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Discovery of novel 2-(4-aryl-2-methylpiperazin-1-yl)-pyrimidin-4-ones as glycogen synthase kinase-3β inhibitors

Autor: Daiki Sakai, Kazutoshi Watanabe, Mika Nabeno, Hiroshi Tanaka, Shinji Tanaka, Shinji Sunada, Jun-ichi Eguchi, Keiko Takiguchi-Hayashi, Ken-Ichi Saito, Shin-ichi Kusaka, Kazuki Nakayama, Kenji Fukunaga, Toshiyuki Kohara, Tomoko Bessho, Takashi Horikawa, Akiko Mori

Publikováno v: Bioorganicmedicinal chemistry letters. 27(16)

We herein describe the results of further evolution of glycogen synthase kinase (GSK)-3β inhibitors from our promising compounds containing a 3-methylmorpholine moiety. Transformation of the morpholine moiety into a piperazine moiety resulted in pot

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e55de72f14f1f283259756ae9c42b53f
https://pubmed.ncbi.nlm.nih.gov/28712706

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Discovery of novel 2-(3-phenylpiperazin-1-yl)-pyrimidin-4-ones as glycogen synthase kinase-3β inhibitors

Publikováno v: Bioorganicmedicinal chemistry letters. 27(16)

We herein describe the results of further evolution of glycogen synthase kinase (GSK)-3β inhibitors from our promising compounds containing a 2-phenylmorpholine moiety. Transformation of the morpholine moiety into a piperazine moiety resulted in pot

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::15af65e99a9d19a8f0c2d46937023c5e
https://pubmed.ncbi.nlm.nih.gov/28712708

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Fused bicyclic heteroarylpiperazine-substituted l-prolylthiazolidines as highly potent DPP-4 inhibitors lacking the electrophilic nitrile group

Autor: Hiroshi Sakashita, Yoshiharu Hayashi, Mika Nabeno, Masahiro Takeuchi, Hiroyuki Kishida, Yoshihito Tanaka, Shuji Sonda, Ikuko Miyaguchi, Tomohiro Yoshida, Fumihiko Akahoshi

Publikováno v: Bioorganic & Medicinal Chemistry. 20:5033-5041

Hypoglycemic agents with a mechanism of depeptidyl peptidase IV (DPP-4) inhibition are suitable for once daily oral dosing. It is difficult to strike a balance between inhibitory activity and duration of action in plasma for inhibitors bearing an ele

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eecab8127cb1e896847bb3931113b436
https://doi.org/10.1016/j.bmc.2012.06.033

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Heterogeneous Environment of the S−H Group of Cys966 near the Flavin Chromophore in the LOV2 Domain of Adiantum Neochrome1

Autor: Minoru Sakurai, Yoshiaki Sato, Satoru Tokutomi, Mika Nabeno, Tatsuya Iwata, Hideki Kandori

Publikováno v: Biochemistry. 46:10258-10265

The primary photochemistry of the blue-light sensor protein, phototropin, is adduct formation between the C4a atom of the flavin mononucleotide (FMN) chromophore and a nearby, reactive cysteine (Cys966), following decay of the triplet excited state o

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::730ef8248a71bb5d6df03a64adf782dd
https://doi.org/10.1021/bi701022v

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A comparative study of the binding modes of recently launched dipeptidyl peptidase IV inhibitors in the active site

Autor: Yoshihito Tanaka, Hiroyuki Kishida, Mika Nabeno, Fumihiko Akahoshi, Ikuko Miyaguchi, Takashi Kadowaki, Shinichi Ishii

Publikováno v: Biochemical and biophysical research communications. 434(2)

In recent years, various dipeptidyl peptidase IV (DPP-4) inhibitors have been released as therapeutic drugs for type 2 diabetes in many countries. In spite of their diverse chemical structures, no comparative studies of their binding modes in the act

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0ec6cf22fddf808e3bc33169e8a89140
https://pubmed.ncbi.nlm.nih.gov/23501107

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Discovery and preclinical profile of teneligliptin (3-[(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl]thiazolidine): a highly potent, selective, long-lasting and orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes

Publikováno v: Bioorganicmedicinal chemistry. 20(19)

Dipeptidyl peptidase IV (DPP-4) inhibition is suitable mechanism for once daily oral dosing regimen because of its low risk of hypoglycemia. We explored linked bicyclic heteroarylpiperazines substituted at the γ-position of the proline structure in

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::886f16383bee6e2ced6da2f121e178d6
https://pubmed.ncbi.nlm.nih.gov/22959556

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2P336 Molecular dynamics simulations of the Gln1029Leu mutant of phy3 LOV2 domain in the dark and S390 states(42. Sensory signal transduction,Poster Session,Abstract,Meeting Program of EABS & BSJ 2006)

Autor: Mika Nabeno, Minoru Sakurai, Hiroaki Kobayashi

Publikováno v: Seibutsu Butsuri. 46:S379

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::705a99de5e6434c1cac82676f8a7ee82
https://doi.org/10.2142/biophys.46.s379_4

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2P337 Computational study on the photochemical reactivities of Adiantum Phy3-LOV1 and LOV2. Role of Phe1010 located near FMN in LOV2.(42. Sensory signal transduction,Poster Session,Abstract,Meeting Program of EABS & BSJ 2006)

Autor: Mika Nabeno, Minoru Sakurai

Publikováno v: Seibutsu Butsuri. 46:S380

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::b0daa24d9a572fa8fdd15586603a4df3
https://doi.org/10.2142/biophys.46.s380_1

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