A5101938671- Microbial Natural Products and Biosynthesis
- Chemical synthesis and alkaloids
- Marine Sponges and Natural Products
- Carbohydrate Chemistry and Synthesis
- Computational Drug Discovery Methods
- Chemical Synthesis and Analysis
- Synthetic Organic Chemistry Methods
- Cholinesterase and Neurodegenerative Diseases
- Cancer Treatment and Pharmacology
- Cancer therapeutics and mechanisms
- Plant biochemistry and biosynthesis
- Traditional and Medicinal Uses of Annonaceae
- Bioactive Compounds and Antitumor Agents
- Click Chemistry and Applications
- Fungal Biology and Applications
- Insect and Pesticide Research
- Enzyme Production and Characterization
- Studies on Chitinases and Chitosanases
- Steroid Chemistry and Biochemistry
- X-ray Diffraction in Crystallography
- Microbial Metabolism and Applications
- Alkaloids: synthesis and pharmacology
- Helminth infection and control
- Crystallization and Solubility Studies
- Insect Resistance and Genetics
Kitasato University
2012-2025
Kitasato Institute Hospital
2007-2024
Tokyo Institute of Technology
2005
Korea Research Institute of Bioscience and Biotechnology
2002
Japan Science and Technology Agency
2002
Philadelphia University
1992-1996
Monell Chemical Senses Center
1996
The structural diversity of chemical libraries, which are systematic collections compounds that have potential to bind biomolecules, can be represented by latent space. A space is a projection compound structure into mathematical based on several molecular features, and it express within library in order explore broader generate novel structures for drug candidates. In this study, we developed deep-learning method, called NP-VAE (Natural Product-oriented Variational Autoencoder), variational...
A total synthesis of the novel neurotrophic agent (+)-lactacystin (1) has been achieved in 11 steps and 14% overall yield from (2R,3S)-3-hydroxyleucine [(+)-16]. The construction bioassay several active analogs are also described. new asymmetric approach furnished four stereoisomers 3-hydroxyleucine, as required starting materials high enantiomeric purity.
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTIndole diterpene synthetic studies. 8. The total synthesis of (+)-paspalicine and (+)-paspalinineAmos B. Smith III, Jill Kingery-Wood, Tamara L. Leenay, Ernest G. Nolen, Toshiaki SunazukaCite this: J. Am. Chem. Soc. 1992, 114, 4, 1438–1449Publication Date (Print):February 1, 1992Publication History Published online1 May 2002Published inissue 1 February...
Five new anti-trypanosomal macrolides, actinoallolides A-E (1-5), were discovered from the cultured broth of Actinoallomurus fulvus MK10-036. The structures actinoallolides, including absolute stereochemistry, elucidated by a combination spectroscopic analyses and series chemical derivatization studies. Actinoallolide A showed most potent selective in vitro activity without cytotoxicity. class promising lead compounds was identified for development drugs both sleeping sickness Chagas disease.
IL-6 is a multifunctional cytokine involved in regulation of differentiation, antibody production, and growth certain types tumor cells. Its excessive production plays major role pathogenesis multiple myeloma postmenopausal osteoporosis. In the course screening program aimed at inhibitor from microbial products, we found madindoline A (MDL-A) B, which have fuloindoline structure with diketocyclopentene bound to methyl group. MDL-A has no cytotoxic activities. It inhibited only activities...
ADVERTISEMENT RETURN TO ISSUEPREVCommunicationNEXTRelative and Absolute Stereochemistries Total Synthesis of (+)-Macrosphelides A B, Potent, Orally Bioavailable Inhibitors Cell−Cell AdhesionToshiaki Sunazuka, Tomoyasu Hirose, Yoshihiro Harigaya, Satoshi Takamatsu, Masahiko Hayashi, Kanki Komiyama, Ōmura, Paul A. Sprengeler, Amos B. SmithView Author Information Research Center for Biological Function The Kitasato Institute School Pharmaceutical Sciences University, Minato-ku, Tokyo 108, Japan...
Abstract Background Fourteen-membered ring macrolides have been effective in reducing chronic airway inflammation and also preventing lung injury fibrosis bleomycin-challenged mice via anti-inflammatory effects. EM703 is a new derivative of erythromycin (EM) without the bactericidal We investigated antifibrotic effects an experimental model bleomycin-induced subsequent mice. Methods Seven-week-old male ICR were used. All experiments used eight mice/group, unless otherwise noted figure...
Current anti-hepatitis B virus (HBV) drugs are suppressive but not curative for HBV infection, so there is considerable demand the development of new anti-HBV agents. In this study, we found that fungus-derived exophillic acid inhibits infection with a 50% maximal inhibitory concentration (IC50) 1.1 µM and cytotoxic (CC50) >30 in primary human hepatocytes. Exophillic inhibited preS1-mediated viral attachment to cells did affect intracellular replication. appears target host reduce their...
The first convergent total synthesis of (±)-arisugacin A was accomplished by stereoselective construction the arisugacin skeleton via a Knoevenagel-type reaction an α,β-unsaturated aldehyde with 4-hydroxy 2-pyrone and dihydroxylation followed deoxygenation.
The acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor (+)-pyripyropene E (1) has been synthesized from farnesyl acetate (9 steps, 9.6% overall yield). convergent and stereoselective route exploited a biomimetic polyene cyclization as the key transformation.
Total synthesis of verticipyrone, a novel NADH-fumarate reductase inhibitor, has been accomplished by convergent approach using "Reverse Julia olefination" method. During total synthetic studies, we also prepared and evaluated several verticipyrone analogues, some which exhibited more potent antiparasitic activity than the natural verticipyrone.
Aging is associated with increased susceptibility to chronic inflammatory bone loss disorders, such as periodontitis, in large part due the impaired regenerative potential of aging tissues. DEL-1 exerts osteogenic activity and promotes regeneration. However, expression declines age. Here we show that systemically administered macrolide antibiotics a non-antibiotic erythromycin derivative, EM-523, restore 18-month-old ("aged") mice while promoting regeneration lost naturally occurring...
Synthesis of beauveriolide III (1b), which is an inhibitor lipid droplet accumulation in macrophages, was achieved by solid-phase assembly linear depsipeptide using a 2-chlorotrityl linker followed solution-phase cyclization. On the basis this strategy, combinatorial library analogues carried out radio frequency-encoded chemistry. After automated purification preparative reversed-phase HPLC, tested for inhibitory activity CE synthesis macrophages to determine structure−activity relationships...
Heart failure with reduced ejection fraction (HFrEF) is characterized not only by left ventricular (EF) but also combined symptoms such as dyspnea, fatigue, and edema. Several pharmacological interventions have been established. However, a treatment targeting novel pathophysiological mechanism still needed. Evidence indicating that inhibition of pyruvate dehydrogenase kinase 4 (PDK4) may be cardioprotective has accumulating. Thus, we focused on vitamin K3 used its framework new PDK4...