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From a Natural Product Lead to the Identification of Potent and Selective Benzofuran-3-yl-(indol-3-yl)maleimides as Glycogen Synthase Kinase 3β Inhibitors That Suppress Proliferation and Survival of Pancreatic Cancer Cells

Autor: Alan P. Kozikowski, Sylvie Y. Blond, Franck Gallier, Andrei V. Ougolkov, Songpo Guo, Daniel D. Billadeau, Irina N. Gaisina, Toru Kurome, Denise L. Holzle, Doris N. Luchini, Ki Hwan Kim

Publikováno v: Journal of Medicinal Chemistry. 52:1853-1863

Recent studies have demonstrated that glycogen synthase kinase 3beta (GSK-3beta) is overexpressed in human colon and pancreatic carcinomas, contributing to cancer cell proliferation and survival. Here, we report the design, synthesis, and biological

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d8b5e73cfb9faf8350c5e0a6466df322
https://doi.org/10.1021/jm801317h

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Selective 5-Hydroxytryptamine 2C Receptor Agonists Derived from the Lead Compound Tranylcypromine: Identification of Drugs with Antidepressant-Like Action

Autor: Toru Kurome, Alan P. Kozikowski, Niels H. Jensen, Sudhakar Kadari, Barbara J. Caldarone, Jessica E. Malberg, Michael Manzano, Sung Jin Cho, Bryan L. Roth

Publikováno v: Journal of Medicinal Chemistry. 52:1885-1902

We report here the design, synthesis, and pharmacological properties of a series of compounds related to tranylcypromine (9), which itself was discovered as a lead compound in a high-throughput screening campaign. Starting from 9, which shows modest

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a5e815a42ffb82a3a5255226ea458da9
https://doi.org/10.1021/jm801354e

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Further Structure−Activity Relationship Studies of Piperidine-Based Monoamine Transporter Inhibitors: Effects of Piperidine Ring Stereochemistry on Potency. Identification of Norepinephrine Transporter Selective Ligands and Broad-Spectrum Transporter Inhibitors

Autor: Kenneth M. Johnson, Rong He, Toru Kurome, Kelly M. Giberson, Alan P. Kozikowski

Publikováno v: Journal of Medicinal Chemistry. 48:7970-7979

4-(4-Chlorophenyl)piperidine analogues each bearing a thioacetamide side chain appendage similar to that found in the wake-promoting drug modafinil have been synthesized. The transporter inhibitory activity of both the cis and trans isomers of these

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3627abd2367cfbb659fbfca5c8505efe
https://doi.org/10.1021/jm050694s

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Syntheses Antifungal Aureobasidin A Analogs with Alkyl Chains for Structure-activity Relationship

Autor: Tetsuya Inoue, Ikunoshin Kato, Toru Kurome, Tetsuo Shiba, Kazutoh Takesako, Kaoru Inami

Publikováno v: The Journal of Antibiotics. 51:359-367

The syntheses of aureobasidin A (AbA) derivatives with alkyl chains and their in vitro structure-biological activity relationships are discussed. The analogs replaced at positions 6, 7, or 8 of AbA with either L-glutamic acid, delta-hydroxy-L-norvali

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::81b9b0e33b6ad4fe3b78d94edbd8036a
https://doi.org/10.7164/antibiotics.51.359

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Total synthesis of an antifungal cyclic depsipeptide aureobasidin A

Autor: Katsushige Ikai, Tetsuya Inoue, Toru Kurome, Ikunoshin Kato, Kazutoh Takesako, Tetsuo Shiba, Kaoru Inami

Publikováno v: Tetrahedron. 52:4327-4346

The first total synthesis of antifungal cyclic depsipeptide aureobasidin A is described. The synthesis was achieved mainly using bromotris(pyrrolidino)phosphonium hexafluorophosphate (PyBroP) as a coupling reagent. Peptide cyclization was carried out

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::db1bcc37b0a4fb596d8723a4ce423e5e
https://doi.org/10.1016/0040-4020(96)00132-9

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Expression of Recombinant Mouse/Human Chimeric Antibody Specific to Human GMP-140/P-selectin

Autor: Kyoko Kamihagi, Masazumi Yasumoto, Ikunoshin Kato, Kimikazu Hashino, Toru Kurome, Keiko Murakami, Masahiko Katayama

Publikováno v: The Journal of Biochemistry. 115:608-614

To construct a mouse/human chimeric antibody, we cloned the genomic DNAs for Ig from a murine hybridoma that produces PL7-6 monoclonal antibody specific to human P-selectin and expressed them in SP2/0 myelomas using a series of pSV2 vectors. Transfec

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d2989fd397fd72e6a308cd46eb82bf8e
https://doi.org/10.1093/oxfordjournals.jbchem.a124383

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Aureobasidins: structure-activity relationships for the inhibition of the human MDR1 P-glycoprotein ABC-transporter

Autor: Francis Loor, Toru Kurome, Agnès Didier, Françoise Tiberghien, Kazutoh Takesako, Tom Wenandy

Publikováno v: Journal of medicinal chemistry. 43(13)

Cyclic depsipeptide cyclo-[D-Hmp(1)-L-MeVal(2)-L-Phe(3)-L-MePhe(4)-L-Pro(5)-L-aIle+ ++(6)-L-MeVal(7)-L-Leu(8)-L-betaHOMeVal(9)], the antifungal antibiotic aureobasidin A (AbA), was reported to interfere with ATP-binding cassette (ABC) transporters in

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0bdc89f460c3b77047d8fb251d6a6b95
https://pubmed.ncbi.nlm.nih.gov/10891114

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Aureobasidins as new inhibitors of P-glycoprotein in multidrug resistant tumor cells

Autor: Takashi Tsuruo, Kazutoh Takesako, Toru Kurome, Ikunoshin Kato

Publikováno v: The Journal of antibiotics. 51(3)

Cyclic depsipeptide antibiotic aureobasidin A (AbA) and its analogs were tested for the inhibitory activity of P-glycoprotein in multidrug resistant cancer cells as well as for the antifungal activity. Some analogs with lower antifungal activity than

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e99bb63c42785e5c407c3c8d694378ec
https://pubmed.ncbi.nlm.nih.gov/9589072

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