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Structural and evolutionary insights into the functioning of glycoprotein hormones and their receptors.
Andrology
January 2025
Department of Biochemistry and Molecular Biophysics, Columbia University, New York, New York, USA.
The neuroendocrine system that comprises the glycoprotein hormones (GpHs) and their receptors is essential for reproduction and metabolism. Each GpH hormone is an αβ heterodimer of cystine-knot proteins and its cognate receptor is a G-protein coupled receptor (GPCR) distinguished by a large leucine-rich-repeat (LRR) extracellular domain that binds the hormone and a class A GPCR transmembrane domain that signals through an associating heterotrimeric G protein. Hence, the receptors are called LRR-containing GPCRs-LGRs.
View Article and Find Full Text PDFLate-Stage Minimal Labeling of Peptides and Proteins for Real-Time Imaging of Cellular Trafficking.
ACS Cent Sci
January 2025
Centre for Inflammation Research, The University of Edinburgh, EH16 4UU Edinburgh, U.K.
The cellular uptake routes of peptides and proteins are complex and diverse, often handicapping therapeutic success. Understanding their mechanisms of internalization requires chemical derivatization with approaches that are compatible with wash-free and real-time imaging. In this work, we developed a new late-stage labeling strategy for unprotected peptides and proteins, which retains their biological activity while enabling live-cell imaging of uptake and intracellular trafficking.
View Article and Find Full Text PDFUnveiling the Redox Characteristics of Rutin Trihydrate-Canvas-Based Sensor for Hydrazine Sensing in Water Samples.
Langmuir
January 2025
Department of Chemistry, Christ University, Bangalore 560029, Karnataka.
The inclusion of redox mediators into electrocatalytic systems facilitates rapid electron shuttling kinetics and boosts the overall catalytic performance of the electrode. This approach overcomes the sluggish reaction dynamics associated with direct electron transfer, which may be impeded by restricted analyte access to the electrode's active sites. In contrast to conventional synthetic redox mediators, naturally sourced phytomolecule rutin trihydrate (RT), extracted from apple juice, offers potential ecological advantages.
View Article and Find Full Text PDFAdvances in cyclotide research: bioactivity to cyclotide-based therapeutics.
Mol Divers
January 2025
Department of Microbiology, Maharshi Dayanand University, Rohtak, Haryana, 124001, India.
Cyclotides are a class of plant-derived cyclic peptides having a distinctive structure with a cyclic cystine knot (CCK) motif. They are stable molecules that naturally play a role in plant defense. Till date, more than 750 cyclotides have been reported among diverse plant taxa belonging to Cucurbitaceae, Violaceae, Rubiaceae, Solanaceae, and Fabaceae.
View Article and Find Full Text PDFDevelopment of novel epoxyketone macrocyclic peptidyl proteasome inhibitors through OPA-mediated one-step cyclization of unprotected peptides.
Bioorg Chem
January 2025
Key Laboratory of Novel Targets and Drug Study for Neural Repair of Zhejiang Province School of Medicine Hangzhou City University China; College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058 Zhejiang Province, China. Electronic address:
Cyclization is a pivotal strategy for enhancing the drug-like characteristics of polypeptides. To develop potent and metabolically stable proteasome inhibitors, we generated a macrocyclic peptide skeleton using a straightforward and efficient cyclization strategy. Subsequent stability assessments confirmed the practicality of this approach.
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