Results 101 to 110 of about 5,480,727 (338)
Structural and Functional Analysis of a β2-Adrenergic Receptor Complex with GRK5. [PDF]
The phosphorylation of agonist-occupied G-protein-coupled receptors (GPCRs) by GPCR kinases (GRKs) functions to turn off G-protein signaling and turn on arrestin-mediated signaling.
Adams, Christopher M.+12 more
core +2 more sources
From omics to AI—mapping the pathogenic pathways in type 2 diabetes
Integrating multi‐omics data with AI‐based modelling (unsupervised and supervised machine learning) identify optimal patient clusters, informing AI‐driven accurate risk stratification. Digital twins simulate individual trajectories in real time, guiding precision medicine by matching patients to targeted therapies.
Siobhán O'Sullivan+2 more
wiley +1 more source
Cryo-EM structure of the adenosine A2A receptor coupled to an engineered heterotrimeric G protein
The adenosine A2A receptor (A2AR) is a prototypical G protein-coupled receptor (GPCR) that couples to the heterotrimeric G protein GS. Here, we determine the structure by electron cryo-microscopy (cryo-EM) of A2AR at pH 7.5 bound to the small molecule ...
Javier García-Nafría+4 more
doaj +1 more source
The anabolic steroid stanozolol is a potent inhibitor of human MutT homolog 1
MutT homolog 1 (MTH1) is a member of the NUDIX superfamily of enzymes and is an anticancer drug target. We show that stanozolol (Stz), an anabolic steroid, is an unexpected nanomolar inhibitor of MTH1. The X‐ray crystal structure of the human MTH1–Stz complex reveals a unique binding scaffold that could be utilized for future inhibitor development ...
Emma Scaletti Hutchinson+7 more
wiley +1 more source
Intrinsic Gating Properties of a Cloned G Protein-activated Inward Rectifier K^+ Channel [PDF]
The voltage-, time-, and K^+-dependent properties of a G protein-activated inwardly rectifying K^+ channel (GIRK1/KGA/Kir3.1) cloned from rat atrium were studied in Xenopus oocytes under two-electrode voltage clamp. During maintained G protein activation
Davidson, Norman+4 more
core +1 more source
Tuberculosis remains a global health challenge and new therapeutic targets are required. Here, we characterized SseA, a sulfurtransferase from Mycobacterium tuberculosis involved in macrophage infection, and its interaction with the newly identified protein SufEMtb that activates SseA enzymatic activity.
Giulia Di Napoli+10 more
wiley +1 more source
Co-expression of Gbeta 5 Enhances the Function of Two Ggamma Subunit-like Domain-containing Regulators of G Protein Signaling Proteins [PDF]
Regulators of G protein signaling (RGS) stimulate the GTPase activity of G protein Galpha subunits and probably play additional roles. Some RGS proteins contain a Ggamma subunit-like (GGL) domain, which mediates a specific interaction with Gbeta 5. The
Chen, Ching-Kang+5 more
core
A new target for G protein signaling
G protein-coupled receptor stimulation inhibits TRPM3 channel activity through direct binding of the Gβγ subunit to the channel.
László Csanády
doaj +1 more source
Mechanisms and kinetic assays of aminoacyl‐tRNA synthetases
FEBS Letters, EarlyView.
Igor Zivkovic+2 more
wiley +1 more source