Keywords: [3H]mepyramine PubChem CID 656400; Chlorpheniramine maleate PubChem CID 5281068; Diphenhydramine Pubmed CID 3100; Histamine dihydrochloride PubChem CID 5818; cAMP; cyclic adenosine monophosphate; CDH3; cadherin 3 type 1 P-cadherin gene; ER; endoplasmic re
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2-Formyl-komarovicine promotes adiponectin production in human mesenchymal stem cells through PPARγ partial agonism
Keywords: hBM-MSCs; human bone marrow-derived mesenchymal stem cells; IBMX; isobutylmethylxanthine; IDX; insulin, dexamethasone, IBMX; FABP4; fatty acid binding protein 4; PPAR; peroxisome proliferator-activated receptor; qRT-PCR; quantitative real-time reverse tra
CMHX008, a PPARγ partial agonist, enhances insulin sensitivity with minor influences on bone loss
Keywords: Osteoblasts; Peroxisome proliferator-activated receptor γ; Thiazolidinediones; TR-FRET; Type 2 diabetes mellitus;
Discovery of orally efficacious RORγt inverse agonists. Part 2: Design, synthesis, and biological evaluation of novel tetrahydroisoquinoline derivatives
Keywords: RORγt; retinoic acid receptor-related orphan receptor-gamma t; EAE; experimental autoimmune encephalomyelitis; BODIPY; boron-dipyrromethene; TR-FRET; time-resolved fluorescence resonance energy transfer; SAR; structure-activity relationship; IFN-γ; inte
Discovery and characterization of an iminocoumarin scaffold as an inhibitor of MEKK2 (MAP3K2)
Keywords: MEKK2; MAP3K2; Kinase; Inhibitor; DMSO; dimethyl sulfoxide; MAPK; mitogen-activated protein kinase; MS; mass spectrometry; ATP; adenosine triphosphate; ADP; adenosine diphosphate; SAR; structure-activity relationship; SD; standard deviation; TR-FRET; time
The hypotensive effect of activated apelin receptor is correlated with β-arrestin recruitment
Keywords: 7TMR; seven transmembrane receptor; Akt; protein kinase B; APJ; apelin receptor; βarr; β-arrestin; BRET; bioluminescence resonance energy transfer; cAMP; cyclic adenosine monophosphate; ERK1/2; extra-cellular regulated kinase 1/2; GPCR; G protein-couple
Quercetin preserves redox status and stimulates mitochondrial function in metabolically-stressed HepG2 cells
Keywords: AmA; antimycin A; AMPK; adenosine monophosphate-activated protein kinase; CoQ; coenzyme Q10; DCF; 2â²,7â²-dichlorofluorescin; DCFH-DA; 2â²,7â²-dichlorofluorescin diacetate; ddPCR; droplet digital PCR; ETS; electron transfer system; FBS; fetal bovine s
Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors
Keywords: BET; Bromodomain and Extra-Terminal; BD1; bromodomain 1; BD2; bromodomain 2; KAc; acetylated-lysine; THQ; tetrahydroquinoline; BETi; Bromodomain inhibitors; HAT; histone acetyltransferase; HDAC; histone deacetylase; TR-FRET; time-resolved fluorescence res
Natural products as modulators of the nuclear receptors and metabolic sensors LXR, FXR and RXR
Keywords: Natural products; Nuclear receptors; Liver X receptor; Farnesoid X receptor; Retinoid X receptor; Metabolic syndrome; Precision medicine; 6-ECDCA; 6α-ethyl-chenodeoxycholic acid (obeticholic acid); AA; arachidonic acid; ABC; ATP-binding cassette transpor
Discovery and optimization of benzimidazole derivatives as a novel chemotype of farnesoid X receptor (FXR) antagonists
Keywords: FXR; farnesoid X receptor; CDCA; chenodeoxycholic acid; CYP7A1; cholesterol 7α-hydroxylase; SHP; small heterodimer partner; RXRα; retinoid X receptor α; 9-cis-RA; 9-cis-retinoic acid; LBD; ligand binding domain; TR-FRET; time-resolved fluorescence reso
Studies of CDK 8/19 inhibitors: Discovery of novel and selective CDK8/19 dual inhibitors and elimination of their CYP3A4 time-dependent inhibition potential
