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Cytotoxic Activity and Structure Activity Relationship of Ceramide Analogues in Caki-2 and HL-60 Cells
YongJinKim, EunAeKim, UyDongSohn, ChulBuYim, ChaeukIm 대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 7 Pages
대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 2010, Vol.14 No.6 14 441-447 (7 pages)
B13, a ceramide analogue, is a ceramidase inhibitor and induces apoptosis to give potent anticancer activity. A series of thiourea B13 analogues was evaluated for their in vitro cytotoxic activities against human renal cancer Caki-2 and leukemic cancer HL-60 in the MTT assay. Some compounds (12, 15, and 16) showed stronger cytotoxicity than B13 and C6-ceramide against both tumor cell lines, and compound (12) gave the most potent activity with IC50 values of 36 and 9</SUB>ՌM,... -
Cytotoxic Activity and Three-Dimensional Quantitative Structure Activity Relationship of 2-Aryl-1,8-naphthyridin-4-ones
YongJinKim, EunAeKim, MiLyangChung, ChaeukIm 대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 6 Pages
대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 2009, Vol.13 No.6 16 511-516 (6 pages)
A series of substituted 2-arylnaphthyridin-4-one analogues, which were previously synthesized in our laboratory, were evaluated for their in vitro cytotoxic activity against human lung cancer A549 and human renal cancer Caki-2 cells using MTT assay. Some compounds (11, 12, and 13) showed stronger cytotoxicity than colchicine against both tumor cell lines, and compound 13 exhibited the most potent activity with IC50 values of 2.3 and 13.4</SUB>ՌM, respectively. Three-dimensional... -
Quantitative Structure Activity Relationship between Diazabicyclo[4.2.0]octanes Derivatives and Nicotinic Acetylcholine Receptor Agonists
EunAeKim, KyoungChulJung, UyDongSohn, ChaeukIm 대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 6 Pages
대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 2009, Vol.13 No.1 9 55-60 (6 pages)
Three dimensional quantitative structure activity relationship between diazabicyclo[4.2.0]octanes and nicotinic acetylcholine receptor (hՁ4Ղ2 and hՁ3Ղ4) agonists was studied using comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA). From 11 CoMFA and CoMSIA models, CoMSIA with steric and electrostatic fields gave the best predictive models (q2=0.926 and 0.945, r2ncv=0.983 and 0.988). This study can be used to develop... -
Single-Channel Recording of TASK-3-like K+ Channel and Up- Regulation of TASK-3 mRNA Expression after Spinal Cord Injury in Rat Dorsal Root Ganglion Neurons
InseokJang, Jun-HoLa, Gyu-TaeKim, Jeong-SoonLee, Eun-JinKim, Eun-ShinLee, Su-JeongKim, Jeong-MinSeo, Sang-HoAhn, Jae-YongPark, Seong-GeunH 대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 8 Pages
대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 2008, Vol.12 No.5 5 245-252 (8 pages)
Single-channel recordings of TASK-1 and TASK-3, members of two-pore domain K+ channel family, have not yet been reported in dorsal root ganglion (DRG) neurons, even though their mRNA and activity in whole-cell currents have been detected in these neurons. Here, we report single-channel kinetics of the TASK-3-like K+ channel in DRG neurons and up-regulation of TASK-3 mRNA expression in tissues isolated from animals with spinal cord injury (SCI). In DRG neurons, the single-channel conductance of... -
Development of Luciferase Reporter Gene-based Cell Bioassay for the Aromatic Hydrocarbon Receptor Agonists
Sun-YoungKim, Eun-JungChoi, Jae-HoYang 대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 6 Pages
대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 2006, Vol.10 No.6 9 349-354 (6 pages)
The aromatic hydrocarbon receptor (AhR) is a ligand-activated transcription factor that mediates many of the biological and toxicological effects of 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD, dioxin) and related chemicals. The application of recombinant reporter plasmid such as the firefly luciferase gene has proven to be a very effective method to detect these chemicals. The bioassay system, CALUX, is sensitive in directly detecting AhR-agonists from a variety of environmental and biologic... -
