Novel methods predict equilibrium vapor methanol content during gas hydrate inhibition
Keywords: بازدارنده; Gas hydrate; Inhibitor; Methanol loss; Correlation; ANN
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An acetylcholinesterase-inspired biomimetic toxicity sensor
Keywords: بازدارنده; Acetylcholinesterase; Inhibitor; Biomimetic; Toxicity; Assay; Neurotoxicity
Discovery and pharmacological characterization of SAR707 as novel and selective small molecule inhibitor of stearoyl-CoA desaturase (SCD1)
Keywords: بازدارنده; Stearoyl-CoA desaturase; SCD1; Hexahydro-pyrrolopyrrole; Inhibitor; Zucker diabetic fatty rat; Fatty acid desaturation
Synthesis and evaluation of α-ketotriazoles and α,β-diketotriazoles as inhibitors of Mycobacterium tuberculosis
Keywords: بازدارنده; Inhibitor; α,β-Diketotriazole; Tuberculosis; Oxidation; Cytotoxicity
Identification of small-molecule inhibitors of the human S100B–p53 interaction and evaluation of their activity in human melanoma cells
Keywords: بازدارنده; S100B; p53; Protein–protein interaction; Surface plasomon resonance; Fragment; Inhibitor
Insight into Nek2A activity regulation and its pharmacological prospects
Keywords: بازدارنده; Nek2A; CEP135; C-Nap1; Rootelin; Mst1/Mst2; HSav1; Eg5; Cancer; Inhibitor; Activity regulation; Functional domains
Synthesis and structure–activity relationships for 1-(4-(piperidin-1-ylsulfonyl)phenyl)pyrrolidin-2-ones as novel non-carboxylate inhibitors of the aldo-keto reductase enzyme AKR1C3
Keywords: بازدارنده; Aldo-keto reductase; Inhibitor; Crystal structure; Computer aided drug designAKR, aldo-keto reductase; COX, cyclo-oxygenase; DCM, dichloromethane; DMSO, dimethyl sulfoxide; NADPH, nicotinamide adenine dinucleotide phosphate; NSAID, non-steroidal anti-infl
PI3K/Akt/mTOR pathway inhibitors in the therapy of pancreatic neuroendocrine tumors
Keywords: بازدارنده; Neuroendocrine tumors; Pancreatic; PI3K; Akt; mTOR; Inhibitor
Identification of novel chromenone derivatives as interleukin-5 inhibitors
Keywords: بازدارنده; Chromenone analogs; Inhibitor; Interleukin-5; Eosinophils
Evaluation of potential Myt1 kinase inhibitors by TR-FRET based binding assay
Keywords: بازدارنده; Protein kinase Myt1; Binding assay; Inhibitor; Organic synthesis; DockingBCA, bicinchoninic acid; Cdk1, cyclin dependent kinase 1; CycB, cyclin B; DMSO, dimethylsulfoxide; DTT, dithiothreitol; GGL, glycoglycerolipid; HEK, human embryonic kidney; HR-MS, hi
Synthesis of substituted 2-(β-d-glucopyranosyl)-benzimidazoles and their evaluation as inhibitors of glycogen phosphorylase
Keywords: بازدارنده; C-Glycopyranosyl-formimidate; C-Glycopyranosyl-thioformimidate; 2-C-Glycopyranosyl benzimidazole; Glycogen phosphorylase; Inhibitor
Sequence characterization and immunogenicity of cystatins from the cattle tick Rhipicephalus (Boophilus) microplus
Keywords: بازدارنده; Inhibitor; Cystatin; Tick; Rhipicephalus (Boophilus) microplus
Synthesis and structure–activity relationships of phenyl-substituted coumarins with anti-tubercular activity that target FadD32
Keywords: بازدارنده; Mycobacterium tuberculosis; Coumarin; Structure–activity relationship (SAR); Inhibitor
Ferrocene tripeptide Gly-Pro-Arg conjugates: Synthesis and inhibitory effects on Alzheimer’s Aβ1–42 fibrillogenesis and Aβ-induced cytotoxicity in vitro
Keywords: بازدارنده; Aβ1–42 fibrillogenesis; Ferrocene; GPR; Inhibitor; Cytotoxicity
Hémophilie A acquise. Étude d’une série rétrospective monocentrique de 39 patients
Keywords: بازدارنده; Hémophilie A acquise; Inhibiteur; Facteur VIIIAcquired haemophilia A; Inhibitor; Factor VIII
Identification and characterisation of small-molecule inhibitors of Rv3097c-encoded lipase (LipY) of Mycobacterium tuberculosis that selectively inhibit growth of bacilli in hypoxia
Keywords: بازدارنده; Mycobacterium; Rv3097c; Lipase; Inhibitor; Hypoxia; Latent TB
Synthesis of 2-(β-d-glucopyranosyl)-5-(substituted-amino)-1,3,4-oxa- and -thiadiazoles for the inhibition of glycogen phosphorylase
