Results 111 to 120 of about 403,629 (240)

Allostery: allosteric networks and allosteric signaling bias

Quarterly Reviews of Biophysics
Abstract Allosteric communication is established by networks through which strain energy generated at the allosteric site by an allosteric event, such as ligand binding, can propagate to the functional site. Exerted on multiple molecules in the cell, it can wield a biased function. Here, we discuss
Ruth Nussinov, Bengi R. Yavuz, Hyunbum Jang   +2 more
openaire   +1 more source

In Silico Study of Allosteric Communication Networks in GPCR Signaling Bias. [PDF]

Int J Mol Sci, 2022
Morales-Pastor A, Nerín-Fonz F, Aranda-García D, Dieguez-Eceolaza M, Medel-Lacruz B, Torrens-Fontanals M, Peralta-García A, Selent J.   +7 more
europepmc   +1 more source

A GLP-1 analogue optimized for cAMP-biased signaling improves weight loss in obese mice

Molecular Metabolism
Objective: Glucagon-like peptide 1 (GLP-1) receptor (GLP-1R) agonism is foundational to modern obesity pharmacotherapies. These compounds were engineered for maximal G protein alpha(s) (Gsα) signaling potency and downstream cAMP production. However, this
Jonathan D. Douros, Aaron Novikoff, Barent DuBois, Rebecca Rohlfs, Jacek Mokrosinski, Wouter F.J. Hogendorf, Robert Augustin, Myrte Merkestein, Lene Brandt Egaa Martini, Lars Linderoth, Elliot Gerrard, Janos Tibor Kodra, Jenny Norlin, Nikolaj Kulahin Roed, Anouk Oldenburger, Stephanie A. Mowery, Maria Waldhoer, Diego Perez-Tilve, Brian Finan, Steffen Reedtz-Runge, Timo D. Müller, Patrick J. Knerr   +21 more
doaj   +1 more source

Shrinkage‐based biased signal‐to‐noise ratio estimator using pilot and data symbols for linearly modulated signals [PDF]

, 2015
Chee‐Hyun Park, Soojeong Lee, Joon‐Hyuk Chang   +2 more
openalex   +1 more source

Host-Pathogen Interactions: Evaluating the Role of Complement Receptor 3 in Immune Bias and Macrophage Cell Signaling Modulation During Experimental Cutaneous Leishmaniasis

, 2022
Cristina Ricardo Carter
openalex   +1 more source

Kinetic multiplex assay to assess biased signaling of clinical GPCR agonists

Pharmacological Research
Studying biased signaling of G protein-coupled receptors (GPCRs) holds promise for the identification of ligands with a better therapeutic window. However, proper examination of biased signaling remains challenging by risking introduction of system or ...
Jara Bouma, Elisa J.M. de Koning, Cas van der Horst, Sanjay Sunil Kumar, Barry J.W. van den Berg, Samuel R.J. Hoare, Matthias B. Wittwer, Wolfgang Guba, Arne C. Rufer, Uwe Grether, Mario van der Stelt, Laura H. Heitman   +11 more
doaj   +1 more source

Structural Insights into M1 Muscarinic Acetylcholine Receptor Signaling Bias between Gαq and β-Arrestin through BRET Assays and Molecular Docking. [PDF]

Int J Mol Sci, 2023
Wang D, Yao Y, Wang S, Hou Y, Zhao L, Wang H, Chen H, Xu J.   +7 more
europepmc   +1 more source

Measuring ligand efficacy at the mu-opioid receptor using a conformational biosensor. [PDF]

, 2018
The intrinsic efficacy of orthosteric ligands acting at G-protein-coupled receptors (GPCRs) reflects their ability to stabilize active receptor states (R*) and is a major determinant of their physiological effects.
Livingston, Kathryn E, Mahoney, Jacob P, Manglik, Aashish, Sunahara, Roger K, Traynor, John R   +4 more
core  

Fusion with Promiscuous Gα₁₆ Subunit Reveals Signaling Bias at Muscarinic Receptors. [PDF]

Int J Mol Sci, 2021
Randáková A, Nelic D, Hochmalová M, Zimčík P, Mulenga MJ, Boulos J, Jakubík J.   +6 more
europepmc   +1 more source

Structures of atypical chemokine receptor 3 reveal the basis for its promiscuity and signaling bias. [PDF]

Sci Adv, 2022
Yen YC, Schafer CT, Gustavsson M, Eberle SA, Dominik PK, Deneka D, Zhang P, Schall TJ, Kossiakoff AA, Tesmer JJG, Handel TM.   +10 more
europepmc   +1 more source