• 제목/요약/키워드: 2-APB

검색결과 58건 처리시간 0.25초

Identification of Lys49-PLA2 from crude venom of Crotalus atrox as a human neutrophil-calcium modulating protein

  • Sultan, Md. Tipu;Li, Hong-Mei;Lee, Yong Zu;Lim, Soon Sung;Song, Dong-Keun
    • The Korean Journal of Physiology and Pharmacology
    • /
    • 제20권2호
    • /
    • pp.177-183
    • /
    • 2016
  • We fortuitously observed a human neutrophil intracellular free-calcium concentration ($[Ca^{2+}]_i$) increasing activity in the commercially available phosphodiesterase I (PDE I), which is actually dried crude venom of Crotalus atrox. As this activity was not observed with another commercially available pure PDE I, we tried to find out the causative molecule(s) present in 'crude' PDE, and identified Lys49-phospholipase A2 (Lys49-PLA2 or K49-PLA2), a catalytically inactive protein which belongs to the phospholipase A2 family, by activity-driven three HPLC (reverse phase, size exclusion, reverse phase) steps followed by SDS-PAGE and LC-MS/MS. K49-PLA2 induced $Ca^{2+}$ influx in human neutrophils without any cytotoxic effect. Two calcium channel inhibitors, 2-aminoetoxydiphenyl borate (2-APB) ($30{\mu}M$) and SKF-96365 ($20{\mu}M$) significantly inhibited K49-PLA2-induced $[Ca^{2+}]_i$ increase. These results suggest that K49-PLA2 modulates $[Ca^{2+}]_i$ in human neutrophils via 2-APB- and SKF-96365-sensitive calcium channels without causing membrane disruption.

G-Protein-Coupled Receptor 120 Mediates DHA-Induced Apoptosis by Regulating IP3R, ROS and, ER Stress Levels in Cisplatin-Resistant Cancer Cells

  • Shin, Jong-Il;Jeon, Yong-Joon;Lee, Sol;Lee, Yoon Gyeong;Kim, Ji Beom;Lee, Kyungho
    • Molecules and Cells
    • /
    • 제42권3호
    • /
    • pp.252-261
    • /
    • 2019
  • The omega-3 fatty acid docosahexaenoic acid (DHA) is known to induce apoptosis and cell cycle arrest via the induction of reactive oxygen species (ROS) production and endoplasmic reticulum (ER) stress in many types of cancers. However, the roles of DHA in drug-resistant cancer cells have not been elucidated. In this study, we investigated the effects of DHA in cisplatin-resistant gastric cancer SNU-601/cis2 cells. DHA was found to induce ROS-dependent apoptosis in these cells. The inositol 1,4,5-triphosphate receptor ($IP_3R$) blocker 2-aminoethyl diphenylboninate (2-APB) reduced DHA-induced ROS production, consequently reducing apoptosis. We also found that G-protein-coupled receptor 120 (GPR120), a receptor of long-chain fatty acids, is expressed in SNU-601/cis2 cells, and the knockdown of GPR120 using specific shRNAs alleviated DHA-mediated ROS production and apoptosis. GPR120 knockdown reduced the expression of ER stress response genes, similar to the case for the pre-treatment of the cells with N-acetyl-L-cysteine (NAC), an ROS scavenger, or 2-APB. Indeed, the knockdown of C/EBP homologous protein (CHOP), a transcription factor that functions under ER stress conditions, markedly reduced DHA-mediated apoptosis, indicating that CHOP plays an essential role in the anti-cancer activity of DHA. These results suggest that GPR120 mediates DHA-induced apoptosis by regulating $IP_3R$, ROS, and ER stress levels in cisplatin-resistant cancer cells, and that GPR120 is an effective chemotherapeutic target for cisplatin resistance.

