86 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
Discovery of 2-(1H-indol-5-ylamino)-6-(2,4-difluorophenylsulfonyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one (7ao) as a potent selective inhibitor of Polo like kinase 2 (PLK2).
Icahn School Of Medicine At Mount Sinai
Synthesis and biological evaluation of 3-([1,2,4]triazolo[4,3-a]pyridin-3-yl)-4-(indol-3-yl)-maleimides as potent, selective GSK-3ß inhibitors and neuroprotective agents.
Zhejiang University
Design and synthesis of protein kinase C epsilon selective diacylglycerol lactones (DAG-lactones).
Seoul National University
Discovery of selective and orally bioavailable protein kinase C¿ (PKC¿) inhibitors from a fragment hit.
Abbvie Bioresearch Center
Strategies for the modulation of phase II metabolism in a series of PKCe inhibitors.
Vertex Pharmaceuticals
Synthesis, biological, and biophysical studies of DAG-indololactones designed as selective activators of RasGRP.
National Institute Of Industrial Technology
Thienoquinolines as novel disruptors of the PKCe/RACK2 protein-protein interaction.
Innsbruck Medical University
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).
Exelixis
Design and optimization of selective protein kinase C¿ (PKC¿) inhibitors for the treatment of autoimmune diseases.
Vertex Pharmaceuticals
Multitargeted drug development: Discovery and profiling of dihydroxy substituted 1-aza-9-oxafluorenes as lead compounds targeting Alzheimer disease relevant kinases.
Martin-Luther-University Halle-Wittenberg
Structure-activity relationship and pharmacokinetic studies of sotrastaurin (AEB071), a promising novel medicine for prevention of graft rejection and treatment of psoriasis.
Novartis Institutes For Biomedical Research
A one-pot synthesis and biological activity of ageladine A and analogues.
Macquarie University
2,6-Naphthyridines as potent and selective inhibitors of the novel protein kinase C isozymes.
Novartis Institutes For Biomedical Research
Structure-activity studies on the spiroketal moiety of a simplified analogue of debromoaplysiatoxin with antiproliferative activity.
Kyoto University
Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases.
Abbott Laboratories
Structure-based optimization of aminopyridines as PKC¿ inhibitors.
Vertex Pharmaceuticals
Exploring aigialomycin d and its analogues as protein kinase inhibitors for cancer targets.
TBA
Substituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors: part 3, aryl substituted pyrrolidines.
Boehringer Ingelheim Pharmaceuticals
Hit to lead account of the discovery of bisbenzamide and related ureidobenzamide inhibitors of Rho kinase.
Boehringer Ingelheim Pharmaceuticals
Binding of curcumin and its long chain derivatives to the activator binding domain of novel protein kinase C.
University Of Houston
C-5 substituted heteroaryl-3-pyridinecarbonitriles as PKCtheta inhibitors: part II.
Wyeth Research
Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors.
University Of California
Synthesis and PKCtheta inhibitory activity of a series of 4-(indol-5-ylamino)thieno[2,3-b]pyridine-5-carbonitriles.
Wyeth Research
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
University Of Oxford
Design and physicochemical properties of new fluorescent ligands of protein kinase C isozymes focused on CH/pi interaction.
Kyoto University
Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure.
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories
Synthesis of anilino-monoindolylmaleimides as potent and selective PKCbeta inhibitors.
Central Pharmaceutical Research Institute
Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family.
Millennium Pharmaceuticals
Synthesis and PKC isozyme surrogate binding of indothiolactam-V, a new thioamide analogue of tumor promoting indolactam-V.
Kyoto University
Binding of isoxazole and pyrazole derivatives of curcumin with the activator binding domain of novel protein kinase C.
University Of Houston
Generation of 'Unnatural Natural Product' library and identification of a small molecule inhibitor of XIAP.
Keio University
Role of the phenolic hydroxyl group in the biological activities of simplified analogue of aplysiatoxin with antiproliferative activity.
Kyoto University
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Ambit Biosciences
Substituted 2H-isoquinolin-1-one as potent Rho-Kinase inhibitors. Part 1: Hit-to-lead account.
Boehringer Ingelheim Pharmaceuticals
Optimization of 5-vinylaryl-3-pyridinecarbonitriles as PKCtheta inhibitors.
Wyeth Research
Synthesis and PKCtheta inhibitory activity of a series of 5-vinyl phenyl sulfonamide-3-pyridinecarbonitriles.
Wyeth Research
C-5 Substituted heteroaryl 3-pyridinecarbonitriles as PKCtheta inhibitors: Part I.
