A5022445799- Cancer-related Molecular Pathways
- PI3K/AKT/mTOR signaling in cancer
- Biochemical and Molecular Research
- Cancer-related gene regulation
- Microtubule and mitosis dynamics
- Ubiquitin and proteasome pathways
- Cancer Mechanisms and Therapy
- Epigenetics and DNA Methylation
- Ocular Oncology and Treatments
- Advanced Breast Cancer Therapies
- DNA and Nucleic Acid Chemistry
- Cancer Research and Treatments
- Cancer Immunotherapy and Biomarkers
- Endometrial and Cervical Cancer Treatments
- Advanced biosensing and bioanalysis techniques
- Cancer therapeutics and mechanisms
- Melanoma and MAPK Pathways
- Synthesis and Biological Evaluation
- Click Chemistry and Applications
- Lung Cancer Research Studies
- Cervical Cancer and HPV Research
- Quinazolinone synthesis and applications
- Protist diversity and phylogeny
Gunma Astronomical Observatory
2025
Taiho Pharmaceutical (Japan)
2018-2023
Food Research Institute
2001-2011
Merck & Co., Inc., Rahway, NJ, USA (United States)
2001
Jikei University School of Medicine
1995
As a first step in structure-based design of highly selective and potent Cdk4 inhibitors, we performed generation novel series inhibitors. A homology model was constructed according to X-ray analysis an activated form Cdk2. Using this model, applied new de novo strategy which combined the program LEGEND with our in-house structure selection supporting system SEEDS generate scaffold candidates. In way, four classes candidates including diarylurea were identified. By constructing informer...
Genetic alteration of one or more components the p16INK4A-CDK4,6/cyclin D-retinoblastoma pathway is found in than half all human cancers. Therefore, CDK4 an attractive target for development a novel anticancer agent. However, it difficult to make CDK4-specific inhibitors that do not possess activity other kinases, especially CDK2, because CDK family has high structural homology. The three-dimensional structure particularly bound with inhibitor, provided useful information synthesis...
The retinoblastoma product (RB1) is frequently deregulated in various types of tumors by mutation, deletion, or inactivation through association with viral oncoproteins. functional loss RB1 recognized to be one the hallmarks that differentiate cancer cells from normal cells. Many researchers are attempting develop anti-tumor agents preferentially effective against RB1-negative tumors. However, identify patients cancers, it imperative predictive biomarkers classify RB1-positive and -negative...
Polo-like kinase 1 (Plk1) is a serine/threonine that plays an important role in M phase progression by regulating various downstream substrates via phosphorylation. Here, we identified β-catenin as novel substrate of Plk1 and determined Ser-718 phosphorylation site for using phospho-specific antibody cross-reacts with Plk1-dependent sites. was directly phosphorylated recombinant vitro, the signal cells increasing overexpression decreasing when endogenous depleted small interfering RNA. The...
Abstract The MAPK and PI3K pathways are involved in cancer growth survival; however, the clinical efficacy of single inhibitors each pathway is limited or transient owing to resistance mechanisms, such as feedback signaling and/or reexpression receptor-type tyrosine kinases (RTK). This study identified a potent novel kinase inhibitor, TAS0612, characterized its properties. We found that TAS0612 potent, orally available compound can inhibit p90RSK (RSK), AKT, p70S6K (S6K) agent showed strong...
Abnormalities in the p16INK4a/ cyclin-dependent kinase (Cdk)4, 6/ Retinoblastoma (Rb) pathway frequently occur various human cancers. Thus, Cdk4/6 is an attractive target for cancer therapy. Here we report biological characterization of a 2-aminothiazole-derived selective inhibitor, named Compound A vitro and vivo. potently inhibits Cdk4 Cdk6 with high selectivity (more than 57-fold) against other Cdks 45 serine/threonine tyrosine kinases. Rb protein (pRb) phosphorylation at Ser780,...
<p>Supplementary Figure 2. Pharmacodynamic marker inhibitions in the HCC70 tumor xenografts treated after repetitive doses of TAS0612. TAS0612, 60 mg/kg, was administered to tumor-bearing mice daily from Day 1 8 by oral gavage, and subcutaneously implanted tumors were dissected at 4 hour post-administration on 8. After sampling, immunoblot analysis performed detect pharmacodynamic inhibitions, signal feedback, apoptosis induction. Clear inhibition markers such as phospho-PRAS40,...
<p>Supplementary Figure 2. Pharmacodynamic marker inhibitions in the HCC70 tumor xenografts treated after repetitive doses of TAS0612. TAS0612, 60 mg/kg, was administered to tumor-bearing mice daily from Day 1 8 by oral gavage, and subcutaneously implanted tumors were dissected at 4 hour post-administration on 8. After sampling, immunoblot analysis performed detect pharmacodynamic inhibitions, signal feedback, apoptosis induction. Clear inhibition markers such as phospho-PRAS40,...
<p>Supplementary Figure 1. Body weight change of each treatment group corresponding to efficacy study shown in Fig. 6B-6E are panel A-D, respectively. In all studies, there was no evidence intolerance, such as rapid and severe reduction. The on Day 0 defined 100%, the increase or decrease measurement day relative is a percentage (mean ± standard error).</p>
<div>Abstract<p>The MAPK and PI3K pathways are involved in cancer growth survival; however, the clinical efficacy of single inhibitors each pathway is limited or transient owing to resistance mechanisms, such as feedback signaling and/or reexpression receptor-type tyrosine kinases (RTK). This study identified a potent novel kinase inhibitor, TAS0612, characterized its properties. We found that TAS0612 potent, orally available compound can inhibit p90RSK (RSK), AKT, p70S6K (S6K)...
<p>Supplementary Figure 1. Body weight change of each treatment group corresponding to efficacy study shown in Fig. 6B-6E are panel A-D, respectively. In all studies, there was no evidence intolerance, such as rapid and severe reduction. The on Day 0 defined 100%, the increase or decrease measurement day relative is a percentage (mean ± standard error).</p>
<div>Abstract<p>The MAPK and PI3K pathways are involved in cancer growth survival; however, the clinical efficacy of single inhibitors each pathway is limited or transient owing to resistance mechanisms, such as feedback signaling and/or reexpression receptor-type tyrosine kinases (RTK). This study identified a potent novel kinase inhibitor, TAS0612, characterized its properties. We found that TAS0612 potent, orally available compound can inhibit p90RSK (RSK), AKT, p70S6K (S6K)...
Abstract Background: Lysine-specific demethylase 1A (LSD1/KDM1A) is a flavin adenine dinucleotide (FAD)-dependent histone that specifically modifies H3 lysine 4 and 9. LSD1 activity implicated in the pathogenesis of several human cancers, recent studies indicated inhibition promising therapeutic strategy for acute myeloid leukemia (AML). Decitabine azacitidine, FDA-approved agents treatment AML myelodysplastic syndrome, alter global DNA methylation by inhibiting methyltransferases (DNMTs),...