東京大学 · 医学
佐々木祐介教授の研究室は、有機合成化学と医療・バイオ分野の橋渡しを目的として、特に金属触媒を用いた高エナンチオ選択性反応の開発に取り組んでいます。特に銅(I)触媒を用いた1,3-ジエンのモノボリル化反応により、光学活性なホモアリル・アリールボロン酸エステルを高効率で合成する新規手法を確立しています。一方で、脂肪肝疾患の治療的アプローチや和牛のミスカルビング形成の遺伝的メカニズムについても、分子生物学的手法を用いて多角的な研究を展開しています。
Figures are computed from collected data and may differ slightly.
Copper(I)-catalyzed asymmetric monoborylation of 1,3-dienes has been developed. We describe the production of either optically active homoallyl- or allylboronates with high regio- and enantioselectivity (88-97% ee) through monoborylation of 1,3-dienes. The reaction with 1,3-cyclohexadiene derivatives afforded the corresponding enantioenriched homoallyboronates. By simply changing the reaction conditions, a drastic change of product preference between homoallyl- and allylboronates was found in th
Non-alcoholic steatohepatitis (NASH) is characterized by macrovesicular steatosis with ballooning degeneration of hepatocytes, diffused lobular inflammation, and fibrosis. PPAR ligands are promising therapeutic agents in NASH; accordingly, we evaluated the effects of the first clinically available selective PPARα modulator, pemafibrate. We found that pemafibrate improves F4/80-positive macrophage accumulation, ballooning degeneration of hepatocytes, and the non-alcoholic fatty liver disease (NAF
Marbling, as defined by the amount of intramuscular fat, is an economically important trait in beef cattle. Intramuscular fat deposition is postulated to arise mainly from a series of adipogenic events in intramuscular adipocyte-lineage cells and in the physiological or anatomical milieux surrounding them. This study was designed to investigate gene-expression patterns associated with fat deposition in musculus longissimus muscle, including adipocyte-lineage cells and part of the milieux. Differ
A series of psi [CH2NH] pseudopeptide analogues of a potent somatostatin octapeptide analogue, H-D-Phe-Cys-Try-D-Trp-Lys-Val-Cys-Thr-NH2, were synthesized by using a newly developed solid-phase method for direct introduction of the CH2NH peptide bond isostere. Analogues were obtained in normal yields via a combination of sodium cyanoborohydride mediated reductive alkylation of resin-bound peptide amine with a tert-butoxycarbonyl amino acid aldehyde for introduction of a CH2NH bond and normal sol
The breeding program for beef cattle in Japan has changed dramatically over 4 decades. Visual judging was done initially, but progeny testing in test stations began in 1968. In the 1980s, the genetic evaluation program using field records, so-called on-farm progeny testing, was first adopted in Oita, Hyogo, and Kumamoto prefectures. In this study, genetic trends for carcass traits in these 3 Wagyu populations were estimated, and genetic gains per year were compared among the 3 different beef cat
Vom Substitutionsmuster der Doppelbindung in den 1,3-Eninsubstraten hängt das Resultat der Titelreaktion ab (siehe Schema), aber beide Produkte, sowohl 1,3-Dienyl- als auch 3-Alkinylboronsäureester, sind mit anderen Methoden nur schlecht zugänglich. Ein interessanter Aspekt ist die in einigen Fällen hoch selektive ligandengesteuerte Borylierung. pin=Pinakolato, THF=Tetrahydrofuran.
ANGPTL2 treatment promotes macrophage accumulation and activation. These results suggest potential mechanisms for insulin resistance.
Pemafibrate is the first clinically-available selective peroxisome proliferator-activated receptor α modulator (SPPARMα) that has been shown to effectively improve hypertriglyceridemia and low high-density lipoprotein cholesterol (HDL-C) levels. Global gene expression analysis reveals that the activation of PPARα by pemafibrate induces fatty acid (FA) uptake, binding, and mitochondrial or peroxisomal oxidation as well as ketogenesis in mouse liver. Pemafibrate most profoundly induces <i>HMGCS2</
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