Wyeth Research
Synthesis and biological evaluation of novel 4-azaindolyl-indolyl-maleimides as glycogen synthase kinase-3beta (GSK-3beta) inhibitors.
Zhejiang University
Anti-AIDS Agents, 11. Betulinic Acid and Platanic Acid as Anti-HIV Principles from Syzigium claviflorum, and the Anti-HIV Activity of Structurally Related Triterpenoids
TBA
Potent and selective PKC inhibitory 5-membered ring analogs of balanol with replacement of the carboxamide moiety
TBA
Protein kinase C inhibitory activities of balanol analogs bearing carboxylic acid replacements
TBA
Conformationally constrained analogues of diacylglycerol (DAG). 31. Modulation of the biological properties of diacylgycerol lactones (DAG-lactones) containing rigid-rod acyl groups separated from the core lactone by spacer units of different lengths.
National Cancer Institute-Frederick
Second generation 4-(4-methyl-1H-indol-5-ylamino)-2-phenylthieno[2,3-b]pyridine-5-carbonitrile PKCtheta inhibitors.
Wyeth Research
2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta.
Wyeth Research
Protein kinase C epsilon regulates gamma-aminobutyrate type A receptor sensitivity to ethanol and benzodiazepines through phosphorylation of gamma2 subunits.
University Of California San Francisco
Synthesis, conformational analysis, and biological evaluation of 1-hexylindolactam-V10 as a selective activator for novel protein kinase C isozymes.
Kyoto University
Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
Design and synthesis of 8-octyl-benzolactam-V9, a selective activator for protein kinase C epsilon and eta.
Kyoto University
Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.
Abbott Bioresearch Center
Imidazoquinoxaline Src-family kinase p56Lck inhibitors: SAR, QSAR, and the discovery of (S)-N-(2-chloro-6-methylphenyl)-2-(3-methyl-1-piperazinyl)imidazo- [1,5-a]pyrido[3,2-e]pyrazin-6-amine (BMS-279700) as a potent and orally active inhibitor with excellent in vivo antiinflammatory activity.
Bristol-Myers Squibb Pharmaceutical Research Institute
New bivalent PKC ligands linked by a carbon spacer: enhancement in binding affinity.
Georgetown University Medical Center
Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3.
Johnson & Johnson Pharmaceutical Research & Development
Synthesis and binding selectivity of 7- and 15-decylbenzolactone-V8 for the C1 domains of protein kinase C isozymes.
Kyoto University
Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCbeta.
Eli Lilly
Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.
Boehringer Ingelheim Pharmaceuticals
Beta-carbolines as specific inhibitors of cyclin-dependent kinases.
Institute Of Molecular And Cell Biology
Rational design, synthesis, and biological evaluation of rigid pyrrolidone analogues as potential inhibitors of prostate cancer cell growth.
Georgetotwn 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
Synthesis of 7,8-disubstituted benzolactam-V8 and its binding to protein kinase C.
Institute Of Organic Chemistry
Selective binding of bryostatin analogues to the cysteine rich domains of protein kinase C isozymes.
Stanford University
Modeling, chemistry, and biology of the benzolactam analogues of indolactam V (ILV). 2. Identification of the binding site of the benzolactams in the CRD2 activator-binding domain of PKCdelta and discovery of an ILV analogue of improved isozyme selectivity.
Georgetown University Medical Center
Synthesis and protein kinase C inhibitory activities of balanol analogs with replacement of the perhydroazepine moiety.
Eli Lilly
(S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta.
Eli Lilly
Reverse Biosynthesis: Generating Combinatorial Pools of Drug Leads from Enzyme-Mediated Fragmentation of Natural Products.
The University Of Sydney
The structural basis for the interaction between L-tryptophan and the Escherichia coli trp aporepressor.
University Of Chicago
Synthesis and in vitro opioid activity profiles of DALDA analogues.
Clinical Research Institute Of Montreal
Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitors.
Johnson & Johnson Pharmaceutical
Synthesis, molecular modeling studies, and selective inhibitory activity against monoamine oxidase of 1-thiocarbamoyl-3,5-diaryl-4,5-dihydro-(1H)- pyrazole derivatives.
Sapienza University Of Rome
Bis-huperzine B: highly potent and selective acetylcholinesterase inhibitors.
Shanghai Institute Of Materia Medica
Specificity and affinity of natural product cyclopentapeptide inhibitors against A. fumigatus, human, and bacterial chitinases.
University Of Dundee