Developing a Biased Unmatched Bivalent Ligand (BUmBL) Design Strategy to Target the GPCR Homodimer Allosteric Signaling (cAMP over β-Arrestin 2 Recruitment) Within the Melanocortin Receptors.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.8b00238
Abstract: Understanding the functional relevance of G protein-coupled receptor (GPCR) homodimerization has been limited by the insufficient tools to assess asymmetric signaling occurring within dimers comprised of the same receptor type. We present unmatched bivalent ligands… read more here.
Keywords: arrestin recruitment; allosteric signaling; unmatched bivalent; receptor ... See more keywords
Conserved Residues Control the T1R3-Specific Allosteric Signaling Pathway of the Mammalian Sweet-Taste Receptor.
Sign Up to like & getrecommendations! Published in 2019 at "Chemical senses"
DOI: 10.1093/chemse/bjz015
Abstract: Mammalian sensory systems detect sweet taste through the activation of a single heteromeric T1R2/T1R3 receptor belonging to class C G-protein-coupled receptors. Allosteric ligands are known to interact within the transmembrane domain, yet a complete view… read more here.
Keywords: taste receptor; sweet taste; allosteric signaling; conserved residues ... See more keywords
Enhanced specificity mutations perturb allosteric signaling in CRISPR-Cas9
Sign Up to like & getrecommendations! Published in 2021 at "eLife"
DOI: 10.7554/elife.73601
Abstract: CRISPR-Cas9 (clustered regularly interspaced short palindromic repeat and associated Cas9 protein) is a molecular tool with transformative genome editing capabilities. At the molecular level, an intricate allosteric signaling is critical for DNA cleavage, but its… read more here.
Keywords: enhanced specificity; specificity; cas9; crispr cas9 ... See more keywords