Doornbos, Maarten L.J. Vermond, Sophie C. Lavreysen, Hilde Tresadern, Gary IJzerman, Adriaan P. Heitman, Laura H.
Published in
Biochemical Pharmacology
While many orthosteric ligands have been developed for the mGlu 2 receptor, little is known about their target binding kinetics and how these relate to those of the endogenous agonist glutamate. Here, the kinetic rate constants, i.e. k on and k off , of glutamate were determined for the first time followed by those of the synthetic agonist LY354740...
Radogna, Flavia Diederich, Marc
Published in
Biochemical Pharmacology
Cancer is evading the host's defense mechanisms leading to avoidance of immune destruction. During tumor progression, immune-evading cancer cells arise due to selective pressure from the hypoxic and nutrient-deprived microenvironment. Thus, therapies aiming at re-establishing immune destruction of pathological cells constitute innovating anti-cance...
Doornbos, Maarten L.J. Van der Linden, Ilse Vereyken, Liesbeth Tresadern, Gary IJzerman, Adriaan P. Lavreysen, Hilde Heitman, Laura H.
Published in
Biochemical Pharmacology
Label-free cellular assays using a biosensor provide new opportunities for studying G protein-coupled receptor (GPCR) signaling. As opposed to conventional in vitro assays, integrated receptor-mediated cellular responses are determined in real-time rather than a single downstream signaling pathway. In this study, we examined the potential of a labe...
Diederich, Marc Muller, Florian Cerella, Claudia
Published in
Biochemical pharmacology
Cardiac glycosides (CGs) are approved for the treatment of cardiovascular alterations and their known cellular target is the alpha subunit of the sodium (Na+)/potassium (K+)-ATPase (NKA). Pharmacologically, they represent a well-known generation of drugs for treating cardiovascular problems, thus allowing the investigation of potential dose-depende...
Seidel, Carole Marc Diederich Mazumder, Aloran Kirsch, Gilbert Dicato, Mario Michael Schnekenburger Marie-Hélène Teiten
Published in
Biochemical Pharmacology
Histone deacetylase (HDAC)6 is a unique isoenzyme targeting specific substrates including α-tubulin and heat shock protein (HSP)90. HDAC6 is involved in protein trafficking and degradation, cell shape and migration. Deregulation of HDAC6 activity is associated with a variety of diseases including cancer leading to a growing interest for developing ...
Radogna, Flavia Dicato, Mario Diederich, Marc
Published in
Biochemical pharmacology
Cell death plays an essential role in the development of organs, homeostasis, and cancer. Apoptosis and programmed necrosis are two major types of cell death, characterized by different cell morphology and pathways. Accumulating evidence shows autophagy as a new alternative target to treat tumor resistance. Besides its well-known pro-survival role,...
Bellusci, Giovanna Ciccone, Sarah Marc Diederich Gonfloni, Stefania Iannizzotto, Valentina Maiani, Emiliano
Published in
Biochemical Pharmacology
The tumor suppressor p53 is a transcription factor that regulates key processes. But, the outcomes of the p53 response go beyond its role as a nuclear transcription factor. Sirtuin (SIRT1) regulates p53 functions as transcription factor. At the same time, SIRT1 protects the genome under stress conditions. The link between p53 and SIRT1 responses is...
Ji, Seungwon Kim, Jaemyun Marc Diederich Barbora Orlikova
Published in
Biochemical Pharmacology
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Claudia Cerella Dicato, Mario Marc Diederich
Published in
Biochemical Pharmacology
Cancer cells depend on an altered energy metabolism characterized by increased rates of both glycolysis and glutaminolysis. Accordingly, corresponding key metabolic enzymes are overexpressed or hyperactivated. As a result, this newly acquired metabolic profile determines most other cancer hallmarks including resistance to cell death. Recent finding...
Trécul, Anne Franck Morceau Anthoula Gaigneaux Michael Schnekenburger Dicato, Mario Marc Diederich
Published in
Biochemical Pharmacology
Valproic acid (VPA) exhibits important pharmacological properties but has been reported to trigger side effects, notably on the hematological system. We previously reported that VPA affects hematopoietic homeostasis by inhibiting erythroid differentiation and promoting myeloid and megakaryocyte differentiation. Here, we analyzed the effect of VPA o...
