91 articles for thisTarget
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Iminoguanidines as Allosteric Inhibitors of the Iron-Regulated Heme Oxygenase (HemO) of Pseudomonas aeruginosa.
University of Maryland
Structure-based design of N-substituted 1-hydroxy-4-sulfamoyl-2-naphthoates as selective inhibitors of the Mcl-1 oncoprotein.
University of Maryland
Small Molecule Inhibitors of Ca(2+)-S100B Reveal Two Protein Conformations.
University of Maryland
BRD4 Structure-Activity Relationships of Dual PLK1 Kinase/BRD4 Bromodomain Inhibitor BI-2536.
University of Maryland
Cyclopropyl-containing positive allosteric modulators of metabotropic glutamate receptor subtype 5.
University of Maryland
Discovery and development of Galeterone (TOK-001 or VN/124-1) for the treatment of all stages of prostate cancer.
University of Maryland
Acyl-2-aminobenzimidazoles: a novel class of neuroprotective agents targeting mGluR5.
University of Maryland
Inhibition by active site directed covalent modification of human glyoxalase I.
University of Maryland
Potent suppression of c-di-GMP synthesis via I-site allosteric inhibition of diguanylate cyclases with 2'-F-c-di-GMP.
University of Maryland
Systematic structure modifications of multitarget prostate cancer drug candidate galeterone to produce novel androgen receptor down-regulating agents as an approach to treatment of advanced prostate cancer.
University of Maryland
Investigations into specificity of azepinomycin for inhibition of guanase: discrimination between the natural heterocyclic inhibitor and its synthetic nucleoside analogues.
University of Maryland
Deconstructing 14-phenylpropyloxymetopon: minimal requirements for binding to mu opioid receptors.
University of Maryland
Studies on ligand binding to histidine triad nucleotide binding protein 1.
University of Maryland
High affinity conformationally constrained nociceptin/orphanin FQ(1-13) amide analogues.
University of Maryland
The influence of esters and carboxylic acids as the N-substituent of opioids. Part 1: Benzomorphans.
University of Maryland
Synthesis and inhibitory activity of oligosaccharide thiazolines as a class of mechanism-based inhibitors for endo-beta-N-acetylglucosaminidases.
University of Maryland
Targeting cytochrome P450 enzymes: a new approach in anti-cancer drug development.
University of Maryland
3-Hydroxy-4-methoxyindolomorphinans as delta opioid selective ligands.
University of Maryland
Inhibition of the bacterial heme oxygenases from Pseudomonas aeruginosa and Neisseria meningitidis: novel antimicrobial targets.
University of Maryland
Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activity, pharmacokinetics, and antitumor activity in the LAPC4 human prostate cancer xenograft model.
University of Maryland
Inhibition of adenosine deaminase by novel 5:7 fused heterocycles containing the imidazo[4,5-e][1,2,4]triazepine ring system: a structure-activity relationship study.
University of Maryland
Synthesis and evaluation of N,N-dialkyl enkephalin-based affinity labels for delta opioid receptors.
University of Maryland
(-)-3 beta-Substituted ecgonine methyl esters as inhibitors for cocaine binding and dopamine uptake.
University of Maryland
Synthesis of substituted 3-carbamoylecgonine methyl ester analogues: irreversible and photoaffinity ligands for the cocaine receptor/dopamine transporter.
University of Maryland
S-(N-aryl-N-hydroxycarbamoyl)glutathione derivatives are tight-binding inhibitors of glyoxalase I and slow substrates for glyoxalase II.
University of Maryland
Synthesis of 3-carbamoylecgonine methyl ester analogues as inhibitors of cocaine binding and dopamine uptake.
University of Maryland
Synthesis of 3-arylecgonine analogues as inhibitors of cocaine binding and dopamine uptake.
University of Maryland
A unique ring-expanded acyclic nucleoside analogue that inhibits both adenosine deaminase (ADA) and guanine deaminase (GDA; guanase): synthesis and enzyme inhibition studies of 4,6-diamino-8H-1-hydroxyethoxymethyl-8-iminoimidazo[4,5-e][1,3]diazepine.
