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Characterization of an orphan G protein-coupled receptor localized in the dorsal root ganglia reveals adenine as a signaling molecule
TLDR
It is demonstrated that adenine functions as a signaling molecule in mammals and adds a third family besides P1 and P2 receptors to the class of purinergic receptors.
Structure of the Human Serotonin 5‐HT4 Receptor Gene and Cloning of a Novel 5‐HT4 Splice Variant
TLDR
The functional characterization of the novel splice variant h, which leads to the insertion of 14 amino acids into the second extracellular loop of the serotonin 5‐HT4 receptor, is concentrated on.
Cloning and Expression of a Human Serotonin 5‐HT4 Receptor cDNA
TLDR
Using a combination of library screening and nested PCR based on a partial human serotonin 5‐ HT4 receptor sequence, the complete coding region for a human 5‐HT4 receptor is cloned and there seem to be at least two possible splice sites in the coding region of the gene.
Preclinical Efficacy of the Novel Monocarboxylate Transporter 1 Inhibitor BAY-8002 and Associated Markers of Resistance
TLDR
In order to address potential acquired resistance mechanisms to MCT1 inhibition, it is shown that resistance can occur by upregulation of MCT4 even in the presence of sufficient oxygen, as well as by shifting energy generation toward oxidative phosphorylation.
Pharmacology of Free Fatty Acid Receptors and Their Allosteric Modulators
TLDR
The molecular pharmacology of FFAR allosteric ligands is discussed, and the opportunities and challenges in research from the perspective of drug discovery are discussed.
The RESOLUTE consortium: unlocking SLC transporters for drug discovery
The Innovative Medicines Initiative Consortium RESOLUTE has started to develop tools and produce data sets to de-orphanize transporters in the solute carrier protein (SLC) superfamily, thereby
Discovery and Characterization of BAY 1214784, an Orally Available Spiroindoline Derivative Acting as a Potent and Selective Antagonist of the Human Gonadotropin-Releasing Hormone Receptor as Proven
TLDR
In a first-in-human study in postmenopausal women, once daily treatment with compound BAY 1214784 effectively lowered plasma luteinizing hormone levels by up to 49%, at the same time being associated with low pharmacokinetic variability and good tolerability.
An Overview of Cell-Based Assay Platforms for the Solute Carrier Family of Transporters
TLDR
This review provides a comprehensive overview of state-of-the-art cellular assay technologies for SLC research and discusses relevant SLC characteristics enabling the choice of an optimal assay technology.
A non-cannabinoid immunogen used to elicit antibodies with broad cross-reactivity to cannabinoid metabolites.
TLDR
The novel benzpyran Immunogen used in this study is the first non-cannabinoid immunogen used to generate cannabinoid-selective antibodies and demonstrates the usefulness of such a structure in developing broadly cross-reactive cannabinoid antibodies.
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