study, several novel PROTACs for the degradation of mTOR
were designed based on MLN0128 (mTOR-binding ligand) and pomalidomide (E3
ligase CRBN ligand). PROTAC compounds exhibited mTOR inhibitory activity and
suppressed MCF-7 cell proliferation. The representative compound P1
could degrade mTOR and reduce the expression of the mTOR downstream protein
p-S6 (Ser240/244) and p-AKT (Ser473). Further studies showed that this compound
could inhibit cancer cell growth by inducing autophagy, but it did not affect
the cell cycle and apoptosis. This is the first mTOR PROTAC reported and these findings
provide new insights in the study of mTOR inhibitors.
conducted a detailed evaluation of the effects of humidification on the quality
of five types of commercial magnesium oxide (MgO) tablet formulations by
near-infrared spectroscopy, microscopic infrared spectroscopy and thermogravimetry.
From these analysis results, it is qualitatively confirmed that the MgO was
changed to magnesium hydroxide by humidification. In addition, most tablet
formulations tended to prolong disintegration time due to humidification. Thus,
in most commercial MgO tablet formulations, it is suggested magnesium hydroxide significantly
contributes to prolongation of disintegration time by humidification. The
results obtained in this study will provide useful information regarding the
handling of MgO tablets in medical sites.
Pd-catalyzed C‒H arylation of [1,1'-biphenyl]-2-ol
with haloarenes, developed by Miura et al., is a useful method to synthesize ortho-teraryls.
However, only bromo- and iodoarenes were used as arylating agents. In this
paper, the authors report that chloroarenes including chloro-containing pharmaceuticals
were successfully used as haloarenes for the reactions under optimized reaction
conditions. In addition, it was revealed that substituted [1,1'-biphenyl]-2-ols and
2-heteroarylphenols instead of [1,1'-biphenyl]-2-ol
were also usable for the reactions. Transformation of the ortho-teraryl
product into a triphenylene derivative is also presented.
A Novel Amphotericin B Hydrogel Composed of Poly(Vinyl Alcohol)/Borate Complex for Ophthalmic Formulation
Released on J-STAGE: January 01, 2023 | Volume 71 Issue 1 Pages 70-73
Kengo Banshoya, Makoto Shirakawa, Yuhzo Hieda, Masatoshi Ohnishi, Yuhki Sato, Atsuko Inoue, Tetsuro Tanaka, Yoshiharu Kaneo