Intrinsic Gating in Inward Rectifier Potassium Channels (Kir2.1) with Low Polyamine Affinity Generated by Site Directed Mutagenesis
ISo, , IAshmole, HSoh, CSPark, PJSpencer, MLeyl, PRStanfield, 대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 12 Pages
대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 2003, Vol.7 No.3 3 131-142 (12 pages)
We have studied mutant forms of Kir2.1 in which an aspartate residue (D172), important for gating by intracellular polyamines, is replaced by one of three basic residues (Arg, Lys or His). Such channels are highly selective for K+, but show inward rectification that is a shallow function of voltage compared with that found in wild type. This inward rectification occurs with a reduced affinity for spermine and persists in the absence of polyamines. Though the unitary current-voltage relation... -
Inhibition of NF-κB Activation Increases Oxygen-Glucose Deprivation-Induced Cerebral Endothelial Cell Death
JinuLee, ChulHoonKim, KyuDaeShim, YoungSooAhn 대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 7 Pages
대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 2003, Vol.7 No.2 3 65-71 (7 pages)
Increasing evidences suggest that ischemia-induced vascular damage is an integral step in the cascade of the cellular and molecular events initiated by cerebral ischemia. In the present study, employing a mouse brain endothelioma-derived cell line, bEnd.3, and oxygen-glucose deprivation (OGD) as an in vitro stroke model, the role of nuclear factor kappa B (NF-κB) activation during ischemic injury was investigated. OGD was found to activate NF-κB and to induce bEnd.3 cell death in a... -
Effects of Acarbose on the Expression of Obese and Neuropeptide Y (NPY) Genes in Mice on High-Carbohydrate Diet
JiyeonKimSunghyunChung 대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 6 Pages
대한생리학회-대한약리학회 The Korean Journal of Physiology & Pharmacology 1999, Vol.3 No.4 8 433-438 (6 pages)
Two components of the neuroendocrine-hormonal response to long-term treatment of acarbose, adipose tissue-derived leptin and central neuropeptide Y (NPY), were investigated in the ICR mice on a high- carbohydrate diet. Acarbose, administered 5 or 50 mg per 100 g diet for four weeks, dose dependently suppressed body weight gain. The body weight gain was reduced along with the amount of daily food intake in 50 mg acarbose-treated group at 7th and 28th day. 5 or 50 mg acarbose treatment... -
지연성 운동장애와 CAG 반복 확장
이상경, 박재훈, 박성우, 심주철, 이상수, 이정구, 안정미, 김도관, 김영훈 대한신경정신의학회 신경정신의학 10 Pages
대한신경정신의학회 신경정신의학 2002, 제 41권 제 3호 3 399-408 (10 pages)
연구목적: 정신분열병환자에서 긴 CAG 반복서열의 빈도가 증가되어 있다는 보고가 있은 이후 이 불안정한 DNA가 정신분열병의 원인에 관여할 가능성에 대한 관심이 고조되어왔다. 항정신병약물에 의해 발생 되는 불수의적 운동장애의 하나인 지연성 운동장애(tardive dyskinesia;TD)는 CAG 반복 확장을 보이는 대표적인 운동장애의 하나인 헌팅톤씨 병과 많은 임상적, 생물학적 공통점을 갖고 있다. 저자 는 정신분열병 TD 환자에서 긴 CAG 반복 확장이 있는지를 조사하였다. 방 법: TD는 Abnormal Involuntary Movement Scale에... -
Immunochemical Studies for the Characterization of Purified(Na+, K+)-ATPase and Its Subunits with a Special Reference of Their Effect on Monovalent Cation Transport in Reconstituted (Na+, K+)-ATPase Vesicles
Rhee H.M., Hokin, L.E. 대한약리학회 대한약리학잡지 16 Pages
대한약리학회 대한약리학잡지 1990, 제 26권 제 1호 5 35-50 (16 pages)
inhibit the coupled counter-transport of Na+ and K+ as studied by means of dual labeling experiments. However, this inhibitory effect of the antibodies on transport of ions in the (Na+, K+)-ATPase vesicles is manifested only on the portion of energy and temperature dependent alkali metal fluxes, not on the portion of ATP and ouabain insensitive ion movement. Simultaneous determination of effects of the antibodies on ion fluxes and vesicular catalytic activity indicates that an inhibition of...


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