106 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
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Article Title
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Probing the Hydrophobic Binding Pocket of G-Protein-Coupled Lysophosphatidylserine Receptor GPR34/LPS
The University of Tokyo
Design and Synthesis of Potent and Selective PIM Kinase Inhibitors by Targeting Unique Structure of ATP-Binding Pocket.
The University of Tokyo
Three new cyclostellettamines, which inhibit histone deacetylase, from a marine sponge of the genus Xestospongia.
The University of Tokyo
Tokaramide A, a new cathepsin B inhibitor from the marine sponge Theonella aff. mirabilis.
The University of Tokyo
Discovery of N-(1-(3-(4-phenoxyphenyl)-1,2,4-oxadiazol-5-yl)ethyl)acetamides as novel acetyl-CoA carboxylase 2 (ACC2) inhibitors with peroxisome proliferator-activated receptora/d (PPARa/d) dual agonistic activity.
The University of Tokyo
Conformational Constraint of the Glycerol Moiety of Lysophosphatidylserine Affords Compounds with Receptor Subtype Selectivity.
The University of Tokyo
Development of a potent and selective FLT3 kinase inhibitor by systematic expansion of a non-selective fragment-screening hit.
The University of Tokyo
Altered activity profile of a tertiary silanol analog of multi-targeting nuclear receptor modulator T0901317.
The University of Tokyo
Styrylphenylphthalimides as Novel Transrepression-Selective Liver X Receptor (LXR) Modulators.
The University of Tokyo
Discovery and structure-activity relationship studies of N6-benzoyladenine derivatives as novel BRD4 inhibitors.
The University of Tokyo
Structure-activity relationships of lysophosphatidylserine analogs as agonists of G-protein-coupled receptors GPR34, P2Y10, and GPR174.
The University of Tokyo
Design and synthesis of novel ROR inverse agonists with a dibenzosilole scaffold as a hydrophobic core structure.
The University of Tokyo
Lower homologues of ahpatinin, aspartic protease inhibitors, from a marine Streptomyces sp.
The University of Tokyo
Structure-activity relationships of oxysterol-derived pharmacological chaperones for Niemann-Pick type C1 protein.
The University of Tokyo
Design, synthesis and structure-activity relationship studies of novel sirtuin 2 (SIRT2) inhibitors with a benzamide skeleton.
The University of Tokyo
Structure-activity relationship-guided development of retinoic acid receptor-related orphan receptor gamma (ROR¿)-selective inverse agonists with a phenanthridin-6(5H)-one skeleton from a liver X receptor ligand.
The University of Tokyo
Design and synthesis of silicon-containing steroid sulfatase inhibitors possessing pro-estrogen antagonistic character.
The University of Tokyo
Development of novel silicon-containing inverse agonists of retinoic acid receptor-related orphan receptors.
The University of Tokyo
Structure-activity relationship studies of Niemann-Pick type C1-like 1 (NPC1L1) ligands identified by screening assay monitoring pharmacological chaperone effect.
The University of Tokyo
Structure-activity relationships of bisphenol A analogs at estrogen receptors (ERs): discovery of an ERa-selective antagonist.
The University of Tokyo
Development of silicon-containing bis-phenol derivatives as androgen receptor antagonists: selectivity switching by C/Si exchange.
The University of Tokyo
Identification of small-molecule inhibitors of the human S100B-p53 interaction and evaluation of their activity in human melanoma cells.
The University of Tokyo
Incorporation of rapid thermodynamic data in fragment-based drug discovery.
The University of Tokyo
Structure-activity relationship of benzodiazepine derivatives as LXXLL peptide mimetics that inhibit the interaction of vitamin D receptor with coactivators.
The University of Tokyo
Small-molecular, non-peptide, non-ATP-competitive polo-like kinase 1 (Plk1) inhibitors with a terphenyl skeleton.
The University of Tokyo
Characterization of the efflux transport of 17beta-estradiol-D-17beta-glucuronide from the brain across the blood-brain barrier.
The University of Tokyo
Effect of 17 beta-estradiol-D-17 beta-glucuronide on the rat organic anion transporting polypeptide 2-mediated transport differs depending on substrates.
The University of Tokyo
Design, synthesis, and biological evaluation of novel transrepression-selective liver X receptor (LXR) ligands with 5,11-dihydro-5-methyl-11-methylene-6H-dibenz[b,e]azepin-6-one skeleton.
The University of Tokyo
Rational evolution of a novel type of potent and selective proviral integration site in Moloney murine leukemia virus kinase 1 (PIM1) inhibitor from a screening-hit compound.
The University of Tokyo
Transport activity of human MRP3 expressed in Sf9 cells: comparative studies with rat MRP3.
