Results 111 to 120 of about 584,709 (292)
Functional selectivity of GPCR-directed drug action through location bias. [PDF]
, 2017 G-protein-coupled receptors (GPCRs) are increasingly recognized to operate from intracellular membranes as well as the plasma membrane. The β 2 -adrenergic GPCR can activate G s -linked cyclic AMP (G s -cAMP) signaling from endosomes.
Conti, Marco +6 more
core +3 more sources
G Protein–Coupled Receptor Rhodopsin [PDF]
Annual Review of Biochemistry, 2006 The rhodopsin crystal structure provides a structural basis for understanding the function of this and other G protein–coupled receptors (GPCRs). The major structural motifs observed for rhodopsin are expected to carry over to other GPCRs, and the mechanism of transformation of the receptor from inactive to active forms is thus likely conserved ...
openaire +3 more sources
Adverse prognosis gene expression patterns in metastatic castration‐resistant prostate cancer
Molecular Oncology, EarlyView.We aggregated a cohort of 1012 mCRPC tissue samples from 769 patients and investigated the association of gene expression‐based pathways with clinical outcomes. Loss of AR signaling, high proliferation, and a glycolytic phenotype were independently prognostic for poor outcomes, and an adverse transcriptional feature score incorporating these pathways ...
Marina N. Sharifi +26 more
wiley +1 more source
On the role of G protein-coupled receptors oligomerization [PDF]
, 2013 The existence of a supramolecular organization of the G protein-coupled receptor (GPCR) is now being widely accepted by the scientific community.
Ahern, Siobhán +3 more
core +2 more sources
Molecular Oncology, EarlyView.TOMM20 increases cancer aggressiveness by maintaining a reduced state with increased NADH and NADPH levels, oxidative phosphorylation (OXPHOS), and apoptosis resistance while reducing reactive oxygen species (ROS) levels. Conversely, CRISPR‐Cas9 knockdown of TOMM20 alters these cancer‐aggressive traits.
Ranakul Islam +9 more
wiley +1 more source
Representation Learning for Class C G Protein-Coupled Receptors Classification
Molecules, 2018 G protein-coupled receptors (GPCRs) are integral cell membrane proteins of relevance for pharmacology. The complete tertiary structure including both extracellular and transmembrane domains has not been determined for any member of class C GPCRs.
Raúl Cruz-Barbosa +2 more
doaj +1 more source
Genetically Encoded Photo-cross-linkers Map the Binding Site of an Allosteric Drug on a G Protein-Coupled Receptor [PDF]
, 2012 G protein-coupled receptors (GPCRs) are dynamic membrane proteins that bind extracellular molecules to transduce signals. Although GPCRs represent the largest class of therapeutic targets, only a small percentage of their ligand-binding sites are ...
Abrol, Ravinder +5 more
core +1 more source
Molecular Oncology, EarlyView.This study investigates an alternative approach to reactivating the oncosuppressor p53 in cancer. A short peptide targeting the association of the two p53 inhibitors, MDM2 and MDM4, induces an otherwise therapeutically active p53 with unique features that promote cell death and potentially reduce toxicity towards proliferating nontumor cells.
Sonia Valentini +10 more
wiley +1 more source
G protein-coupled receptors: Role in metabolic disorders
Frontiers in Endocrinology, 2022 Luiz F. Barella, Shanu Jain, Sai P. Pydi
doaj +1 more source
Uncovering new disease indications for G-protein coupled receptors and their endogenous ligands
BMC Bioinformatics, 2018 Background The Open Targets Platform integrates different data sources in order to facilitate identification of potential therapeutic drug targets to treat human diseases.
Johannes M Freudenberg +3 more
doaj +1 more source