• Journal of Animal Reproduction and Biotechnology
• /
• v.36 no.4
• /
• pp.169-174
• /
• 2021

Mutations in the luteinizing hormone/chorionic gonadotropin receptors (LH/CGRs), representatives of the G protein-coupled receptor family, have been rapidly identified over the last 20 years. This review aims to compare and analyze the data reported the activating and inactivating mutations of the LH/CGRs between human, rat, equine and fish, specifically (Japanese eel Anguilla japonica). Insights obtained through detailed study of these naturally-occurring mutations provide a further update of structure-function relationship of these receptors. Specifically, we present a variety of data on eel LH/CGR. These results provide important information about LH/CGR function in fish and the regulation of mutations of the highly conserved amino acids in glycoprotein hormone receptors.

• Applied Chemistry for Engineering
• /
• v.33 no.4
• /
• pp.440-443
• /
• 2022

A key step in the synthesis of camostat mesylate, which is most widely used as a treatment for chronic pancreatitis, was conducted. Camostat mesylate was synthesized through the esterification reaction of two intermediates, GBA (4-guanidinobenzoic acid hydrochloride) and DOHA [2-(dimethylamino)-2-oxoethyl-2-(4-hydroxyphenyl)acetate]. In order to overcome the problem raised due to the low yield and expensive reagents, a new economical synthesis method was developed that can produce camostat mesylate with a high yield of 80% by activating the acid functional group of GBA using the Vilsmeier-Haack reaction and coupling it with DOHA.

• Journal of Yeungnam Medical Science
• /
• v.39 no.4
• /
• pp.332-335
• /
• 2022

We report on changes in the ascending reticular activating system (ARAS) concurrent with the recovery of impaired consciousness following rehabilitation and cranioplasty in a patient with traumatic brain injury (TBI), which were demonstrated on diffusion tensor tractography (DTT). A 34-year-old male patient was diagnosed with a traumatic intracerebral hemorrhage after falling from a height of approximately 7 m and underwent a right frontoparietotemporal decompressive craniectomy and hematoma removal. At 5 months after onset, when starting rehabilitation, the patient showed impaired consciousness, with a Glasgow Coma Scale (GCS) score of 4. Comprehensive rehabilitative therapy was provided until 14 months after onset, and his GCS score improved to 8. Cranioplasty was performed using auto-bone at 14 months after onset. One month after cranioplasty, his GCS score improved to 12. On the 15-month DTT, the deviated lower dorsal ARAS was restored on both sides, and the right side had become thicker. The right lower ventral ARAS was reconstructed, and increased neural connectivity of the upper ARAS was detected in both the prefrontal cortices. Thus, changes in the ARAS were demonstrated in a patient with TBI during recovery of consciousness following rehabilitation and cranioplasty.

• Composites Research
• /
• v.35 no.1
• /
• pp.1-7
• /
• 2022

The activated carbon is a very good choice for using as supercapacitor electrode materials. Herein, the flower of Shorea robusta, a bio-waste material was successfully used to synthesize the activated carbons for application as supercapacitor electrode materials. The activated carbon was synthesized through chemical activation process followed by thermal treatment at 700℃ in presence of N₂ atmosphere using KOH, ZnCl₂ and H₃PO₄ as the activating agents. The physicochemical analyses demonstrate that the obtained activated carbons are graphitic in nature and the degree of disorder of the graphitic carbons is changed with the activating agents. The activated carbon obtained from Shorea robusta flower (ACSF-K) electrode shows the specific capacitance of ~610 F g^-1 at 2 A g^-1 current density, which is higher than ACSF-Z (560 F g^-1) and ACSF-H (470 F g^-1) electrode material under the identical current density. The synthesized graphitic carbons also demonstrated good rate capability and high electrochemical stability as supercapacitor electrode.

