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Volume 90, Issue 3
Displaying 1-7 of 7 articles from this issue
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Hiroki KakutaArticle type: Article
2016 Volume 90 Issue 3 Pages 101-108
Published: March 25, 2016
Released on J-STAGE: December 26, 2017
JOURNAL FREE ACCESSSo-called modern diseases such as type 2 diabetes, cancer, Alzheimer's disease and others are closely related to glucose and lipid metabolism. Therefore, improvement of the internal environment might be an effective therapeutic approach for these modern diseases. Since retinoid X receptors (RXRs), which are nuclear receptors that act as ligand-dependent transcription factors, function as homodimers or heterodimers with other nuclear receptors, a wide variety of biological effects and therapeutic effects on the above described diseases can be expected. However, the past RXR agonists cause serious side effects such as blood triglyceride elevation, hypothyroidism and others. Our research group has been advocating a strategy of "revival drug discovery" to revive abandoned drug targets based on the idea to avoid the side effects of drugs. In this review, our past discovery research of drugs targeting RXRs will be introduced.View full abstractDownload PDF (940K) -
Tsutomu Suenaga, Takato Nozaki, Toshie FujishimaArticle type: Article
2016 Volume 90 Issue 3 Pages 109-114
Published: March 25, 2016
Released on J-STAGE: December 26, 2017
JOURNAL FREE ACCESSTwo novel stereoisomeric analogues of active vitamin D, 1,25-dihydroxyvitamin D_3, in which a spirooxetane structure exists at the C3 position of the A-ring, have been designed and synthesized in a convergent manner. This is the first attempt to utilize spiro-oxetane structures as surrogates of vital hydroxy groups in vitamin D analogues. The enyne precursors, which were required for the construction of the A-ring, were prepared from 3,3-bis(2-hydroxyethyl)oxetane in excellent yield according to the eight-step procedure. The absolute configuration at the C1-position of the synthesized compounds was determined by the circular dichroism exciton chirality method using the corresponding C1-allylic benzoates. The replacement of the C3-hydroxy group of active vitamin D with a spiro-oxetane structure provided more preferable conformation for its binding to vitamin D receptors by shifting the conformational equilibrium of the A-ring to its β-chair form.View full abstractDownload PDF (581K) -
Suemi YABUTA, Motofumi MASAKI, Yoshihiro SHIDOJIArticle type: Article
2016 Volume 90 Issue 3 Pages 115-118
Published: March 25, 2016
Released on J-STAGE: December 26, 2017
JOURNAL FREE ACCESSDownload PDF (2610K) -
Feedback regulation of vitamin C biosynthesis in plants via upstream Open Reading Frame in VTC2 geneTsubasa Sodeyama, Takahiro IshikawaArticle type: Article
2016 Volume 90 Issue 3 Pages 119-121
Published: March 25, 2016
Released on J-STAGE: December 26, 2017
JOURNAL FREE ACCESSDownload PDF (2553K) -
Toshinobu KuroishiArticle type: Article
2016 Volume 90 Issue 3 Pages 122-125
Published: March 25, 2016
Released on J-STAGE: December 26, 2017
JOURNAL FREE ACCESSDownload PDF (528K) -
Yoshiki KoriyamaArticle type: Article
2016 Volume 90 Issue 3 Pages 126-128
Published: March 25, 2016
Released on J-STAGE: December 26, 2017
JOURNAL FREE ACCESSDownload PDF (361K) -
Akihito IshigamiArticle type: Article
2016 Volume 90 Issue 3 Pages 129-132
Published: March 25, 2016
Released on J-STAGE: December 26, 2017
JOURNAL FREE ACCESSDownload PDF (2721K)
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