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Pascal Heitel, Philipp Barbie, Alessia Gambardella, Marta Pinto et autres
The Frontiers in Medicinal Chemistry (FiMC) was held in Münster from March 24 th to 27 th as the largest international Medicinal Chemistry conference in Germany. Welcoming more than 240 participants from around 20 countries, it was a vibrant conference, celebrating the …
de (code pays fourni par la source)
Florian Roßner, Thomas A. Jepps, Bo Hjorth Bentzen, Nathalie Strutz‐Seebohm et autres
ABSTRACT The voltage‐gated potassium channel K V 7.1 (KCNQ1) is essential for cardiac repolarization. Loss‐of‐function mutations prolong the action potential and cause long QT syndrome 1, predisposing to malignant arrhythmias. Pharmacological activators of K V 7.1 are therefore of therapeutic interest. Among …
de, dk (code pays fourni par la source)
Ricardo Köchel, Stefan Wagner, Hans‐Jörg Breyholz, M Schäfers et autres
displayed high accumulation in the tumor tissue with very high tumor-to-background ratios. This PET tracer shows promising imaging characteristics and could serve as a lead compound for next-generation imaging probes targeting FAP.
de, us (code pays fourni par la source)
Nina Schulte-Gauczinski, Judith Schmidt, Jens Köhler, Dirk Schepmann et autres
) = 6.4 nM, 9-fold selectivity) represents the most promising ligand. The highest ligand-lipophilicity efficiency (LLE) was obtained for the secondary cyclohexylmethylamine 3d (LLE = 6.7). However, the highest metabolic stability (phase I metabolism) was determined for the benzylamine 3b (89% intact …
de (code pays fourni par la source)
Héctor Noguera Hurtado, Jurek Hense, Nina Klöpper, Jana Osthues et autres
Long-term activation of NMDA receptors of pancreatic islet-cells increases oxidative stress and alters insulin secretion. Previously, we demonstrated that inhibition of GluN2B-containing NMDA receptors protects against islet-cell death. The aim of our current study was to further characterize the pathways influenced by …
de (code pays fourni par la source)
Lea Flämig, Thomas Schidelko, Luca Blicker, Katharina Hoffmann et autres
Ethylenediamines represent a promising class of κ receptor agonists. Recently, the first ethylenediamine – morphan hybrid 4 with high κ receptor affinity, but poor selectivity over the σ 1 receptor was reported. Herein, the chiral pool synthesis of substituted morphans 19 and …
de (code pays fourni par la source)
Gianluca Civenni, Giada Sandrini, Jessica Merulla, Carola Musumeci et autres
Abstract Cancer stem cells (CSCs) are pervasively present in human cancers and have a fundamental role in treatment failure and disease recurrence. Identifying critical elements that sustain the CSC phenotype may lead to novel strategies for cancer treatment. Here, we provide evidence …
ch, it, de (code pays fourni par la source)
Dirk Schepmann, Bernhard Wünsch
Background/Objectives: Ligands blocking σ1 receptors or NMDA receptors show promising pharmacological properties, such as analgesia or neuroprotection. It had been shown that depending on the stereochemistry and substitution pattern, 1,3-dioxnaes can selectively interact with either σ1 receptors or the phencyclidine binding site …
de (code pays fourni par la source)
Insa Thale, Joana Massa, Elke Naß, Laura Vinnenberg et autres
High Resolution Image Download MS PowerPoint Slide Upregulation of K Ca 3.1 channels was observed in highly aggressive tumor cells, such as non small cell lung cancer cells of the A549 line. In order to visualize K Ca 3.1 channels in these …
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Zigli Abdulai, Natasha Agbo, J Anderson, Faye Astley et autres
High Resolution Image Download MS PowerPoint Slide Neglected tropical diseases (NTDs) make up a diverse group of debilitating illnesses disproportionately affecting impoverished communities in tropical and subtropical regions. Despite their significant global health burden, they are often overshadowed by more prominent diseases, …
Ghana, gb, us, br, de, be, ch (code pays fourni par la source)
Ricardo Köchel, Katrin Schwegmann, Hans‐Jörg Breyholz, Michael Schäfers et autres
Abstract The fibroblast activation protein (FAP) is highly expressed by cancer associated fibroblasts in the microenvironment of tumors. The PET tracer [68Ga]Ga-oncoFAP-DOTAGA (1) is clinically used to detect FAP-positive tumors. In order to improve the imaging properties, fluorinated FAP inhibitors 8, 9, …
de, at, Gabon (code pays fourni par la source)
Ricardo Köchel, Stefan Wagner, Katrin Schwegmann, Michael Schäfers et autres
Radiolabeled probes addressing the fibroblast activation protein (FAP) expressed among others by cancer associated fibroblasts in the microenvironment of tumors emerged as promising drugs for diagnostic imaging and therapy of tumors. 68 Ga-chelator-based FAP inhibitors are clinically used for the diagnosis of …
de (code pays fourni par la source)
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