• Hanyang Medical Reviews
• /
• v.33 no.1
• /
• pp.59-64
• /
• 2013

Cancer remains the leading cause of death worldwide despite intense efforts in developing innovative treatments. Current approaches in cancer therapy are mainly directed to a selective targeting of cancer cells to avoid potential side effects associated with conventional therapy. In this respect, Natural killer (NK) cells have gained growing attention and are now being considered as promising therapeutic tools for cancer therapy owing to their intrinsic ability to rapidly recognize and kill cancer cells, while sparing normal healthy cells. NK cells play a key role in the first line of defense against transformed and virus-infected cells. NK cells sense their target through a whole array of receptors, both activating and inhibitory. Functional outcome of NK cell against target cells is determined by the balance of signals transmitted from diverse activating and inhibiting receptors. Despite significant progress made in the role of NK cells attack as a pivotal sentinel in tumor surveillance, the molecular has been that regulate NK cell responses remain unclear, which restricts the use of NK cells as a therapeutic measure. Accordingly, current efforts for NK cell-based cancer therapy have largely relied on the strategies that are based on the manipulation of inhibitory receptor function. However, if we better understand the mechanisms governing NK cell activation, including those mediated by diverse activating receptors, this knowledge can be applied to the development of optimal design for cancer immunotherapy by targeting NK cells.

• Clinical and Experimental Reproductive Medicine
• /
• v.33 no.1
• /
• pp.15-23
• /
• 2006

Objective: Pituitary adenylate cyclase-activating polypeptide (PACAP), a novel hypothalamic neuropeptide, has been suggested to play a role in ovarian folliculogenesis. The present study evaluated the effect of PACAP on the growth of preantral follicles. Methods: Preantral follicles were mechanically isolated from ovaries of 21-day-old rats and cultured in groups for 3 days in serum-free medium in the absence or presence of PACAP-38 ($10^{-6}M$). Results: Treatment with PACAP-38 resulted in an increase in follicle diameter by 75% whereas treatment with follicle stimulating hormone (FSH) increased follicle diameter by 65%. PACAP-38 treatment enhanced the granulosa cell proliferation as measured by thymidine incorporation analysis. Furthermore, the production of progesterone by cultured granulosa cells and GFSHR-17 cell line was stimulated by PACAP-38. Interestingly, PACAP enhanced FSH action on stimulation of SF-1 and aromatase gene expression. Conclusion: The present results demonstrate that PACAP stimulated preantral follicle growth by potentiating proliferation and by stimulating steroidogenesis.

• Journal of Life Science
• /
• v.28 no.9
• /
• pp.1100-1117
• /
• 2018

The Ras superfamily of small G-proteins acts as a molecular switch on the intracellular signaling pathway. Upon ligand stimulation, inactive GTPases (Ras-GDP) are activated (Ras-GTP) using guanine nucleotide exchange factor (GEF) and transmit signals to their downstream effectors. Following signal transmission, active Ras-GTP become inactive Ras-GDP and cease signaling. However, the intrinsic GTPase activity of Ras proteins is weak, requiring Ras GTPase-activating protein (RasGAP) to efficiently convert RAS-GTP to Ras-GDP. Since deregulation of the Ras pathway is found in nearly 30% of all human cancers, it might be useful to clarify the structural and physiological roles of Ras GTPases. Recently, RasGAP has emerged as a new class of tumor-suppressor protein and a potential therapeutic target for cancer. Therefore, it is important to clarify the physiological roles of the individual GAPs in human diseases. The first RasGAP discovered was RASA1, also known as p120 RasGAP. RASA1 is widely expressed, independent of cell type and tissue distribution. Subsequently, neurofibromatosis type 1 (NF1) was discovered. The remaining GAPs are affiliated with the GAP1 and synaptic GAP (SynGAP) families. There are more than 170 Ras GTPases and 14 Ras GAP members in the human genome. This review focused on the current understanding of Ras GTPase and RasGAP in human diseases, including cancers.