Transient Receptor Potential C4/5 Like Channel Is Involved in Stretch-Induced Spontaneous Uterine Contraction of Pregnant Rat

  • Chung, Seungsoo;Kim, Young-Hwan;Joeng, Ji-Hyun;Ahn, Duck-Sun
    • The Korean Journal of Physiology and Pharmacology
    • /
    • 제18권6호
    • /
    • pp.503-508
    • /
    • 2014
  • Spontaneous myometrial contraction (SMC) in pregnant uterus is greatly related with gestational age and growing in frequency and amplitude toward the end of gestation to initiate labor. But, an accurate mechanism has not been elucidated. In human and rat uterus, all TRPCs except TRPC2 are expressed in pregnant myometrium and among them, TRPC4 are predominant throughout gestation, suggesting a possible role in regulation of SMC. Therefore, we investigated whether the TRP channel may be involved SMC evoked by mechanical stretch in pregnant myometrial strips of rat using isometric tension measurement and patch-clamp technique. In the present results, hypoosmotic cell swelling activated a potent outward rectifying current in G protein-dependent manner in rat pregnant myocyte. The current was significantly potentiated by $1{\mu}M$ lanthanides (a potent TRPC4/5 stimulator) and suppressed by $10{\mu}M$ 2-APB (TRPC4-7 inhibitor). In addition, in isometric tension experiment, SMC which was evoked by passive stretch was greatly potentiated by lanthanide ($1{\mu}M$) and suppressed by 2-APB ($10{\mu}M$), suggesting a possible involvement of TRPC4/5 channel in regulation of SMC in pregnant myometrium. These results provide a possible cellular mechanism for regulation of SMC during pregnancy and provide basic information for developing a new agent for treatment of premature labor.

Involvement of Transient Receptor Potential Melastatin 7 Channels in Sophorae Radix-induced Apoptosis in Cancer Cells - Sophorae Radix and TRPM7 -

  • Kim, Byung-Joo
    • 대한약침학회지
    • /
    • 제15권3호
    • /
    • pp.31-38
    • /
    • 2012
  • Sophorae Radix (SR) plays a role in a number of physiologic and pharmacologic functions in many organs. Objective: The aim of this study was to clarify the potential role for transient receptor potential melastatin 7 (TRPM7) channels in SR-inhibited growth and survival of AGS and MCF-7 cells, the most common human gastric and breast adenocarcinoma cell lines. Methods: The AGS and the MCF-7 cells were treated with varying concentrations of SR. Analyses of the caspase-3 and - 9 activity, the mitochondrial depolarization and the poly (ADPribose) polymerase (PARP) cleavage were conducted to determine if AGS and MCF-7 cell death occured by apoptosis. TRPM7 channel blockers ($Gd^{3+}$ or 2-APB) and small interfering RNA (siRNA) were used in this study to confirm the role of TRPM7 channels. Furthermore, TRPM7 channels were overexpressed in human embryonic kidney (HEK) 293 cells to identify the role of TRPM7 channels in AGS and MCF-7 cell growth and survival. Results: The addition of SR to a culture medium inhibited AGS and MCF-7 cell growth and survival. Experimental results showed that the caspase-3 and -9 activity, the mitochondrial depolarization, and the degree of PARP cleavage was increased. TRPM7 channel blockade, either by $Gd^{3+}$ or 2-APB or by suppressing TRPM7 expression with small interfering RNA, blocked the SR-induced inhibition of cell growth and survival. Furthermore, TRPM7 channel overexpression in HEK 293 cells exacerbated SR-induced cell death. Conclusions: These findings indicate that SR inhibits the growth and survival of gastric and breast cancer cells due to a blockade of the TRPM7 channel activity. Therefore, TRPM7 channels may play an important role in the survival of patients with gastric and breast cancer.

