ALK inhibitors of bis-ortho-alkoxy-para-piperazinesubstituted-pyrimidines and -triazines for cancer treatment

Lee, Hyeon Ji,Latif, Muhammad,Choe, Hyeonjeong,Ali, Imran,Lee, Heung Kyoung,Yang, Eun Hye,Yun, Jeong In,Chae, Chong Hak,Jung, Jae-Kyung,Kim, Hyoung Rae,Lee, Chong Ock,Park, Chi Hoon,Lee, Kwangho 대한약학회 2014 Archives of Pharmacal Research Vol.37 No.9

Syntheses of various bis-ortho-alkoxy-parapiperazineanilino-pyrimidines and -triazines of KRCA-0008 analogs are described and their structure-activity-relationship to anaplastic lymphoma kinase (ALK) is discussed. 5-trifluoromethyl-2,4-pyrimidine analog (2) seems to be most potent in both biochemical and cellular assay in this study, however it shows inferior mice xenograft activity to Crizotinib presumably due to its sub-optimal PK parameters. 4,6-disubstituted pyrimidine and 2,4-disubstituted triazine derivatives of KRCA-0008 are less potent or inactive to ALK wt., and this observation is explained with their molecular modeling compared to KRCA-0008.

음성 스트리밍 서비스 음질 개선 및 노이즈 제거를 위한 ASRNNoise 모델 개발

이광호(KwangHo Lee),제정륭(JungRyung Je),이호욱(HoWook Lee),오동빈(Dongpin Oh),이호용(Hoyong Lee),추동원(DongWon Choo),강석우(SeokWoo Kang),송길태(Giltae Song) 한국정보과학회 2018 한국정보과학회 학술발표논문집 Vol.2018 No.12

Intravenous Single-dose Toxicity of Mountain Ginseng Pharmacopuncture in Sprague-Dawley Rats

Lee, Kwangho,Sun, Seungho,Yu, Junsang,Lim, Chungsan,Kwon, Kirok KOREAN PHARMACOPUNCTURE INSTITUTE 2014 Journal of pharmacopuncture Vol.17 No.3

Objectives: Mountain ginseng pharmacopuncture (MGP) is an extract distilled from either mountain cultivated ginseng or mountain wild ginseng. This is the first intravenous injection of pharmacopuncture in Korea. The word intravenous does not discriminate between arteries, veins, and capillaries in Oriental Medicine, but only the vein is used for MGP. The aim of this study is to evaluate the intravenous injection toxicity of MGP through a single-dose test in Sprague-Dawley (SD) rats. Methods: Male and female 6-week-old SD rats were injected intravenously with MGP (high dosage of 20 mL/kg or low dosage of 10 mL/kg). Normal saline was injected into the rats in the control group by using the same method. After the rats has treated, we conducted clinical observations, body-weight measurements and histological observations. Results: In this study, no mortalities were observed in any of the experimental groups. Also, no significant changes by the intravenous injection of MGP were observed in the body weights, or the histological observations in any of the experimental groups compared to the control group. The lethal dose for intravenous injection of MGP was found to be over 20 mL/kg in SD rats. Conclusion: Considering that the dosage of MGP generally used each time in clinical practice is about 0.3 mL/kg, we concluded with confidence that MGP is safe pharmacopuncture.

A 2.44-pJ/b 1.62–10-Gb/s Receiver for Next Generation Video Interface Equalizing 23-dB Loss With Adaptive 2-Tap Data DFE and 1-Tap Edge DFE

Lee, Jinhyung,Park, Kwanseo,Lee, Kwangho,Jeong, Deog-Kyoon IEEE 2018 IEEE TRANSACTIONS ON CIRCUITS AND SYSTEMS PART 2 E Vol.65 No.10

<P>This brief presents a 1.62-to-10-Gb/s receiver for next generation video interconnected with an adaptive decision-feedback equalizer (DFE). The adaptive DFE facilitates the best bit error rate (BER) performance for various losses of video cables. A differential-pair stage is added to the DFE for extending an effective DFE range, presetting a minimum data level, and calibrating a mismatch offset. Circuit techniques are proposed to relax timing constraints for the direct-feedback DFE architecture. A referenceless frequency acquisition is performed during a dedicated clock recovery phase. The measured BER at 10 Gb/s is lower than 10<SUP>−12</SUP> with a 23-dB loss cable. The RMS jitter and the peak-to-peak jitter of a recovered clock are measured as 2.38 ps and 17.5 ps, respectively. The prototype chip is implemented in 65-nm CMOS technology and occupies an active area of 0.254 mm<SUP>2</SUP>. This receiver consumes 24.4 mW at 10 Gb/s, corresponding to the energy efficiency of 2.44 pJ/b, which is the lowest compared to other recently published video interface receivers.</P>

