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Novel insights into mechanisms and selectivity of the heterotrimeric G protein inhibitors BIM-46187 and FR900359
(2015-04-24)
Selective silencing of Gα protein subfamilies by small molecules is of great value to explore the contribution of G protein signaling in physiology and disease. It also represents a new opportunity to treat diseases, such ...
Carbon-carbon double-bond shift in the biosynthesis of the antibiotic corallopyronin A: CorJ DH*: a shift domain
(2015-03-13)
Corallopyronin A is a myxobacterial compound, which was isolated in our lab from the strain Corallococcus coralloides B035. It is a potent in vivo active antibiotic, which is currently undergoing preclinical studies. ...
Nanocarrier system for overcoming multidrug resistance in cancer
(2015-02-04)
Of all the cases, majority of cancer patients respond to therapeutic interventions transiently or incompletely. These multidrug resistant (MDR) cancer cases are either resistant to chemotherapy or acquire resistance during ...
Untersuchung des Einflusses des Endocannabinoidsystems auf das Schicksal, die Funktion und die Interaktion kardialer Zellen in vitro und in vivo
(2015-01-19)
Diverse Arbeiten demonstrieren den Einfluss des Endocannabinoidsystems (ECS) auf regulatorische Mechanismen im ischämischen Myokard. Besonders der Cannabinoidrezeptor 2 (CB2R) scheint an diesen Prozessen zu partizipieren ......
New bioactive metabolites from the marine-derived fungus Dichotomomyces cejpii and their pharmacological relevance
(2015-01-13)
Natural products from fungal sources provide an astonishing diversity of bioactive molecules. The secondary metabolite production in fungi is strongly affected by environmental influences and the isolation of fungal strains ......
Mechanistic Study on the Antitumor Potential of the Endocannabinoid Reuptake Inhibitor OMDM-2
(2014-11-11)
Introduction: Endocannabinoid signalling has been shown to be enhanced in several cancer tissues. Previous studies propose that this up-regulation contributes to the inhibition of the cancer cell proliferation by affecting ......
Role of Endothelin-1 in the Brown Adipose Tissue
(2021-06-22)
ET-1 was shown to inhibit adipogenesis in murine mesenchymal stem cells derived from new-born brown adipose tissue in vitro and antagonism of Endothelin-1 (ET-1) signaling at the respective level of the Endothelin-1 receptor ...
Massenspektrometrische Analyse von enzymatisch-chemischen Verdaus zur Detektion vonPhotoaffinitätsmarkierungen des ABC-Transporters P-Glykoprotein
(2015-08-19)
Der ATP-binding cassette (ABC) Transporter P-Glykoprotein (P-gp) stellt den aus medizinischer Sicht wichtigsten humanen ABC-Transporter dar. Aufgrund seiner ubiquitären Expression in Geweben mit Barrierefunktion und ...
Synthesis and structure-activity relationships of α,β-methylene-ADP derivatives: potent and selective ecto-5-nucleotidase inhibitors
(2015-08-19)
Ecto-5'-nucleotidase (ecto-5'-NT, eN, CD73, EC 3.1.3.5) is a member of the group of ecto-nucleotidases which dephosphorylate extracellular nucleotides. eN catalyzes the dephosphorylation of nucleoside monophosphates and ......
Muskarinische M3-Rezeptoren: Einfluss des orthosterischen / allosterischen Epitops Trp 7.35 auf Ligandbindung, Rezeptoraktivierung und Signalweiterleitung
(2015-08-19)
Muskarinische Acetylcholinrezeptoren (M1-M5) sind G-Protein gekoppelte Rezeptoren, die an einer Vielzahl von physiologischen und pathophysiologischen Prozessen beteiligt sind. M1-, M3- und M5-Rezeptoren koppeln vorwiegend ...