University of Maryland
N-Cyclohexylethyl-N-noroxymorphindole: a mu-opioid preferring analogue of naltrindole.
University of Maryland
Targeting zymogen activation to control the matriptase-prostasin proteolytic cascade.
University of Maryland
Molecular switch controlling the binding of anionic bile acid conjugates to human apical sodium-dependent bile acid transporter.
University of Maryland
The effect of the pyridyl nitrogen position in pyridylpiperazine sigma ligands.
University of Maryland
Identification and validation of human DNA ligase inhibitors using computer-aided drug design.
University of Maryland
Trifluoromethoxyl substituted phenylethylene diamines as high affinity sigma receptor ligands with potent anti-cocaine actions.
University of Maryland
Nitrile analogs of meperidine as high affinity and selective sigma-1 receptor ligands.
University of Maryland
Functionalization of the 6,14-bridge of the orvinols. Part 3: preparation and pharmacological evaluation of 18- and 19-hydroxyl substituted orvinols.
University of Maryland
Synthesis, binding affinity, and inhibitory capacity of cyclodextrin-based multivalent glycan ligands for human galectin-3.
University of Maryland
Discovery and anti-tumor activity of 4-(benzylamino)-6-(3,5-dimethylisoxazol-4-yl)quinolin-2(1H)-one (CG13250), a potent, selective and orally bioavailable BET bromodomain inhibitor.
University of Maryland
Characterization of ATP-independent ERK inhibitors identified through in silico analysis of the active ERK2 structure.
University of Maryland
Design of inhibitors against guanase: synthesis and biochemical evaluation of analogues of azepinomycin.
University of Maryland
Recent applications of covalent chemistries in protein-protein interaction inhibitors.
University of Maryland
Selective inhibition of MCF-7(piGST) breast tumors using glutathione transferase-derived 2-methylene-cycloalkenones.
University of Maryland
Identification of novel extracellular signal-regulated kinase docking domain inhibitors.
University of Maryland
Ethers of 3-hydroxyphenylacetic acid as selective gamma-hydroxybutyric acid receptor ligands.
University of Maryland
Improving the solubility and antileukemia activity of Wnt/β-catenin signaling inhibitors by disrupting molecular planarity.
University of Maryland
Scaffold hopping from indoles to indazoles yields dual MCL-1/BCL-2 inhibitors from MCL-1 selective leads.
University of Maryland
Novel retinoic acid metabolism blocking agents endowed with multiple biological activities are efficient growth inhibitors of human breast and prostate cancer cells in vitro and a human breast tumor xenograft in nude mice.
University of Maryland
Identification and characterization of small molecule inhibitors of the calcium-dependent S100B-p53 tumor suppressor interaction.
University of Maryland
Identification of non-phosphate-containing small molecular weight inhibitors of the tyrosine kinase p56 Lck SH2 domain via in silico screening against the pY + 3 binding site.
University of Maryland
Critical structural motif for the catalytic inhibition of human topoisomerase II by UK-1 and analogs.
University of Maryland
Sensitivity of neuronal nicotinic acetylcholine receptors to the opiate antagonists naltrexone and naloxone: receptor blockade and up-regulation.
University of Maryland
Synthesis and opioid activity of side-chain-to-side-chain cyclic dynorphin A-(1-11) amide analogues cyclized between positions 2 and 5. 1. Substitutions in position 3.
University of Maryland
Effects of the substitution of Phe4 in the opioid peptide [D-Ala8]dynorphin A-(1-11)NH2.
University of Maryland
A novel N-terminal cyclic dynorphin A analogue cyclo(N,5)[Trp(3),Trp(4),Glu(5)] dynorphin A-(1-11)NH(2) that lacks the basic N-terminus.
University of Maryland
Identification of arodyn, a novel acetylated dynorphin A-(1-11) analogue, as a kappa opioid receptor antagonist.
