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Development of novel NK3 receptor antagonists with reduced environmental impact.

Kyoto University

Structure-activity relationships of dibenzoylhydrazines for the inhibition of P-glycoprotein-mediated quinidine transport.

Kyoto University

Structure-activity relationship study of 4-(thiazol-5-yl)benzoic acid derivatives as potent protein kinase CK2 inhibitors.

Kyoto University

Structural insights into mechanisms for inhibiting amyloidß42 aggregation by non-catechol-type flavonoids.

Kyoto University

Development of novel CXC chemokine receptor 7 (CXCR7) ligands: selectivity switch from CXCR4 antagonists with a cyclic pentapeptide scaffold.

Kyoto University

Development of novel neurokinin 3 receptor (NK3R) selective agonists with resistance to proteolytic degradation.

Kyoto University

Optimization of diaryl amine derivatives as kinesin spindle protein inhibitors.

Kyoto University

Preparation of asymmetric urea derivatives that target prostate-specific membrane antigen for SPECT imaging.

Kyoto University

Affinity-based screening of MDM2/MDMX-p53 interaction inhibitors by chemical array: identification of novel peptidic inhibitors.

Kyoto University

Synthesis and biological evaluation of novel styryl benzimidazole derivatives as probes for imaging of neurofibrillary tangles in Alzheimer's disease.

Kyoto University

Structure-activity relationship study of tachykinin peptides for the development of novel neurokinin-3 receptor selective agonists.

Kyoto University

Three-dimensional quantitative structure-activity relationship analyses of RGD mimetics as fibrinogen receptor antagonists.

Kyoto University

Structure-based design of novel potent protein kinase CK2 (CK2) inhibitors with phenyl-azole scaffolds.

Kyoto University

Evaluation of hydrogen bonds of ecdysteroids in the ligand-receptor interactions using a protein modeling system.

Kyoto University

Comparison of benzil and trifluoromethyl ketone (TFK)-mediated carboxylesterase inhibition using classical and 3D-quantitative structure-activity relationship analysis.

Kyoto University

Function of the alkyl side chains of Deltalac-acetogenins in the inhibitory effect on mitochondrial complex I (NADH-ubiquinone oxidoreductase).

Kyoto University

Pharmacophore identification of a specific CXCR4 inhibitor, T140, leads to development of effective anti-HIV agents with very high selectivity indexes.

Kyoto University

A sulfoximine-based inhibitor of human asparagine synthetase kills L-asparaginase-resistant leukemia cells.

Kyoto University

Structure-activity studies on the spiroketal moiety of a simplified analogue of debromoaplysiatoxin with antiproliferative activity.

Kyoto University

Synthesis and biological evaluation of novel oxindole derivatives for imaging neurofibrillary tangles in Alzheimer's disease.

Kyoto University

Structure-activity relationship study of a CXC chemokine receptor type 4 antagonist, FC131, using a series of alkene dipeptide isosteres.

Kyoto University

A critical electrostatic interaction mediates inhibitor recognition by human asparagine synthetase.

Kyoto University

Design and physicochemical properties of new fluorescent ligands of protein kinase C isozymes focused on CH/pi interaction.

Kyoto University

Synthesis and inhibitory activity of ubiquinone-acetogenin hybrid inhibitor with bovine mitochondrial complex I.

Kyoto University

Development of specific CXCR4 inhibitors possessing high selectivity indexes as well as complete stability in serum based on an anti-HIV peptide T140.

Kyoto University

Synthesis and PKC isozyme surrogate binding of indothiolactam-V, a new thioamide analogue of tumor promoting indolactam-V.

Kyoto University

Synthesis and evaluation of diarylthiazole derivatives that inhibit activation of sterol regulatory element-binding proteins.

Kyoto University

Structure-activity relationships of carboline and carbazole derivatives as a novel class of ATP-competitive kinesin spindle protein inhibitors.

Kyoto University

Diphenylpropynone derivatives as probes for imagingß-amyloid plaques in Alzheimer's brains.

Kyoto University

Role of the phenolic hydroxyl group in the biological activities of simplified analogue of aplysiatoxin with antiproliferative activity.

Kyoto University

Ligand-directed tosyl chemistry for protein labeling in vivo.

Kyoto University

Kinesin spindle protein (KSP) inhibitors with 2,3-fused indole scaffolds.

Kyoto University

Design, synthesis and evaluation of carbamate-modified (-)-N(1)-phenethylnorphysostigmine derivatives as selective butyrylcholinesterase inhibitors.

Kyoto University

Design, synthesis, evaluation and QSAR analysis of N(1)-substituted norcymserine derivatives as selective butyrylcholinesterase inhibitors.