A Study of American English Metaphoric and Metonymic Expressions of Anger

Lee, Kwangho 호남대학교 2000 호남대학교 학술논문집 Vol.21 No.1

본 논문에서는 분노를 나타내는 미국 영어의 은유 및 환유 표현에 관해 살펴보고 그 표현들이 어떤 개념 구조를 지니고 있는지 고찰해본다. 은유와 환유 표현들은 체계 없이 임의적으로 만들어지는 것이 아니다. 그러한 표현들은 사람들의 경험을 개념화시켜 나타내는 것이 가능하게 해주는 일정한 체계를 지니고 있다. 분노에 관한 은유 및 환유 표현들을, 분노시 나타나는 신체적 현상에 관한 문화적 모형에 입각하여 분석해 보면 분노를 나타내는 구체적인 개념과 추상적인 개념 사이에 존재론적 그리고 인식론적 대응 관계가 있다는 사실을 발견할 수 있다. 구체적인 개념들은 추상적인 개념들을 보다 구체적으로 개념화 할 수 있도록 도와주는 역할을 한다. 이러한 분석 연구를 통해 감정이 단순한 느낌만인 것이 아니라 복잡한 인지적 개념 구조를 가지고 있는 것이라는 사실을 발견할 수 있게 된다.

A 4-Week, Repeated, Intravenous Dose, Toxicity Test of Mountain Ginseng Pharmacopuncture in Sprague-Dawley Rats

Lee, Kwangho,Yu, Junsang,Sun, Seungho,Kwon, Kirok,Lim, Chungsan KOREAN PHARMACOPUNCTURE INSTITUTE 2014 Journal of pharmacopuncture Vol.17 No.4

Objectives: Mountain ginseng pharmacopuncture (MGP) is a pharmacopuncture made by distilling extract from mountain cultivated ginseng or mountain wild ginseng. This pharmacopuncture is injected intravenously, which is a quick, lossless way of strongly tonifying Qi function. The present study was undertaken to evaluate a 4-week, repeated, intravenous injection, toxicity test of MGP in Sprague-Dawley (SD) rats. Methods: Twenty male and female 6-week-old SD rats were used as subjects. We divided the SD rats into 4 groups: the high-dosage (10 mL/kg), medium-dosage (5 mL/kg), low-dosage (2.5 mL/kg) and control (normal saline) groups. MGP or normal saline was injected intravenously into the caudal vein of the rats once daily for 4 weeks. Clinical signs, body weights, and food consumption were monitored during the observation period, and hematology, serum biochemistry, organ weight, necropsy, and histological examinations were conducted once the observations had been completed. Results: No mortality was observed in any of the groups during the observation period. No changes due to MGP were observed in the experimental groups regarding clinical signs, body weights, food consumption, hematology, serum biochemistry, organ weight and necropsy. No histological changes due to MGP were observed in any of the male or female rats in the high-dosage group. Conclusion: During this 4-week, repeated, intravenous injection, toxicity test of MGP in SD rats, no toxic changes due to MGP were observed in any of the male or female rats in the high-dosage group. Thus, we suggest that the high and the low doses in a 13-week, repeated test should be 10 mL/kg and 2.5 mL/kg, respectively.

Small Active Command Design for High Density DRAMs

Kwangho Lee(이광호),Jongmin Lee(이종민) 한국컴퓨터정보학회 2019 韓國컴퓨터情報學會論文誌 Vol.24 No.11

본 논문에서는 DRAM으로 전송되는 커맨드 버스의 전력 소모량을 감소시킬 수 있는 Small Active Command 기법을 제안한다. 이를 위해, DRAM으로 전달되는 주소 중 가장 큰 크기를 차지하는 Row 주소를 포함하고 다중패킷으로 구성된 ACTIVE 커맨드를 대상으로 한다. 제안된 Small Active Command 기법은 자주 참조되는 Row 주소를 Hot 페이지로 식별하고 메모리 컨트롤러와 DRAM에 적재된 작은 캐시(테이블)의 인덱스 번호를 Row 주소를 대신하여 단일 패킷으로 전달한다. 제안된 기법에서는 인덱스 번호 전달과 캐시 동기화 관리를 위해 기존 DRAM커맨드의 사용하지 않는 비트를 활용한 I-ACTIVE와 I-PRECHARGE 커맨드를 추가하였다. 시뮬레이션을 이용한 실험 결과 제안된 방식은 Close-page 정책과 Open-page 정책에서 각각 평균적으로 20%, 8.1%의 커맨드 버스 전력 소모량을 감소시켰다. In this paper, we propose a Small Active Command scheme which reduces the power consumption of the command bus to DRAM. To do this, we target the ACTIVE command, which consists of multiple packets, containing the row address that occupies the largest size among the addresses delivered to the DRAM. The proposed scheme identifies frequently referenced row addresses as Hot pages first, and delivers index numbers of small caches (tables) located in the memory controller and DRAM. I-ACTIVE and I-PRECHARGE commands using unused bits of existing DRAM commands are added for index number transfer and cache synchronization management. Experimental results show that the proposed method reduces the command bus power consumption by 20% and 8.1% on average in the close-page and open-page policies, respectively.

