Background: Understanding the function of FFA2 has been slowed by a lack of selective orthosteric ligands.Results: Residues within FFA2 that dictate the recognition and function of potent and selective orthosteric agonists are described.Conclusion: Key aspects of ligand interaction with the orthosteric binding pocket of FFA2 are defined.Significance: This work will be invaluable in future drug development at the FFA2 receptor.

Background: Differences in ligand potency and selectivity are observed between human and mouse FFA2 and FFA3 orthologs.Results: Potency differences result from differential constitutive activity between species.Conclusion: An “ionic lock” between extracellular loop 2 and the ligand binding pocket regulates constitutive activity.Significance: Understanding species differences in FFA2 and FFA3 function is critical to future studies with these receptors.

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A novel report on microwave assisted synthesis of bright carbon dots (C-dots) using gum arabic (GA) and its use as molecular vehicle to ferry ciprofloxacin hydrochloride, a broad spectrum antibiotic, is reported in the present work. Density gradient centrifugation (DGC) was used to separate different types of C-dots. After careful analysis of the fractions obtained after centrifugation, ciprofloxacin was attached to synthesize ciprofloxacin conjugated with C-dots (Cipro@C-dots conjugate). Release of ciprofloxacin was found to be extremely regulated under physiological conditions. Cipro@C-dots were found to be biocompatible on Vero cells as compared to free ciprofloxacin (1.2 mM) even at very high concentrations. Bare C-dots (∼13 mg mL−1) were used for microbial imaging of the simplest eukaryotic model—Saccharomyces cerevisiae (yeast). Bright green fluorescent was obtained when live imaging was performed to view yeast cells under fluorescent microscope suggesting C-dots incorporation inside the cells. Cipro@C-dots conjugate also showed enhanced antimicrobial activity against both model gram positive and gram negative microorganisms. Thus, the Cipro@C-dots conjugate paves not only a way for bioimaging but also an efficient new nanocarrier for controlled drug release with high antimicrobial activity, thereby serving potential tool for theranostics.