University of Maryland
Solid phase synthesis and evaluation of Tyr-Tic-Phe-Phe(p-NHCOCH(2)Br) ([Phe(p-bromoacetamide)(4)]TIPP), a potent affinity label for delta opioid receptors.
University of Maryland
N-arylalkylpiperidines as high-affinity sigma-1 and sigma-2 receptor ligands: phenylpropylamines as potential leads for selective sigma-2 agents.
University of Maryland
Extended TIP(P) analogues as precursors for labeled delta-opioid receptor ligands.
University of Maryland
Synthesis and evaluation of isothiocyanate-containing derivatives of the delta-opioid receptor antagonist Tyr-Tic-Phe-Phe (TIPP) as potential affinity labels for delta-opioid receptors.
University of Maryland
Role of hydrophobic interactions in binding S-(N-aryl/alkyl-N-hydroxycarbamoyl)glutathiones to the active site of the antitumor target enzyme glyoxalase I.
University of Maryland
Identification of Novel Steroidal Androgen Receptor Degrading Agents Inspired by Galeterone 3β-Imidazole Carbamate.
University of Maryland
A sigma-1 receptor selective analogue of BD1008. A potential substitute for (+)-opioids in sigma receptor binding assays.
University of Maryland
DL5050, a Selective Agonist for the Human Constitutive Androstane Receptor.
University of Maryland
Synthesis and guanase inhibition studies of a novel ring-expanded purine analogue containing a 5:7-fused, planar, aromatic heterocyclic ring system.
University of Maryland
Triazole-Based Inhibitors of the Wnt/β-Catenin Signaling Pathway Improve Glucose and Lipid Metabolisms in Diet-Induced Obese Mice.
University of Maryland
Human constitutive androstane receptor agonist DL5016: A novel sensitizer for cyclophosphamide-based chemotherapies.
University of Maryland
Novel 17-azolyl steroids, potent inhibitors of human cytochrome 17 alpha-hydroxylase-C17,20-lyase (P450(17) alpha): potential agents for the treatment of prostate cancer.
University of Maryland
17-Imidazolyl, pyrazolyl, and isoxazolyl androstene derivatives. Novel steroidal inhibitors of human cytochrome C17,20-lyase (P450(17 alpha).
University of Maryland
Synthesis and evaluation of pregnane derivatives as inhibitors of human testicular 17 alpha-hydroxylase/C17,20-lyase.
University of Maryland
Progress toward B-Cell Lymphoma 6 BTB Domain Inhibitors for the Treatment of Diffuse Large B-Cell Lymphoma and Beyond.
University of Maryland
Synthetic, structural mimetics of the β-hairpin flap of HIV-1 protease inhibit enzyme function.
University of Maryland
Perturbation of the c-Myc-Max protein-protein interaction via synthetic α-helix mimetics.
University of Maryland
Chlorophenylpiperazine analogues as high affinity dopamine transporter ligands.
University of Maryland
Effect of ring-constrained phenylpropyloxyethylamines on sigma receptors.
University of Maryland
Potent inhibition of NTPase/helicase of the West Nile Virus by ring-expanded ("fat") nucleoside analogues.
University of Maryland
Structure-based design and biological evaluation of inhibitors of the pseudomonas aeruginosa heme oxygenase (pa-HemO).
University of Maryland
Identification of Thiourea-Based Inhibitors of the B-Cell Lymphoma 6 BTB Domain via NMR-Based Fragment Screening and Computer-Aided Drug Design.
University of Maryland
Expanding the Cancer Arsenal with Targeted Therapies: Disarmament of the Antiapoptotic Bcl-2 Proteins by Small Molecules.
University of Maryland
d-Amino acid mutation of PMI as potent dual peptide inhibitors of p53-MDM2/MDMX interactions.
University of Maryland
Effect of beta-cyclodextrin charge type on the molecular recognition thermodynamics of reactions with (ferrocenylmethyl)dimethylaminium derivatives.
Nankai University