A5023090524- Cancer therapeutics and mechanisms
- Estrogen and related hormone effects
- Synthesis of Organic Compounds
- Cancer, Hypoxia, and Metabolism
- Chemical Synthesis and Analysis
- Cancer Treatment and Pharmacology
- Microbial Natural Products and Biosynthesis
- DNA and Nucleic Acid Chemistry
- Bioactive Compounds and Antitumor Agents
- Synthesis and Reactions of Organic Compounds
- Biosimilars and Bioanalytical Methods
- Click Chemistry and Applications
- Metal complexes synthesis and properties
- Drug Transport and Resistance Mechanisms
- Natural product bioactivities and synthesis
- Eicosanoids and Hypertension Pharmacology
- Pharmaceutical studies and practices
- Fungal Biology and Applications
- Metalloenzymes and iron-sulfur proteins
- DNA Repair Mechanisms
- Peptidase Inhibition and Analysis
- Synthesis and Biological Evaluation
- Carbohydrate Chemistry and Synthesis
- Synthesis and biological activity
- Phytochemical Studies and Bioactivities
Nippon Kayaku (Japan)
2008-2025
University of Hyogo
2023
Chapman University
2018
The University of Texas MD Anderson Cancer Center
1990-2011
Shikoku Cancer Center
2007
Chulalongkorn University
2003
Microbial Chemistry Research Foundation
1997-1998
National Cancer Center
1984
Kyoto University
1973
Estrogen receptor (ER) status is an essential determinant of clinical and biological behavior human breast cancers. While ER‐positive cancers respond well to adjuvant hormone therapy, ER‐negative tumors are generally resistant. To date, no attempts have succeeded in finding molecular markers for classifying with respect postoperative prognosis. identify a set prognostic this type cancer, we used cDNA microarray consisting 25,344 genes investigate expression profiles ten primary from patients...
Topoisomerase II (Top2) is a ubiquitous nuclear enzyme that relieves torsional stress in chromosomal DNA during various cellular processes. Agents target Top2, involving etoposide, doxorubicin, and mitoxantrone, are among the most effective anticancer drugs used clinic. Mammalian cells possess two genetically distinct Top2 isoforms, both of which these agents. Top2alpha essential for cell proliferation highly expressed vigorously growing cells, whereas Top2beta nonessential growth has...
Crystallographic studies have elucidated the binding mechanism of forskolin and P-site inhibitors to adenylyl cyclase. Accordingly, computer-assisted drug design has enabled us identify isoform-selective regulators After examining more than 200 newly synthesized derivatives forskolin, we found that modification at positions C6 C7, in general, enhances isoform selectivity. The 6-(3-dimethylaminopropionyl) led an enhanced selectivity for type V, whereas 6-[N-(2-isothiocyanatoethyl)...
Four new chalcone derivatives (1, 4, 7, 10) were isolated from the stem bark of Millettia leucantha KURZ (Leguminosae) along with two known ones (2, 6) and five flavones (3, 5, 8, 9, 11). Structure elucidation unambiguous assignment isolates achieved aid 1D 2D NMR extensive studies. Correlation 10 to 4 was successfully done by reduction Et3SiH/CF3CO2H. Moderate cytotoxic activity observed in chalcones 10), whereas dihydrochalcones (4, showed moderate anti-Herpes Simplex Virus (HSV) activity....
CT-P6, the first trastuzumab biosimilar, was approved on basis of data limited to human epidermal growth factor receptor-2 (HER2)-positive early breast cancer. Usage for other indications granted by extrapolation, and post-approval clinical studies were conducted confirm effect CT-P6 in HER2-positive gastric After approval Japan 2018, a prospective post-marketing surveillance 171 patients (130 male, 41 female) with unresectable advanced or recurrent The safety efficacy evaluated over 1 year....
Flutamide (2-methyl-<i>N</i>-[4-nitro-3-(trifluoromethyl)phenyl]-propanamide), a nonsteroidal antiandrogen, is used in the treatment of prostate cancer but occasionally associated with hepatic dysfunction. In present study, metabolism flutamide including formation possible reactive toxic metabolites was investigated using human liver microsomes and 10 isoforms recombinant cytochrome P450 (P450). 2-Hydroxyflutamide (OH-flutamide) 4-nitro-3-(trifluoromethyl)phenylamine (FLU-1) were main...
Angiogenesis is an inevitable event in tumor progression and metastasis, thus has been a compelling target for cancer therapy recent years. Effective inhibition of metastasis could become promising way to treat tumor‐induced angiogenesis. We discovered that fungus, Neosartorya sp., isolated from soil sample, produced new angiogenesis inhibitor, which we designated azaspirene. Azaspirene was previously shown inhibit human umbilical vein endothelial cell (HUVEC) migration induced by vascular...
Antiestrogen agents are commonly used to treat patients with estrogen receptor (ER)-positive breast cancer. Tamoxifen has been the mainstay of endocrine treatment for early and advanced cancer many years. Following tamoxifen failure, however, there still limited options subsequent hormonal therapy. We discovered a novel compound, NK150460, that inhibits 17β-estradiol (E2)-dependent transcription without affecting binding E2 ER. Against our expectations, NK150460 inhibited growth not only...
Abstract Based on extrapolation of similar clinical outcomes in rheumatoid arthritis to the originator infliximab (IFX) randomized trials, first biosimilar antibody CT‐P13 was approved for treatment psoriasis. To evaluate safety, efficacy, and drug survival psoriasis real‐world practice, prospective post‐marketing surveillance conducted 165 Japanese patients. During a 1‐year follow‐up period, adverse reactions (ADRs) occurred 29 patients (17.6%). Infusion reaction most frequent ADR (6.7%),...
We previously reported that the aminopeptidase inhibitor bestatin induced apoptosis in several human leukemia cell lines. The present study was performed to examine whether can also induce solid tumor Bestatin alone exhibited neither direct growth inhibition nor induction of lines examined. However, it significantly augmented growth-inhibitory effect and by agonistic anti-Fas antibody (CH11). augmentation observed with other death ligands including necrosis factor-alpha (TNF-alpha) EBC-1...
Abstract NK314 is a novel synthetic benzo[c]phenanthridine alkaloid that has recently entered clinical trials as an antitumor compound, based on impressive activities in preclinical models. The present investigations were directed at determining the mechanism of action this agent. induced significant G2 cell cycle arrest several lines, independent p53 status, suggesting existence common checkpoint activation. Chk1-Cdc25C-Cdk1 pathway was activated response to 100 nmol/L ML-1 human acute...
An interim analysis of post-marketing surveillance CT-P13, an infliximab biosimilar, was performed to evaluate its safety and efficacy in Japanese patients with inflammatory bowel disease.Patients were prospectively enrolled between November 2014 March 2017, after the launch CT-P13 Japan, case report forms followed for at least 4 months analyzed as July 2018.Of 523 set, 372 remained on therapy, while 54 (20.2%) 267 Crohn's disease, 97 (37.9%) 256 ulcerative colitis withdrawn during...
Sixteen cases of malignant peripheral nerve tumors that were recorded in the files Department Orthopedics, National Cancer Center Hospital, Tokyo, between 1972-July 1983 studied clinicopathologically. The patients' ages ranged from 24-51 years, and both sexes affected equally. Histologically, 13 sheath spindle-cell type, two these patients had manifestation multiple neurofibromatosis (von Recklinghausen's disease). One epithelioid schwannoma was found to arise tibial nerve. Other primitive...