Kyoto University

Identification of novel non-peptide CXCR4 antagonists by ligand-based design approach.

Kyoto University

Synthesis, conformational analysis, and biological evaluation of 1-hexylindolactam-V10 as a selective activator for novel protein kinase C isozymes.

Kyoto University

SAR and QSAR studies on the N-terminally acylated pentapeptide agonists for GPR54.

Kyoto University

Structure-activity relationships of cyclic peptide-based chemokine receptor CXCR4 antagonists: disclosing the importance of side-chain and backbone functionalities.

Kyoto University

Design and synthesis of 8-octyl-benzolactam-V9, a selective activator for protein kinase C epsilon and eta.

Kyoto University

Identification of novel low molecular weight CXCR4 antagonists by structural tuning of cyclic tetrapeptide scaffolds.

Kyoto University

Stereoselective synthesis of [L-Arg-L/D-3-(2-naphthyl)alanine]-type (E)-alkene dipeptide isosteres and its application to the synthesis and biological evaluation of pseudopeptide analogues of the CXCR4 antagonist FC131.

Kyoto University

Essential structural features of acetogenins: role of hydroxy groups adjacent to the bis-THF rings.

Kyoto University

Synthesis and binding selectivity of 7- and 15-decylbenzolactone-V8 for the C1 domains of protein kinase C isozymes.

Kyoto University

Design, synthesis, and target identification of new hypoxia-inducible factor 1 (HIF-1) inhibitors containing 1-alkyl-1H-pyrazole-3-carboxamide moiety.

Kyoto University

Reduction of peptide character of HIV protease inhibitors that exhibit nanomolar potency against multidrug resistant HIV-1 strains.

Kyoto University

Essential structural factors of acetogenins, potent inhibitors of mitochondrial complex I.

Kyoto University

Synthesis and biological activities of simplified aplysiatoxin analogs focused on the CH/π interaction.

Kyoto University

Synthesis and evaluation of pseudopeptide analogues of a specific CXCR4 inhibitor, T140: the insertion of an (E)-alkene dipeptide isostere into the betaII'-turn moiety.

Kyoto University

Identification of a new class of non-electrophilic TRPA1 agonists by a structure-based virtual screening approach.

Kyoto University

The amide hydrogen of (-)-indolactam-V and benzolactam-V8's plays a critical role in protein kinase C binding and tumor-promoting activities.

Kyoto University

The C4 hydroxyl group of phorbol esters is not necessary for protein kinase C binding.

Kyoto University

Beta-D-glycosylamidines: potent, selective, and easily accessible 1-glycosidase inhibitors.

Kyoto University

Conformational study of a highly specific CXCR4 inhibitor, T140, disclosing the close proximity of its intrinsic pharmacophores associated with strong anti-HIV activity.

Kyoto University

Scaffold hopping of fused piperidine-type NK3 receptor antagonists to reduce environmental impact.

Kyoto University

Design, synthesis, and structure-activity relationships of 1-ethylpyrazole-3-carboxamide compounds as novel hypoxia-inducible factor (HIF)-1 inhibitors.

Kyoto University

Effects of the methoxy group in the side chain of debromoaplysiatoxin on its tumor-promoting and anti-proliferative activities.

Kyoto University

Structure-Activity Relationships and in Vivo Evaluation of Quinoxaline Derivatives for PET Imaging of β-Amyloid Plaques.

Kyoto University

Synthesis and biological evaluation of a targeted DNA-binding transcriptional activator with HDAC8 inhibitory activity.

Kyoto University

Structure-activity studies on the side chain of a simplified analog of aplysiatoxin (aplog-1) with anti-proliferative activity.

Kyoto University

Hybrid ubiquinone: novel inhibitor of mitochondrial complex I.

Kyoto University

Antiproliferative and apoptotic activities of sequence-specific histone acetyltransferase inhibitors.

Kyoto University

Design, synthesis, and evaluation of DNA topoisomerase II-targeted nucleosides.

Kyoto University

Structure-Activity Relationship Study of Cyclic Pentapeptide Ligands for Atypical Chemokine Receptor 3 (ACKR3).

Kyoto University

Synthesis and biological evaluation of steroidal derivatives bearing a small ring as vitamin D receptor agonists.

Kyoto University

Identification of selective inhibitors of sphingosine kinases 1 and 2 through a structure-activity relationship study of 4-epi-jaspine B.

Kyoto University

Investigation of the inhibitory mechanism of apomorphine against MDM2-p53 interaction.

Kyoto University

Inhibitors of cyclin-dependent kinase 7 (CDK7)

Syros Pharmaceuticals

Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors

Array Biopharma

Nitrogen-containing heterocyclic compound and use thereof

Takeda Pharmaceutical

Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor.

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