• The Korean Journal of Physiology and Pharmacology
• /
• v.14 no.3
• /
• pp.119-125
• /
• 2010

We investigated the effects of a hot-water extract of Artemisia iwayomogi, a plant belonging to family Compositae, on cardiac ventricular delayed rectifier $K^+$ current ($I_K$) using the patch clamp technique. The carbohydrate fraction AIP1 dose-dependently increased the heart rate with an apparent $EC_{50}$ value of $56.1{\pm}5.5\;{\mu}g/ml$. Application of AIP1 reduced the action potential duration (APD) in concentration-dependent fashion by activating $I_K$ without significantly altering the resting membrane potential ($IC_{50}$ value of $APD_{50}$: $54.80{\pm}2.24$, $IC_{50}$ value of $APD_{90}$: $57.45{\pm}3.47\;{\mu}g/ml$). Based on the results, all experiments were performed with $50\;{\mu}g/ml$ of AIP1. Pre-treatment with the rapidly activating delayed rectifier $K^+$ current ($I_{Kr}$) inhibitor, E-4031 prolonged APD. However, additional application of AIP1 did not reduce APD. The inhibition of slowly activating delayed rectifier $K^+$ current ($I_{Ks}$) by chromanol 293B did not change the effect of AIP1. AIP1 did not significantly affect coronary arterial tone or ion channels, even at the highest concentration of AIP1. In summary, AIP1 reduces APD by activating $I_{Kr}$ but not $I_{Ks}$. These results suggest that the natural product AIP1 may provide an adjunctive therapy of long QT syndrome.

• Resources Recycling
• /
• v.15 no.2 s.70
• /
• pp.50-57
• /
• 2006

Production of activated carbon from woody fish parking cases has been studied using waste sulfuric acid as an activating agent for the purpose or promoted recycling of woody fishing port wastes. The adsorption capacity of produced activated carbon was observed to increase with activation temperature and reached its maximum at ca. $650^{\circ}C$ under the experimental conditions. However, the adsorption capacity of activated carbon became deteriorated above this temperature due to the thermal degeneration of its structure. Optimal activation time was found to be about 120 minutes and 1:3 weight ratio of raw material and activating agent was appropriate for increased adsorption capacity of activated carbon under the conditions of $550^{\circ}C$ and 60 minutes of activation time. Regarding the effect of the concentration of activating agent on activation, ca. 1.2 M of sulfuric acid was observed to be proper for an optimal activation or raw material. Comparison of the activation power of sulfuric acid with nitric acid showed that sulfuric acid was superior to nitric acid, however, with regard to the yield of activated carbon there was no significant difference between the two activating agents. The degree of dispersion of carbon particles was shown to be relatively high in neutral condition and the produced activated carbon was considered to be effectively employed for the treatment of metal ions in wastewater due to its negative surface charge in aqueous condition.

• The Korean Journal of Pharmacology
• /
• v.32 no.1
• /
• pp.103-112
• /
• 1996

Roles of protein kinase C and protein tyrosine kinase in the activation of neutrophil respiratory burst, degranulation and elevation of cytosolic $Ca^{2+}$ in platelet-activating factor (PAF)-stimulated neutrophils were investigated. Superoxide and $H_2O_2$ production and myeloperoxidase and acid phosphatase release in PAF-stimulated neutrophils were inhibited by protein kinase C inhibitors, staurosporine and H-7 and protein tyrosine kinase inhibitors, genistein and tyrphostin. The PAF-induced elevation of $[Ca^{2+}]_i$ in neutrophils was inhibited by staurosporine, genistein and methyl-2,5-dihydroxycinnamate. Staurosporine inhibited both intracellular $Ca^{2+}$ release and $Mn^{2+}$ influx in PAF-stimulated neutrophils. Genistein and methyl-2,5-dihydroxycinnamate inhibited $Mn^{2+}$ influx induced by PAF, whereas their effects on intracellular $Ca^{2+}$ release were not detected. In neutrophils preactivated by PMA, the stimulatory effect of PAF on the elevation of $[Ca^{2+}]_i$ was reduced. Protein kinase C and protein tyrosine kinase may be involved in respiratory burst, lysosomal enzyme release and $Ca^{2+}$ mobilization in PAF-stimulated neutrophils. The elevation of $[Ca^{2+}]_i$ appears to be accomplished by intracullular $Ca^{2+}$ release and $Ca^{2+}$ influx which are differently regulated by protein kinases. Preactivation of protein kinase C appears to attenuate the stimulatory action of PAF on intracellular $Ca^{2+}$ mobilization.