Keywords: ADME; absorption, distribution, metabolism, and excretion; AML; acute myelogenous leukemia; AUC; area under the blood concentration time curve; b.i.d.; twice a day; CDK; Cyclin-dependent kinase; CLtotal; clearance; Cmax; maximum drug concentration; CRC; c
Structure of a Myeloid cell leukemia-1 (Mcl-1) inhibitor bound to drug site 3 of Human Serum Albumin
Keywords: Mcl-1; Myeloid cell leukemia 1; HSA; Human Serum Albumin; BSA; Bovine Serum Albumin; FBS; Fetal Bovine Serum; FITC; fluorescein isothiocyanate; TR-FRET; time resolved fluorescence energy transfer; Human Serum Albumin; Free fraction; Apoptosis; Cancer; Mcl
Comparative effect of imatinib and ponatinib on autophagy and miRNome in chronic myeloid leukemia
Keywords: TKI; tyrosine kinase inhibitor; CML; chronic myeloid leukemia; LSC; leukemia stem cells; WST-1; Water Soluble Tetrazolium-1; GFP; Green Florescent Protein; TR-FRET; Time-resolved Fluorescence Energy Transfer; LC3B; light chain 3 B; miRNA; Micro Ribonuclei
Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents
Keywords: Estrogen-related receptor α; ERRα; Nuclear receptor; Anti-diabetic; Metabolic syndrome; Indazole; Thiazolidenedione; TZD; Insulin resistance; ERR; estrogen-related receptor; ER; estrogen receptor; ERE; estrogen response element; ERRE; estrogen-related r
Salicylates are interference compounds in TR-FRET assays
Keywords: Interference compounds; Salicylates; TR-FRET; Assay development; PAINS
Synthesis of 5-trifluoromethyl-2-sulfonylpyridine PPARβ/δ antagonists: Effects on the affinity and selectivity towards PPARβ/δ
Keywords: DWICMVYFMPAZJL-UHFFFAOYSA-N; ZDQUBYIEQLXZGB-UHFFFAOYSA-N; GKZPYWFFVYSYAD-UHFFFAOYSA-NPPAR; Antagonist; Covalent; Selectivity; TR-FRET
Dynamics of ligand binding to GPCR: Residence time of melanocortins and its modulation
Keywords: BBV; budded baculovirus; EDTA; ethylenediaminetetraacetic acid; FA; fluorescence anisotropy; FCS; fluorescence correlation spectroscopy; FRET; Förster/fluorescence resonance energy transfer; GPCR; G protein-coupled receptor; MC; melanocortin; MSH; melano
Lateral diffusion contributes to FRET from lanthanide-tagged membrane proteins
Keywords: GPI-anchored proteins; FRET; GPCR; Diffusion; HTRF; TR-FRET;
TR-FRET binding assay targeting unactivated form of Bruton's tyrosine kinase
Keywords: Bruton's tyrosine kinase; Kinase inhibitor; Screening; Fluorescent probe; TR-FRET;
3-Hydroxyflavone and structural analogues differentially activate pregnane X receptor: Implication for inflammatory bowel disease
Keywords: 3-Hydroxyflavone (PubChem CID: 11349); Galangin (PubChem CID: 5281616); Datiscetin (PubChem CID: 5281610); Kaempferol (PubChem CID: 5280863); Morin (PubChem CID: 5281670); Quercetin dihydrate (PubChem CID: 5284452); Isorhamnetin (PubChem CID: 5281654); Ta
The dipeptide H-Trp-Glu-OH (WE) shows agonistic activity to peroxisome proliferator-activated protein-α and reduces hepatic lipid accumulation in lipid-loaded H4IIE cells
Keywords: WE; H-Trp-Glu-OH; PPARs; peroxisome proliferator-activated proteins; LBD; ligand-binding domain; SPR; surface plasmon resonance; TR-FRET; time-resolved fluorescence resonance energy transfer; FATP4; fatty-acid transport protein 4; ACS; acyl-CoA synthetase
Time-resolved FRET reveals the structural mechanism of SERCA-PLB regulation
Keywords: IAF; 5-iodoacetamidofluorescein; DOPC; 1,2-dioleoyl-sn-glycero-3-phosphocholine; DOPE; 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine; EGTA; ethylene glycol-bis-(2-aminoethylether)-N,N,Nâ²,Nâ²-tetraacetic acid; ESI-MS; electrospray ionization mass spectr