Keywords: بازدارنده; C-Glycosyl-formaldehyde (thio)semicarbazone; C-Glycosyl-1,3,4-oxadiazole; C-Glycosyl-1,3,4-thiadiazole; Glycogen phosphorylase; Inhibitor
Synthesis of 2-(β-d-glucopyranosylamino)-5-substituted-1,3,4-oxadiazoles for inhibition of glycogen phosphorylase
Keywords: بازدارنده; Semicarbazone; 1,3,4-Oxadiazole; β-d-Glucopyranosyl derivatives; Glycogen phosphorylase; Inhibitor
Synthesis and biological evaluation of 1,3,4-thiadiazole analogues as novel AChE and BuChE inhibitors
Keywords: بازدارنده; 1,3,4-Thiadiazole; Acetylcholinesterase; Butyrylcholinesterase; Inhibitor; Molecular docking; In silico pharmacokineticsLUUBFKSVLSVPHF-UHFFFAOYSA-N; ACIGSJRBBBHKIQ-UHFFFAOYSA-N; RJSYSUGJKUEMIH-UHFFFAOYSA-N; OUYOREWJDHTKEJ-UHFFFAOYSA-N; WTGWMDGYJWJQKS-UHFF
Evodiamine inhibits STAT3 signaling by inducing phosphatase shatterproof 1 in hepatocellular carcinoma cells
Keywords: بازدارنده; Evodiamine; STAT3; SHP-1; HCC; Inhibitor
Sirtuins as emerging anti-parasitic targets
Keywords: بازدارنده; Sirtuin; Protein deacetylase; Inhibitor; Parasite; Disease; Therapy
Epigenetic modification enzymes: catalytic mechanisms and inhibitors
Keywords: بازدارنده; Epigenetic modification; Histone acetylation; Histone methylation; DNA methylation; Catalytic mechanism; Inhibitor
Thermodynamic and Adsorption Behaviour of Medicinal Nitramine as a Corrosion Inhibitor for AISI Steel Alloy in HCl Solution
Keywords: بازدارنده; Steel 4130; Corrosion; Inhibitor; Adsorption isotherm; Temkin
2-Hydroxy-4-methoxy-acetophenone as an environment-friendly corrosion inhibitor for AZ91D magnesium alloy
Keywords: بازدارنده; Magnesium alloy; Inhibitor; Corrosion; Inhibition
Multiple drug resistant mechanisms against darunavir, amprenavir, and nelfinavir of HIV-1 PR
Keywords: بازدارنده; HIV-1 PR; Inhibitor; Resistance; Mutation; Molecular dynamics simulation
Glycogen synthase kinase 3 inhibitor attenuates endotoxin-induced liver injury
Keywords: بازدارنده; Lipopolysaccharide tolerance; Glycogen synthase kinase 3; Inhibitor; Attenuate; Liver injury; Organic protection; Kupffer; Glycogen metabolism; Inflammation; Phagocytosis
Characterization of arylalkylamine N-acetyltransferase from silkmoth (Antheraea pernyi) and pesticidal drug design based on the baculovirus-expressed enzyme
Keywords: بازدارنده; Arylalkylamine N-acetyltransferase (AANAT); Antheraea pernyi; Baculovirus rapid expression system; Inhibitor
Targeting the sphingosine kinase/sphingosine 1-phosphate pathway in disease: Review of sphingosine kinase inhibitors
Keywords: بازدارنده; Sphingolipid; Sphingosine kinase (SK); Sphingosine 1-phosphate (S1P); Inhibitor; Disease; Biomarker
Identification of benzofuran-3-yl(phenyl)methanones as novel SIRT1 inhibitors: Binding mode, inhibitory mechanism and biological action
Keywords: بازدارنده; Benzofuran-3-yl(phenyl)methanones; Binding mode; Deacetylation; Inhibitor; SIRT1
Development of novel molecular probes of the Rio1 atypical protein kinase
Keywords: بازدارنده; RIO kinase; Atypical; Inhibitor; Molecular docking; Ribosome biogenesis; Enzyme–inhibitor complex
Identification and characterization of inhibitors of cytoplasmic 5′-nucleotidase cN-II issued from virtual screening
Keywords: بازدارنده; cN-II; Virtual screening; Enzymatic assay; Inhibitor; Crystallography
Small-molecular, non-peptide, non-ATP-competitive polo-like kinase 1 (Plk1) inhibitors with a terphenyl skeleton
Keywords: بازدارنده; Polo-like kinase; Inhibitor; Small molecule; Terphenyl skeleton; Non-peptide; Non-ATP-competitive
Synthesis, characterization, screening and docking analysis of 4-anilinoquinazoline derivatives as tyrosine kinase inhibitors
Keywords: بازدارنده; Receptor tyrosine kinase; Epidermal growth factor receptor (EGFR); Anilinoquinazoline; Inhibitor; Docking analysis
Rational design of apoptosis signal-regulating kinase 1 inhibitors: Discovering novel structural scaffold
Keywords: بازدارنده; Apoptosis signal-regulating kinase 1; ASK1; Inhibitor; Virtual screening; Compound library; Kinase assayASK1, apoptosis signal-regulating kinase 1; AngII, angiotensin II; eNOS, endothelial nitric oxide synthase; ALS, amyotrophic lateral sclerosis; polyQ,