온칩버스를 이용한 런타임 하드웨어 트로이 목마 검출 SoC 설계 (Run-Time Hardware Trojans Detection Using On-Chip Bus for System-on-Chip Design)

  • ;박승용;류광기
    • 한국정보통신학회논문지
    • /
    • 제20권2호
    • /
    • pp.343-350
    • /
    • 2016
  • 본 논문에서는 감염된 IP로부터 악성 공격을 감지하고 예방하기 위한 안전하고 효율적인 온칩버스를 기술한다. 대부분의 상호-연결 시스템(온칩버스)은 모든 데이터와 제어 신호가 밀접하게 연결되어있기 때문에 하드웨어 말웨어 공격에 취약하다. 본 논문에서 제안하는 보안 버스는 개선된 아비터, 어드레스 디코딩, 마스터와 슬레이브 인터페이스로 구성되며, AHB (Advanced High-performance Bus)와 APB(Advance Peripheral Bus)를 이용하여 설계되었다. 또한, 보안 버스는 매 전송마다 아비터가 마스터의 점유율을 확인하고 감염된 마스터와 슬레이브를 관리하는 알고리즘으로 구현하였다. 제안하는 하드웨어는 Xilinx ISE 14.7을 사용하여 설계하였으며, Virtex4 XC4VLX80 FPGA 디바이스가 장착된 HBE-SoC-IPD 테스트 보드를 사용하여 검증하였다. TSMC $0.13{\mu}m$ CMOS 표준 셀 라이브러리로 합성한 결과 약 39K개의 게이트로 구현되었으며 최대 동작주파수는 313MHz이다.

R 피크 검출 정확도를 개선한 홀터 심전도 모니터의 개발 (Development of Holter ECG Monitor with Improved ECG R-peak Detection Accuracy)

  • 최정현;강민호;박준호;권기구;배태욱;박준모
    • 융합신호처리학회논문지
    • /
    • 제23권2호
    • /
    • pp.62-69
    • /
    • 2022
  • 의료현장에서는 최근 디지털 헬스케어의 중요성이 대두되면서, 다양한 형태의 생체신호 측정 관련 연구가 활발히 진행되고 있다. 생체신호 중 가장 중요한 신호로 심전도를 들 수 있으며, 특히 부정맥 환자에 있어 심전도 신호의 연속 모니터링은 매우 중요하다. 부정맥은 동결절(sinus node), 동빈맥(sinus tachycardia), 심방조기수축(atrial premature beat, APB), 심실세동 (ventricular fibrillation) 등으로 그 발병원에 따른 형태가 다양하며, 발병 이후의 예후가 좋지 않으므로 일상 중 연속 모니터링은 부정맥의 조기 진단과 치료방향 설정에서 매우 중요하다. 부정맥 환자의 심전도 신호는 매우 불안정하며, 부정맥을 자동 검출하기 위한 주요 특징점으로 작용하는 정확한 R-peak 포인트의 검출이 어렵다. 본 연구에서는 연속 측정하는 홀터 심전도 모니터링 기기와 분석용 소프트웨어를 개발하였으며, 부정맥 데이터베이스를 통해 심전도 신호의 R-peak 효용성을 확인하였다. 향후 연구에서는 다양한 발병원인으로 인한 부정맥의 형태적 구분 및 예측을 위한 알고리즘과 임상 데이터에 근거한 유효성 검증에 관한 추가 연구가 필요하다.

온칩버스를 이용한 악성 회로 공격 탐지 SoC 설계 (SoC Design for Malicious Circuit Attack Detection Using on-Chip Bus)

