Molecular Mechanism of the Arrestin-Biased Agonism of Neurotensin Receptor 1 by an Intracellular Allosteric Modulator

Chemistry, Medicinal Chemistry, Medicine, Basic Medical Sciences, Pharmacy, Life Sciences, Biochemistry,
G protein-coupled receptors   allosteric modulators   arrestin-biased agonism   neurotensin receptor 1   cryo-EM structures   signal transduction   drug discovery  

Academic Background G protein-coupled receptors (GPCRs) are the most abundant family of cell surface receptors in the human body and are also the most common targets of FDA-approved drugs. GPCRs play a crucial role in the treatment of various diseases, including pain, diabetes, cardiovascular diseases, and cancer. However, drug development targetin...

Cryptoic Acids A and B, Benzene-Containing Polyketides, and Cyclocryptamide, a Modified Diketopiperazine, from an Actinomycete of the Genus Cryptosporangium

Chemistry, Organic Chemistry, Medicinal Chemistry, Life Sciences, Biochemistry, Microbiology,
Cryptosporangium   polyketides   diketopiperazine   biological activity   actinomycetes   natural products   drug discovery  

Novel Benzene-Containing Polyketides and Modified Diketopiperazine from Actinomycete of the Genus Cryptosporangium Academic Background Microbial natural products hold significant value in drug development, particularly actinomycetes, which provide a rich source of various therapeutic compounds, such as aminoglycosides, macrolides, and tetracyclines...

Conformation- and Activation-Based BRET Sensors Differentially Report on GPCR-G Protein Coupling

Medicine, Life Sciences, Cell Biology, Biochemistry, Biophysics,
GPCR   G protein   signaling   BRET sensors   conformational changes   downstream effectors   drug discovery  

Differential Study of GPCR-G Protein Coupling Biosensors Background Introduction G protein-coupled receptors (GPCRs) are important molecules for transmembrane signal transduction, capable of selectively binding to heterotrimeric G proteins composed of Gα, Gβ, and Gγ subunits and regulating various intracellular signaling processes. Studying the fun...