Identification of coregulators influenced by estrogen receptor subtype specific binding of the ER antagonists 4-hydroxytamoxifen and fulvestrant
Keywords: 4OHT; 4-hydroxytamoxifen; ATP; adenosine triphosphate; BSA; bovine serum albumin; CCD; charge coupled device; CDTA; 1,2-diaminocyclohexanetetraacetic acid monohydrate; DCC-FCS; dextran-coated charcoal-treated fetal calf serum; DMEM; Dulbecco's modified
Cell proliferation and modulation of interaction of estrogen receptors with coregulators induced by ERα and ERβ agonists
Keywords: ATP; adenosine triphosphate; BrdU; 5-bromo-2â²-deoxyuridine; BSA; bovine serum albumin; CCD; charge coupled device; CDTA; 1,2-diaminocyclo-hexanetetraacetic acid; CHO; Chinese hamster ovary; DCC-FCS; dextran-coated charcoal-treated fetal calf serum; DMEM
LXR-α antagonist meso-dihydroguaiaretic acid attenuates high-fat diet-induced nonalcoholic fatty liver
Keywords: ABCA1, ABCG1; ATP-binding cassette transporter A1 or G1; AMPK; AMP-activated protein kinase; ACC; acetyl-coenzyme A carboxylase; FAS; fatty acid synthase; HDL; high density lipoprotein; HFD; high fat diet; LBD; ligand binding domain; LXR; liver X receptor
trans-Caryophyllene is a natural agonistic ligand for peroxisome proliferator-activated receptor-α
Keywords: PPAR; peroxisome proliferator-activated receptor; LBD; ligand-binding domain; SPR; surface plasmon resonance; TR-FRET; time-resolved fluorescent resonance energy transfer; TG; triglyceride; HTG; hypertriglyceridemia; RXR; retinoid X receptor; EO; essentia
Kamolonol suppresses angiotensin II-induced stress fiber formation and cellular hypertrophy through inhibition of Rho-associated kinase 2 activity
Keywords: Ang II; angiotensin II; ROCK; Rho-associated kinase; IMAP; immobilized metal affinity for phosphochemicals; TR-FRET; time-resolved fluorescence resonance energy transfer; MYPT; myosin phosphatase; MLC; myosin light chain; DMEM; Dulbecco's modified Eagle
Cyanidin, a natural flavonoid, is an agonistic ligand for liver X receptor alpha and beta and reduces cellular lipid accumulation in macrophages and hepatocytes
Keywords: LXR; liver X receptor; LBD; ligand-binding domain; RXR; retinoid X receptor; KD; equilibrium dissociation constant; EC50; the half maximal effective concentration; SPR; surface plasmon resonance; TR-FRET; time-resolved fluorescent resonance energy transfe
Honokiol: A non-adipogenic PPARγ agonist from nature
Keywords: AMPK; AMP-activated kinase; ANOVA; analysis of variance; ATCC; American type culture collection; BADGE; bisphenol A diglycidyl ether; BMP; bone morphogenic protein 4; BSA; bovine serum albumin; CMCNa; sodium carboxymethyl cellulose; DMEM; Dulbecco's modif
Development of time resolved fluorescence resonance energy transfer-based assay for FXR antagonist discovery
Keywords: FXR; farnesoid X receptor; NRs; nuclear receptors; HTS; high-throughput screen; LBD; ligand-binding domain; TR-FRET; time resolved fluorescence resonance energy transfer;
Anti-HER3 Domain 1 and 3 Antibodies Reduce Tumor Growth by Hindering HER2/HER3 Dimerization and AKT-Induced MDM2, XIAP, and FoxO1 Phosphorylation
Keywords: Ab; antibody; NRG; neuregulin; PBS; phosphate-buffered saline; TR-FRET; time-resolved fluorescence resonance energy transfer; XIAP; X-linked inhibitor of apoptosis; FoxO1; forkhead box O1; MDM2; murine double minute 2; GSK3; glycogen synthase kinase 3;
In vitro and in silico studies on substrate recognition and acceptance of human PKMYT1, a Cdk1 inhibitory kinase
Keywords: Cdk; cyclin dependent kinase; CycB; cyclin B; DTT; Dithiothreitol; eTY; EKIGEGTYGVVYKC; FPIA; fluorescence polarization immunoassay; F5M; fluorescein-5-maleimid; GST; glutathione S-transferase; HEK; human embryonic kidney; MD; molecular dynamics; MPF; mat
