A5028549446- Receptor Mechanisms and Signaling
- Circadian rhythm and melatonin
- Diabetes Treatment and Management
- Spaceflight effects on biology
- Neuropeptides and Animal Physiology
- Asthma and respiratory diseases
- Light effects on plants
- Alcohol Consumption and Health Effects
- Nitric Oxide and Endothelin Effects
- Monoclonal and Polyclonal Antibodies Research
- Eicosanoids and Hypertension Pharmacology
- Anesthesia and Sedative Agents
- Allergic Rhinitis and Sensitization
- Reproductive System and Pregnancy
- Adenosine and Purinergic Signaling
- Influenza Virus Research Studies
- ATP Synthase and ATPases Research
- Atrial Fibrillation Management and Outcomes
- Ion channel regulation and function
- Dietary Effects on Health
- Hormonal Regulation and Hypertension
- Organic Chemistry Cycloaddition Reactions
- Atomic and Subatomic Physics Research
- Endometriosis Research and Treatment
- Amino Acid Enzymes and Metabolism
Taisho Pharmaceutical (Japan)
2012-2023
Kyushu University
2010-2013
Nara Institute of Science and Technology
2003
Ovarian development is related to cell proliferation, differentiation, and apoptosis of granulosa cells luteal under the control various modulators, including follicle-stimulating hormone (FSH), luteinizing (LH), growth factors. In present study, expression clock genes regulation mechanism were analyzed in different ovarian types during differentiation apoptosis. The authors focused on circadian Per2 as a core gene for maintenance rhythms. By using real-time monitoring system promoter...
Circadian rhythms are modulated in a variety of peripheral tissues, including the uterus where endometrial stromal cells (UESCs) undergo proliferation and differentiation (decidualization) during gestation. Here authors focused on circadian UESCs implantation decidualization rodents. As revealed by analyses cultured from pregnant Per2 promoter–dLuc transgenic rats, oscillation ∼24 h was observed response to dexamethasone. enhanced implantation, whereas they were attenuated decidualization....
Circadian rhythms are modulated in a variety of peripheral tissues including the prostate, which mesenchyme and epithelium cells controlled under androgens. Here, we investigated testosterone regulation core clock genes such as Bmal1, Clock, Per2 Nr1d1 deficient state testosterone. In vivo studies showed that Bmal1 mRNA expression prostates displayed peak at ZT 20 trough 12. Both Clock transcripts decreased after castration. Conversely, is promoted by binding heterodimers to E-box, enhanced...
20-Hydroxyeicosatetraenoic acid (20-HETE) is one of the major oxidized arachidonic (AA) metabolites produced by cytochrome P450 (CYP) 4A11 and CYP4F2 isozymes in human liver kidney. Numerous studies have suggested involvement 20-HETE pathogenesis renal diseases, suppression production inhibition CYP4A11 may be an attractive therapeutic strategy for diseases. At first, we identified methylthiazole derivative 2 as a potent dual inhibitor CYP4F2. An optimization study series derivatives with...
Synthesis and structure-activity relationship of a novel series isoquinoline CRTH2 antagonists bearing methylene linker between the benzamide moieties were described. Optimization focusing on substituents portion in right hand part molecule led to identification TASP0412098 (9l), which is potent, selective antagonist (binding affinity: IC50=2.1 nM, functional activity: IC50=12 nM). Compound 9l, was orally bioavailable mice guinea pigs, showed vivo efficacy after oral administration bronchial...
Sodium-glucose cotransporter 1 (SGLT1) is the primary transporter for glucose absorption from gastrointestinal tract. While C-phenyl D-glucitol derivative SGL5213 has been reported to be a potent intestinal SGLT1 inhibitor use in treatment of type 2 diabetes, no selectivity was found vitro (IC50 29 nM hSGLT1 and 20 hSGLT2). In this study we new method synthesizing key intermediates 12 by one-pot three-component condensation reaction discovered 41j (TP0454614), which >40-fold 26 1101 The...
The circadian rhythm is a fundamental biological system in mammals involved the regulation of various physiological functions such as energy metabolism, endocrine and reproduction. molecular oscillations underlying generation rhythmicity develop gradually during ontogenesis. However, process mammalian cellular oscillator formation remains unknown differentiated granulosa cells apoptotic luteal cells. Two studies were conducted to detect expression clock genes related mechanisms different...
Abstract The most potent compound, TASP0376377 (I) shows good CRTH2 antagonist potency, as well sufficient selectivity for binding to over the DP1 prostanoid receptor and COX‐1 COX‐2 enzymes.