apparent efficacy may change in magnitude and direction depending on the constitutive activity of a receptor. Yet, this intriguing phenomenon has been poorly ...
The orphan G protein-coupled receptor GPR17: its pharmacology and function in recombinant and primary cell expression systems
(2017-04-26)
The reconstitution of myelin sheaths, so called remyelination, represents an innovative therapeutic goal in multiple sclerosis (MS), the most common inflammatory-demyelinating disease of the central nervous system (CNS). ...
Therapeutic concepts: Proposing a new regulatory pathway for combination therapies
(2017-03-24)
Combinations of different medicinal products are widely use in the medical practice and are in fact essential for the treatment of several diseases. The existing regulation for approval of medicinal products offers only a ...
Analysis of the natural product biosynthesis in gliding bacteria using in vitro assays
(2017-01-10)
Natural products are most important in drug discovery and therapy, e.g. more than 80% of antibiotics are derived from microorganisms. Antimicrobial resistance is a global threat and thus an urgent need for new antimicrobial ...
Identification of Potential Biomarkers for Depressive Disorders
(2017-09-29)
The understanding of the individual variability of depressive disorders is in urgent need of improvement which could be accelerated by identification of biomarkers for the diagnosis and treatment individualization of ...
The impact and underlying molecular mechanisms of cell adhesion molecules integrins and syndecans in the cisplatin chemoresistance of melanoma cells
(2019-12-06)
Cancer is a complex, but also devastating disease, which today, more than ever, is present in our lives and society. Practically every person has a close relative or friend, or has been themselves affected by this disease. ...
Assay Development, Identification, Optimization and Pharmacological Characterization of Inhibitors for Ecto-5′-nucleotidase (CD73)
(2019-10-29)
Extracellular ATP acts as a proinflammatory signaling molecule via G protein-coupled P2Y receptors and ATP-gated P2X ion channel receptors. ATP is hydrolyzed by ecto-nucleotidases: In a first step ecto-nucleoside triphosphate ...
Investigation of BCRP-inhibitors using QSAR and machine learning methods
(2019-08-05)
BCRP is the second member of the subfamily G of the ABC transporters. BCRP is involved in several physiological functions, including protection of the human body from xenobiotics. The overexpression of this membrane protein ...
Investigation of Quinazoline Derivatives as Inhibitors of Breast Cancer Resistance Protein (BCRP/ABCG2)
(2018-03-12)
The treatment of cancer with chemotherapeutic drugs is strongly limited by intrinsic or aquired resistance of the cancer cells. This is the main reason of a failure of the therapy. The cellular resistance mostly originates ...
The role of guanine nucleotide exchange factors (GEFs) in EGF-receptor signalling: Screening for a small molecule inhibitor of the Rin1-mediated Rab5 activation
(2018-06-04)
The small GTPase Rab5 is a key regulator of early endosomal trafficking. It functions as a molecular switch that can be activated by guanine nucleotide exchange factors (GEFs) and inactivated via hydrolysis of GTP with the ...