Alastair J. H. Brown

TL;DR: GPR41 is reportedly expressed in murine adipose tissue and mediates short chain fatty acid (SCFA)‐stimulated leptin secretion by activating Gαi, but in the presence of adenosine deaminase to minimise G αi signalling via the adenosines A1 receptor, SCFA stimulated adipocytes from wild‐type but not GPR41 knockout mice.

TL;DR: A review of peptide drugs targeting G protein-coupled receptors (GPCRs) is presented in this paper, with a focus on evolving strategies to improve pharmacokinetic and pharmacodynamic properties.

TL;DR: The use of FBLG is exemplified with case studies in the following drug discovery areas: antibacterial enzyme targets, GPCRs (melanocortin 4 receptor modulators), prostaglandin D2 synthase inhibitors, phosphatase inhibitors (protein tyrosine phosphotase 1B), and protease inhibitors

TL;DR: The third intracellular loop insertion in GPR120L prevents G protein-dependent intrACEllular calcium and DMR responses, but this receptor isoform remains functionally coupled to the β-arrestin pathway, providing one of the first examples of a native β-Arrestin-biased receptor.

TL;DR: This work proposes a model to explain the understanding of how residence time and rebinding might influence sustained signaling by internalized receptors and highlights the anticipated benefit for drug discovery of fully understanding and exploiting these phenomena to target desirable receptor response profiles selectively.