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Diacylglycerol (DAG)-lactones, a new class of protein kinase C (PKC) agonists, induce apoptosis in LNCaP prostate cancer cells by selective activation of PKCalpha.

Tyrosine phosphorylation of protein kinase Cdelta is essential for its apoptotic effect in response to etoposide.

Structural basis of RasGRP binding to high-affinity PKC ligands.

Pharmacological characterization of vanilloid receptor located in the brain.

Phenolic modification as an approach to improve the pharmacology of the 3-acyloxy-2-benzylpropyl homovanillic amides and thioureas, a promising class of vanilloid receptor agonists and analgesics.

Infection of glioma cells with Sindbis virus induces selective activation and tyrosine phosphorylation of protein kinase C delta. Implications for Sindbis virus-induced apoptosis.

Thapsigargin binds to and inhibits the cloned vanilloid receptor-1.

Synthesis and modeling study of (2S,5R,6R)- and (2S,5R,6S)-6-hydroxy- 8-(1-decynyl)-benzolactam-V8 as protein kinase C modulators.

Endovanilloid signaling in pain.

High affinity antagonists of the vanilloid receptor.

Isolation and structure of pedilstatin from a republic of maldives Pedilanthus sp.

New amide-bearing benzolactam-based protein kinase C modulators induce enhanced secretion of the amyloid precursor protein metabolite sAPPalpha.

Altered protein kinase C (PKC) isoforms in non-small cell lung cancer cells: PKCdelta promotes cellular survival and chemotherapeutic resistance.

Differential binding modes of diacylglycerol (DAG) and DAG lactones to protein kinase C (PK-C).

Conformationally constrained analogues of diacylglycerol (DAG). Effect on protein kinase C (PK-C) binding by the isosteric replacement of sn-1 and sn-2 esters in DAG-lactones.

Arachidonyl dopamine as a ligand for the vanilloid receptor VR1 of the rat.

Conformationally constrained analogues of diacylglycerol. 19. Synthesis and protein kinase C binding affinity of diacylglycerol lactones bearing an N-hydroxylamide side chain.

Synthetic diacylglycerols (DAG) and DAG-lactones as activators of protein kinase C (PK-C).

Use of a cDNA microarray to determine molecular mechanisms involved in grey platelet syndrome.

N-(3-acyloxy-2-benzylpropyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues: novel potent and high affinity antagonists and partial antagonists of the vanilloid receptor.

[3H]Phorbol 12,13-dibutyrate binding assay for protein kinase C and related proteins.

High-affinity partial agonists of the vanilloid receptor.

Activation of latent HIV-1 expression by the potent anti-tumor promoter 12-deoxyphorbol 13-phenylacetate.

New bivalent PKC ligands linked by a carbon spacer: enhancement in binding affinity.

Rational design of drugs that induce human immunodeficiency virus replication.

RasGRP1 Represents a Novel Non-protein Kinase C Phorbol Ester Signaling Pathway in Mouse Epidermal Keratinocytes.

Ligand structure-activity requirements and phospholipid dependence for the binding of phorbol esters to protein kinase d.

N-[4-(Methylsulfonylamino)benzyl]thiourea analogues as vanilloid receptor antagonists: analysis of structure-activity relationships for the 'C-Region'.

Conformationally constrained analogues of diacylglycerol. 20. The search for an elusive binding site on protein kinase C through relocation of the carbonyl pharmacophore along the sn-1 side chain of 1,2-diacylglycerol lactones.

Design of a high-affinity competitive antagonist of the vanilloid receptor selective for the calcium entry-linked receptor population.

Structure-activity relationships of simplified resiniferatoxin analogues with potent VR1 agonism elucidates an active conformation of RTX for VR1 binding.

The V5 Domain of Protein Kinase C Plays a Critical Role in Determining the Isoform-Specific Localization, Translocation, and Biological Function of Protein Kinase C-delta and -epsilon.

Conformationally constrained diacylglycerol (DAG) analogs: 4-C-hydroxyethyl-5-O-acyl-2,3-dideoxy-D-glyceropentono-1,4-lactone analogs as protein kinase C (PKC) ligands.

Molecular Determinants of Vanilloid Sensitivity in TRPV1.

Antineoplastic agents. 499. Synthesis of hystatin 2 and related 1H-benzo[de][1,6]-naphthyridinium salts from aaptamine.

Antineoplastic agents 491. Synthetic conversion of aaptamine to isoaaptamine, 9-demethylaaptamine, and 4-methylaaptamine.

Analysis of structure-activity relationships for the 'B-region' of N-(3-acyloxy-2-benzylpropyl)-N(')-[4-(methylsulfonylamino)benzyl]thiourea analogues as vanilloid receptor antagonists: discovery of an N-hydroxythiourea analogue with potent analgesic activity.

Sensitization of recombinant vanilloid receptor-1 by various neurotrophic factors.

Characterization of the interaction of ingenol 3-angelate with protein kinase C.

Conformationally constrained analogues of diacylglycerol. 21. A solid-phase method of synthesis of diacylglycerol lactones as a prelude to a combinatorial approach for the synthesis of protein kinase C isozyme-specific ligands.

Analysis of structure-activity relationships with the N-(3-acyloxy-2-benzylpropyl)- [Formula: see text] -[4-(methylsulfonylamino)benzyl]thiourea template for vanilloid receptor 1 antagonism.

PKCdelta associates with and is involved in the phosphorylation of RasGRP3 in response to phorbol esters.

Conformationally constrained analogues of diacylglycerol. 24. Asymmetric synthesis of a chiral (R)-DAG-lactone template as a versatile precursor for highly functionalized DAG-lactones.

Macrocyclic diacylglycerol-bis-lactones as conformationally constrained analogues of diacylglycerol-lactones. Interactions with protein kinase C.

Evodiamine functions as an agonist for the vanilloid receptor TRPV1.

Conformationally constrained analogues of diacylglycerol (DAG). 23. Hydrophobic ligand-protein interactions versus ligand-lipid interactions of DAG-lactones with protein kinase C (PK-C).

Interaction between protein kinase Cmu and the vanilloid receptor type 1.

Analysis by fluorescence resonance energy transfer of the interaction between ligands and protein kinase Cdelta in the intact cell.

Role of phorbol ester localization in determining protein kinase C or RasGRP3 translocation: real-time analysis using fluorescent ligands and proteins.

Roles of tyrosine phosphorylation and cleavage of protein kinase Cdelta in its protective effect against tumor necrosis factor-related apoptosis inducing ligand-induced apoptosis.



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