The University of Tokyo
Characterization of bile acid transport mediated by multidrug resistance associated protein 2 and bile salt export pump.
The University of Tokyo
E297G mutated bile salt export pump (BSEP) function enhancers derived from GW4064: structural development study and separation from farnesoid X receptor-agonistic activity.
The University of Tokyo
Application of a 3,3-diphenylpentane skeleton as a multi-template for creation of HMG-CoA reductase inhibitors.
The University of Tokyo
Cyclotheonamides E2 and E3, new potent serine protease inhibitors from the marine sponge of the genus Theonella.
The University of Tokyo
Synthesis of the novel analogues of dysidiolide and their structure-activity relationship.
The University of Tokyo
Peroxisome proliferator-activated receptors (PPARs) have multiple binding points that accommodate ligands in various conformations: phenylpropanoic acid-type PPAR ligands bind to PPAR in different conformations, depending on the subtype.
The University of Tokyo
Gliotoxin analogues from a marine-derived fungus, Penicillium sp., and their cytotoxic and histone methyltransferase inhibitory activities.
The University of Tokyo
Peroxisome proliferator-activated receptor agonists with phenethylphenylphthalimide skeleton derived from thalidomide-related liver X receptor antagonists: relationship between absolute configuration and subtype selectivity.
The University of Tokyo
Improvement in aqueous solubility in small molecule drug discovery programs by disruption of molecular planarity and symmetry.
The University of Tokyo
Non-competitive and selective dipeptidyl peptidase IV inhibitors with phenethylphenylphthalimide skeleton derived from thalidomide-relateda-glucosidase inhibitors and liver X receptor antagonists.
The University of Tokyo
Improvement of water-solubility of biarylcarboxylic acid peroxisome proliferator-activated receptor (PPAR)d-selective partial agonists by disruption of molecular planarity/symmetry.
The University of Tokyo
LXXLL peptide mimetics as inhibitors of the interaction of vitamin D receptor with coactivators.
The University of Tokyo
Novel biphenylcarboxylic acid peroxisome proliferator-activated receptor (PPAR) delta selective antagonists.
The University of Tokyo
beta-Naphthoflavone analogs as potent and soluble aryl hydrocarbon receptor agonists: improvement of solubility by disruption of molecular planarity.
The University of Tokyo
Separation of alpha-glucosidase-inhibitory and liver X receptor-antagonistic activities of phenethylphenyl phthalimide analogs and generation of LXRalpha-selective antagonists.
The University of Tokyo
Axial chirality and affinity at the GABA(A) receptor of pyrimido[1,2-a][1,4]benzodiazepines and related compounds.
The University of Tokyo
Improvement of the transactivation activity of phenylpropanoic acid-type peroxisome proliferator-activated receptor pan agonists: effect of introduction of fluorine at the linker part.
The University of Tokyo
Progesterone receptor antagonists with a 3-phenylquinazoline-2,4-dione/2-phenylisoquinoline-1,3-dione skeleton.
The University of Tokyo
4-(Anilino)pyrrole-2-carboxamides: Novel non-steroidal/non-anilide type androgen antagonists effective upon human prostate tumor LNCaP cells with mutated nuclear androgen receptor.
The University of Tokyo
Development of a novel fluorescent probe for fluorescence correlation spectroscopic detection of kinase inhibitors.
The University of Tokyo
Demonstration of direct binding of cIAP1 degradation-promoting bestatin analogs to BIR3 domain: Synthesis and application of fluorescent bestatin ester analogs.
The University of Tokyo
Degradation-promoters of cellular inhibitor of apoptosis protein 1 based on bestatin and actinonin.
The University of Tokyo
3,3-diphenylpentane skeleton as a steroid skeleton substitute: novel inhibitors of human 5alpha-reductase 1.
The University of Tokyo
Design, synthesis, and evaluation of isoindolinone-hydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
The University of Tokyo
Switching Lysophosphatidylserine G Protein-Coupled Receptor Agonists to Antagonists by Acylation of the Hydrophilic Serine Amine.
The University of Tokyo
Ligands with dual vitamin D3-agonistic and androgen-antagonistic activities.
The University of Tokyo
Building on endogenous lipid mediators to design synthetic receptor ligands.
The University of Tokyo
Design and synthesis of novel Cdc25A-inhibitors having phosphate group as a hydrophilic residue.
The University of Tokyo
Design and synthesis of dysidiolide analogs from vitamin D3: novel class of Cdc25A inhibitors.
The University of Tokyo
Anti-androgens with full antagonistic activity toward human prostate tumor LNCaP cells with mutated androgen receptor.
