Results 91 to 100 of about 83,092 (356)
Advanced Science, EarlyView.TarPass provides a rigorous benchmark for target‐aware de novo molecular generation by jointly evaluating protein‐ligand interactions, molecular plausibility, and drug‐likeness on 18 well‐studied targets. Results show that current models often fail to consistently surpass random baseline in target‐specific enrichment, while post hoc multi‐tier virtual ...
Rui Qin +11 more
wiley +1 more source
JCI Insight, 2021 GPCRs are highly desirable drug targets for human disease. Although GPCR dysfunction drives development and progression of many tumors, including breast cancer (BC), targeting individual GPCRs has limited efficacy as a cancer therapy because numerous ...
Cancan Lyu +5 more
doaj +1 more source
Advanced Science, EarlyView.Ovarian macrophage depletion reverses OHSS resistance in estrildid finches and exacerbates OHSS symptoms in rats. Activating macrophage GPR183 alleviates OHSS by reducing pro‐inflammatory factors, increasing immunomodulatory molecules, remodeling CD44/SDC4‐mediated communication, and restoring immune homeostasis.
Xiaofei Yan +11 more
wiley +1 more source
eLifeDeep Mutational Scanning (DMS) is an emerging method to systematically test the functional consequences of thousands of sequence changes to a protein target in a single experiment.
Conor J Howard +17 more
doaj +1 more source
TBXA2R gene variants associated with bleeding
Platelets, 2018 Platelet activity is regulated by a number of surface expressed G protein-coupled receptors (GPCRs) including the α isoform of the thromboxane receptor (TPα receptor). With the advance of genomic technologies, there has been a substantial increase in the
Stuart James Mundell, Andrew Mumford
doaj +1 more source
Physicochemical properties of amino acid sequences of G-proteins for understanding GPCR-G-protein coupling [PDF]
, 2006 A G-protein binds to a G-protein-coupled-receptor (GPCR) by physical interactions between the amino acid sequences. Various physical properties of possible binding regions at the C-and N-termini of the α subunits of G-proteins were analyzed in order to ...
美宅, 成樹 +11 more
core
GPCR Synonyms (GO:0004930) and terms associated with GPCR activity.
, 2017 GPCR Synonyms (GO:0004930) and terms associated with GPCR activity.
Ming-Ying Leung (76155) +4 more
core +1 more source
Stage‐Specific H3K14 and H3K23 Succinylation Orchestrates Insect Metamorphosis and Oogenesis
Advanced Science, EarlyView.Stage‐specific succinylation of histone H3 at lysine 14 and 23 differentially controls insect metamorphosis and oogenesis through distinct GPCR‐PKC signaling cascades, revealing an evolutionarily conserved epigenetic mechanism that coordinates key life‐history traits.
Yu‐Pu Jing +9 more
wiley +1 more source
Multicomponent Stapling of Glucagon‐Like Peptide‐1 Enables Receptor‐Guided PROTAC Delivery
Angewandte Chemie, EarlyView.We report a stapled glucagon‐like peptide‐1 (GLP‐1) analogue created via multicomponent tryptophan‐mediated Petasis reaction (TMPR). This strategy yields a stabilised peptide with superior helicity and improved potency. Conjugation to a bromodomain‐containing protein 4 (BRD4) degrader creates the first GLP‐1‐guided targeted protein degrader (PROTAC ...
Jan L. Venne +5 more
wiley +2 more sources
Advanced Science, EarlyView.SMarT‐Diff introduces a multi‐objective generative paradigm that integrates scaffold hopping with structure‐aware scoring to enable controlled exploration beyond the training distribution. The framework consistently balances drug‐likeness, synthesizes accessibility and bioactivity, yielding chemically diverse candidates with enhanced properties.
Yuwei Yang +8 more
wiley +1 more source