Synthesis and in vitro biological evaluation of 2,6,9-trisubstituted purines targeting multiple cyclin-dependent kinases
Keywords: بازدارنده; Cyclin-dependent kinase; Inhibitor; Roscovitine; Cancer; Apoptosis; Cell cycleCDK, cyclin-dependent kinase; DIAD, diisopropyldiazadicarboxylate; NMP, N-methylpyrrolidone; PARP, poly(ADP-ribose)polymerase; TLC, thin layer chromatography
Synthesis and evaluation of 5′-modified thymidines and 5-hydroxymethyl-2′-deoxyuridines as Mycobacterium tuberculosis thymidylate kinase inhibitors
Keywords: بازدارنده; Mycobacterium tuberculosis; Thymidine monophosphate kinase; Inhibitor; Nucleoside analogues; 5-Hydroxymethyl pyrimidines; Phosphate bioisosteres
Development of small-molecule P-gp inhibitors of the N-benzyl 1,4-dihydropyridine type: Novel aspects in SAR and bioanalytical evaluation of multidrug resistance (MDR) reversal properties
Keywords: بازدارنده; Structure–activity relationships (SAR); Multidrug resistance (MDR); P-glycoprotein (P-gp); Inhibitor; Efflux pump inhibition
Aberrant signalling by protein kinase CK2 in imatinib-resistant chronic myeloid leukaemia cells: Biochemical evidence and therapeutic perspectives
Keywords: بازدارنده; Chronic myeloid leukaemia; CK2; Bcr-Abl; Imatinib-resistance; Inhibitor
Pruritus in patients treated with targeted cancer therapies: Systematic review and meta-analysis
Keywords: بازدارنده; Bcr-Abl; cancer; CD20; epidermal growth factor receptor; inhibitor; itch; mammalian target of rapamycin; pruritus; Raf; vascular endothelial growth factor receptorAE, adverse events; CD20, B-lymphocyte antigen cluster of differentiation 20; CI, confidence
Metal complexes as inhibitors of transcription factor activity
Keywords: بازدارنده; Transcription factor; Metal complex; Inhibitor; Protein; DNA
Synthesis and SAR study of new thiazole derivatives as vascular adhesion protein-1 (VAP-1) inhibitors for the treatment of diabetic macular edema
Keywords: بازدارنده; VAP-1; Inhibitor; Macular edema; Thiazole; Guanidine
The development of a new class of inhibitors for betaine-homocysteine S-methyltransferase
Keywords: بازدارنده; BHMT; Inhibitor; Homocysteine; Phosphonate; Phosphinate; Amino acid derivative; Bioisostere; S-Alkylated homocysteineBHMT, betaine-homocysteine S-methyltransferase; Boc, tert-butoxycarbonyl; Boc2O, di-tert butyl dicarbonate; CDI, 1,1′-carbonyldiimidazole;
Inhibition of VEGF transcription through blockade of the hypoxia inducible factor-1α–p300 interaction by a small molecule
Keywords: بازدارنده; HIF-1α–p300 interaction; VEGF; Inhibitor; Fluorescence polarization; Protein–protein interaction
Verrulactones A and B, new inhibitors of Staphylococcus aureus enoyl-ACP reductase produced by Penicillium verruculosum F375
Keywords: بازدارنده; FabI; Enoyl-ACP reductase; Staphylococcus aureus; Penicillium verruculosum; Inhibitor
Discovery of novel P3-oxo inhibitor of hepatitis C virus NS3/4A serine protease
Keywords: بازدارنده; HCV; HCV protease; HCV protease inhibitor; Inhibitor
Inhibition of beta-carbonic anhydrases from the bacterial pathogen Brucella suis with inorganic anions
Keywords: بازدارنده; Carbonic anhydrase; Anion; Beta-class enzyme; Inhibitor; Brucella suis
Elevation of cellular O-GlcNAcylation level by a potent and selective O-GlcNAcase inhibitor based on tetrahydroimidazopyridine scaffold
Keywords: بازدارنده; O-GlcNAc; O-GlcNAcase; Inhibitor; Selectivity;
Orally available pyridinylpyrimidine derivatives as novel RANKL-induced osteoclastogenesis inhibitors
Keywords: بازدارنده; RANKL; Inhibitor; Osteoclastogenesis; Pyrimidine; Benzyl;
Isomannide derivatives as new class of inhibitors for human kallikrein 7
Keywords: بازدارنده; Serine protease; Kallikrein; Pseudo-peptide; Inhibitor; Molecular dynamics;
2-Substituted 4,5-dihydrothiazole-4-carboxylic acids are novel inhibitors of metallo-β-lactamases
Keywords: بازدارنده; Metallo-β-lactamase; Inhibitor; Rational design; Molecular modeling;