The University of Tokyo
Non-naturally Occurring Regio Isomer of Lysophosphatidylserine Exhibits Potent Agonistic Activity toward G Protein-Coupled Receptors.
The University of Tokyo
Bisphosphonate esters interact with HMG-CoA reductase membrane domain to induce its degradation.
The University of Tokyo
Fluorescent bioprobes for visualization of puromycin-sensitive aminopeptidase in living cells.
The University of Tokyo
Hydrophobic modifications at 1-phosphate of inositol 1,4,5-trisphosphate analogues enhance receptor binding.
The University of Tokyo
Phosphine boranes as less hydrophobic building blocks than alkanes and silanes: Structure-property relationship and estrogen-receptor-modulating potency of 4-phosphinophenol derivatives.
The University of Tokyo
Luciferase-based HMG-CoA reductase degradation assay for activity and selectivity profiling of oxy(lano)sterols.
The University of Tokyo
Structure-activity relationship studies of non-carboxylic acid peroxisome proliferator-activated receptor α/δ (PPARα/δ) dual agonists.
The University of Tokyo
Structure-activity relationship study of estrogen receptor down-regulators with a diphenylmethane skeleton.
The University of Tokyo
Synthesis and evaluation of 1-position-modified inositol 1,4,5-trisphosphate analogs.
The University of Tokyo
Rationally Designed Small-Molecule Inhibitors Targeting an Unconventional Pocket on the TLR8 Protein-Protein Interface.
The University of Tokyo
Phenanthridin-6-one derivatives as the first class of non-steroidal pharmacological chaperones for Niemann-Pick disease type C1 protein.
The University of Tokyo
Design and synthesis of an in vivo-efficacious PIM3 kinase inhibitor as a candidate anti-pancreatic cancer agent.
The University of Tokyo
Design and synthesis of silicon-containing tubulin polymerization inhibitors: replacement of the ethylene moiety of combretastatin A-4 with a silicon linker.
The University of Tokyo
Involvement of multispecific organic anion transporter, Oatp14 (Slc21a14), in the transport of thyroxine across the blood-brain barrier.
The University of Tokyo
Charged amino acids in the transmembrane domains are involved in the determination of the substrate specificity of rat Mrp2.
The University of Tokyo
Shishicrellastatins, inhibitors of cathepsin B, from the marine sponge Crella (Yvesia) spinulata.
The University of Tokyo
Sodium 1-(12-hydroxy)octadecanyl sulfate, an MMP2 inhibitor, isolated from a tunicate of the family Polyclinidae.
The University of Tokyo
Callysponginol sulfate A, an MT1-MMP inhibitor isolated from the marine sponge Callyspongia truncata.
The University of Tokyo
Nobiloside, a new neuraminidase inhibitory triterpenoidal saponin from the marine sponge Erylus nobilis.
The University of Tokyo
Aeruginosin 103-A, a thrombin inhibitor from the cyanobacterium Microcystis viridis.
The University of Tokyo
Dehydroradiosumin, a trypsin inhibitor from the cyanobacterium Anabaena cylindrica.
The University of Tokyo
Isolation of 1-carboxymethylnicotinic acid from the marine sponge anthosigmella cf. raromicrosclera As a cysteine protease inhibitor1
The University of Tokyo
New anabaenopeptins, potent carboxypeptidase-A inhibitors from the cyanobacterium Aphanizomenon flos-aquae.
The University of Tokyo
Tubulin polymerization inhibitors with a fluorinated phthalimide skeleton derived from thalidomide.
The University of Tokyo
Callyspongynic acid, a polyacetylenic acid which inhibits alpha-glucosidase, from the marine sponge Callyspongia truncata.
The University of Tokyo
Development of novel silanol-based human pregnane X receptor (PXR) agonists with improved receptor selectivity.
The University of Tokyo
Structure-activity studies of a macrocyclic peptide inhibitor of histone lysine demethylase 4A.
The University of Tokyo
Structural development of tetrachlorophthalimides as liver X receptor β (LXRβ)-selective agonists with improved aqueous solubility.
The University of Tokyo
Novel Nonsteroidal Progesterone Receptor (PR) Antagonists with a Phenanthridinone Skeleton.
The University of Tokyo
Development of nonsteroidal glucocorticoid receptor modulators based on N-benzyl-N-(4-phenoxyphenyl)benzenesulfonamide scaffold.
The University of Tokyo
Switching subtype-selectivity: Fragment replacement strategy affords novel class of peroxisome proliferator-activated receptorα/δ (PPARα/δ) dual agonists.
The University of Tokyo
Structure-activity relationships of rosiglitazone for peroxisome proliferator-activated receptor gamma transrepression.
The University of Tokyo