  • ;류광기
    • 한국정보통신학회:학술대회논문집
    • /
    • 한국정보통신학회 2015년도 추계학술대회
    • /
    • pp.885-888
    • /
    • 2015
  • 본 논문에서는 감염된 IP로부터 악성 공격을 감지하고 예방하기 위한 안전하고 효율적인 온칩버스를 기술한다. 대부분의 상호-연결 시스템(온칩버스)은 모든 데이터와 제어 신호가 밀접하게 연결되어있기 때문에 하드웨어 말웨어 공격에 취약하다. 본 논문에서 제안하는 보안 버스는 개선된 아비터, 어드레스 디코딩, 마스터와 슬레이브 인터페이스로 구성되며, AHB(Advanced High-performance Bus)와 APB(Advance Peripheral Bus)를 이용하여 설계되었다. 또한, 보안 버스는 매 전송마다 아비터가 마스터의 점유율을 확인하고 감염된 마스터와 슬레이브를 관리하는 알고리즘으로 구현하였다. 제안하는 하드웨어는 Xilinx ISE 14.7을 사용하여 설계하였으며, Virtex4 XC4VLX80 FPGA 디바이스가 장착된 HBE-SoC-IPD 테스트 보드를 사용하여 검증하였다. TSMC 0.13um CMOS 표준 셀 라이브러리로 합성한 결과 약 26.2K개의 게이트로 구현되었으며 최대 동작주파수는 250MHz이다.

  • PDF

AMBA Platform을 기반으로 하는 SoC 상의 DMAC 설계 (Implementation of DMAC on SoC based on AMBA Platform)

  • 황인기;김정식
    • 대한전기학회:학술대회논문집
    • /
    • 대한전기학회 2004년도 학술대회 논문집 정보 및 제어부문
    • /
    • pp.417-419
    • /
    • 2004
  • Because of the demands for high performance and high integrated system, the needs for optimal platform becomes more importance. Optimal platform can handle more data effectively with same resources. AMBA(Advanced Microprocessor Bus Architecture)$^{TM}$ defines on-chip communication standard for designing high performance embedded micro-controllers. It is consisted of AHB, ASB and APB. It can support fast implementation and reliability in system that is composed with reusable IPs. DMAC is one of master in system and generate master signals of AHB to communicate data from one slave(peripheral or memory) to another slave. It can reduce burden of CPU and increase system performance. We designed DMAC based on AMBA and it supports 13 Channels. Each channel can be controlled by software program. It decides channel's priority using round-robin method. It can support P2P, P2M, M2P and P2P communication.

  • PDF

컴퓨터 비전응용을 위한 하드웨어 설계 및 구현 (Design and Implementation of Hardware for various vision applications)

  • 양근탁;이봉규
    • 전기학회논문지
    • /
    • 제60권1호
    • /
    • pp.156-160
    • /
    • 2011
  • This paper describes the design and implementation of a System-on-a-Chip (SoC) for pattern recognition to use in embedded applications. The target Soc consists of LEON2 core, AMBA/APB bus-systems and custom-designed accelerators for Gaussian Pyramid construction, lighting compensation and histogram equalization. A new FPGA-based prototyping platform is implemented and used for design and verification of the target SoC. To ensure that the implemented SoC satisfies the required performances, a pattern recognition application is performed.

SAGCM APD 에서의 가드링 형태에 따른 I-V 특성 연구 (I-V Characteristics of SAGCM APD by Varing Guard-Ring Depth)

  • 현경숙;백영미
    • 한국광학회:학술대회논문집
    • /
    • 한국광학회 2003년도 하계학술발표회
    • /
    • pp.100-101
    • /
    • 2003
  • 본 논문은 초고속 광통신용 검출기로 사용되고 있는 InP/InGaAs Avalanche Photodiode (APD)에 대한 연구로서 구조 변화에 따른 APD의 특성에 대해 연구하였다. 채택된 APB의 기본 구조는 Separated Absorption, Grading, Charge and Multiplication (SAGCM)구조로 u-InP 의 두께 3.5$\mu\textrm{m}$에~2.9$\mu\textrm{m}$ 만큼 Zn diffusion 하였으며, u-InGaAs 의 흡수층 두께는 0.8$\mu\textrm{m}$ 로 하였다. charge sheet 층의 도핑 농도는 ~ 3.5 $\times$ 10/sup 12//cm/sup 2/ 이고, 전극 구조는 back side illumination type이다. (중략)

  • PDF