Y-configuration Stent-assisted Coil Embolization for Wide-necked Intracranial Bifurcation Aneurysms

Kwangho Lee,Hyun Park,박인성,박석규,O-ki Kwon,한종우 대한뇌혈관외과학회 2016 Journal of Cerebrovascular and Endovascular Neuros Vol.18 No.4

Objective:The objective of this study was to determine the efficiency and safety of Y configuration stent-assisted coiling with double-closed stents for wide-necked intracranial aneurysms located at arterial bifurcations thorough analysis of a multicenter case series. Materials and Methods:A retrospective chart review was done on 10 patients who underwent endovascular treatment of wide-necked intracranial aneurysms with Y-configuration stent-assisted coil embolization in three centers from August 2011 to March 2014. The degree of aneurysmal occlusion was assessed using the Raymond scale. Clinical outcomes were assessed before operation, at discharge, and at the last follow-up visit using the Glasgow outcome scale. Results:The 10 patients included 6 females and 4 males with a mean age of 58.6 years. Indications for treatment included 6 unruptured intracranial aneurysms and 4 ruptured intracranial aneurysms. Five aneurysms were located at the basilar artery bifurcation, four aneurysms were located in an anterior communicating artery, and one aneurysm was in the pericallosal artery. The mean size of the 10 aneurysms was 9.7 mm. All aneurysms had a dome-to-neck ratio of < 1.5 (mean, 0.89). Immediate complications included one thromboembolic event out of the 10 cases. Immediate posttreatment angiograms showed complete occlusion in 1 aneurysm and residual necks in 9 aneurysms. Follow-up results showed 8 complete occlusions and 2 residual necks. No delayed complications were observed during the follow-up period (mean: 20 months). Conclusion:Y configuration using double-closed cell stents is feasible and safe in selected patients. This method is an acceptable option for managing complex wide-necked bifurcations.

3D-QSAR Studies on Chemical Features of 3-(benzo[d]oxazol-2-yl)pyridine-2-amines in the External Region of c-Met Active Site

Lee, Joo Yun,Lee, Kwangho,Kim, Hyoung Rae,Chae, Chong Hak Korean Chemical Society 2013 Bulletin of the Korean Chemical Society Vol.34 No.12

The three dimensional-quantitative structure activity relationship (3D-QSAR) studies on chemical features of pyridine-2-amines in the external region of c-Met active site (ER chemical features of pyridine-2-amines) were conducted by docking, comparative molecular field analysis (CoMFA), and topomer CoMFA methods. The CoMFA model obtained the partial least-squares (PLS) statistical results, cross-validated correlation coefficient ($q^2$) of 0.703, non cross-validated correlation coefficient ($r^2$) of 0.947 with standard error of estimate (SEE) of 0.23 and the topomer CoMFA obtained $q^2$ of 0.803, $r^2$ of 0.940, and SEE of 0.24. Further, the test set was applied to validate predictive abilities of models, where the predictive $r^2$ ($r{^2}_{pred}$) for CoMFA and topomer CoMFA models were 0.746 and 0.608, respectively. Each contribution of ER chemical features of pyridine-2-amines to the inhibitory potency showed correlation coefficients, $r^2$ of 0.670 and 0.913 for two core parts, 3-(benzo[d]oxazol-2-yl)pyridine-2-amine and 3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy) pyridine-2-amine, respectively, with corresponding experimental $pIC_{50}$.

Electron transport mechanism of bathocuproine exciton blocking layer in organic photovoltaics

Lee, Jeihyun,Park, Soohyung,Lee, Younjoo,Kim, Hyein,Shin, Dongguen,Jeong, Junkyeong,Jeong, Kwangho,Cho, Sang Wan,Lee, Hyunbok,Yi, Yeonjin The Royal Society of Chemistry 2016 Physical chemistry chemical physics Vol.18 No.7

<P>Efficient exciton management is a key issue to improve the power conversion efficiency of organic photovoltaics (OPVs). It is well known that the insertion of an exciton blocking layer (ExBL) having a large band gap promotes the efficient dissociation of photogenerated excitons at the donor-acceptor interface. However, the large band gap induces an energy barrier which disrupts the charge transport. Therefore, building an adequate strategy based on the knowledge of the true charge transport mechanism is necessary. In this study, the true electron transport mechanism of a bathocuproine (BCP) ExBL in OPVs is comprehensively investigated by in situ ultraviolet photoemission spectroscopy, inverse photoemission spectroscopy, density functional theory calculation, and impedance spectroscopy. The chemical interaction between deposited Al and BCP induces new states within the band gap of BCP, so that electrons can transport through these new energy levels. Localized trap states are also formed upon the Al-BCP interaction. The activation energy of these traps is estimated with temperature-dependent conductance measurements to be 0.20 eV. The Al-BCP interaction induces both transport and trap levels in the energy gap of BCP and their interplay results in the electron transport observed.</P>