Ethyl 2,4,6-trihydroxybenzoate is an agonistic ligand for liver X receptor that induces cholesterol efflux from macrophages without affecting lipid accumulation in HepG2 cells
Keywords: ABC; ATP-binding cassette transporter; FAS; fatty acid synthase; HDL; high-density lipoprotein; LBD; ligand-binding domain; LDL; low-density lipoprotein; LXR; liver X receptor; NPC1L1; Niemann-Pick C1 Like 1; SCD-1; stearoyl-CoA desaturase 1; SPR; surface
Fluorescence resonance energy transfer-based technologies in the study of protein-protein interactions at the cell surface
Keywords: FRET; Protein-protein interactions; Cell surface; GPCR; TIRF; SNAP; TR-FRET;
Mutagenesis and computer modeling studies of a GPCR conserved residue W5.43(194) in ligand recognition and signal transduction for CB2 receptor
Keywords: AC; adenylyl cyclase; BGH; bovine growth hormone; cAMP; Cyclic adenosine monophosphate; CB1; cannabinoid receptor subtype 1; CB2; cannabinoid receptor subtype 2; CNS; central nervous system; DTT; dithiothreitol; GPCR; G protein-coupled receptor; HA; influ
Homogeneous time-resolved fluorescence-based assay to screen for ligands targeting the growth hormone secretagogue receptor type 1a
Keywords: G protein-coupled receptor; Growth hormone secretagogue receptor type 1a; Ghrelin; Tag-lite; HTRF; SNAP-tag; Ligand-binding; TR-FRET
DNA site-specific N3-adenine methylation targeted to estrogen receptor-positive cells
Keywords: FNOTXVZCRJUJHO-UHFFFAOYSA-N; CLFQPILSIJHCDR-VEQMNXKASA-N; DLVFYGTVQDMLBR-VEQMNXKASA-N; N3-methyladenine; DNA damage; Breast cancer; Estrogen receptor; Cell-targeting; Sequence-specific DNA methylation; 3-MeA; N3-methyladenine; 7-MeG; N7-methylguanine; EC5
Bisubstrate fluorescent probes and biosensors in binding assays for HTS of protein kinase inhibitors
Keywords: ARC; adenosine analogue-oligoarginine conjugate; CHO; Chinese Hamster Ovary; EFC; enzyme fragment complementation technology; FA; fluorescence anisotropy; FITC; Fluorescein isothiocyanate; FRET; Förster-resonance energy transfer; GST; glutathione S-tra
Thin solid europium(III) dye layers as donors in time-resolved fluorescence resonance energy transfer assays
Keywords: TR-FRET; Europium; Thin solid surface; Immunoassay;
The CERT antagonist HPA-12: First practical synthesis and individual binding evaluation of the four stereoisomers
Keywords: Sphingolipid; CERT; CIAT; HPA-12; TR-FRET
Time-resolved fluorescence resonance energy transfer and surface plasmon resonance-based assays for retinoid and transthyretin binding to retinol-binding protein 4
Keywords: RBP4; Fenretinide; Diabetes; Macular degeneration; Binding assay; TR-FRET
Time-resolved Förster-resonance-energy-transfer DNA assay on an active CMOS microarray
Keywords: Oligonucleotide microarray; Active microarray; Single-photon avalanche diode; SPAD array; TR-FRET; Quantum dots
A substrate for deubiquitinating enzymes based on time-resolved fluorescence resonance energy transfer between terbium and yellow fluorescent protein
Keywords: Green fluorescent protein; Deubiquitination; TR-FRET
Time-resolved fluorescence resonance energy transfer kinase assays using physiological protein substrates: Applications of terbium–fluorescein and terbium–green fluorescent protein fluorescence resonance energy transfer pairs
Keywords: Green fluorescent protein; Kinase assay; TR-FRET
Identification of coumarin derivatives as a novel class of allosteric MEK1 inhibitors
Keywords: MEK1; Coumarins; Allosteric Inhibitors; TR-FRET; COT; RAF