• 약학회지
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• 제60권3호
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• pp.135-140
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• 2016

Heat shock protein 90 (Hsp90) is a ubiquitous molecular chaperone, which is associated with stabilization of many oncogenic proteins for cancer cell survival. Hsp90 is overexpressed 2-10 fold higher in cancer cells than normal cells. Due to its potential to simultaneously disable multiple signaling pathway, Hsp90 has been identified as a validated target for cancer therapy. Accordingly, we designed and synthesized 2',4'-dimethoxychalcone derivatives to inhibit Hsp90 chaperone function. Among 2',4'-dimethoxychalcone derivatives, we found that compound 1g disrupted Hsp90 chaperoning function and impaired the growth of cancer cells. These findings indicated that 1g could serve a potential lead compound to target Hsp90 in cancer chemotherapy.

• 한국생물물리학회:학술대회논문집
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• 한국생물물리학회 2003년도 정기총회 및 학술발표회
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• pp.63-63
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• 2003

$\alpha$$_1$-Antityrpsin is a member of the serine protease inhibitor (SERPIN) family that shares a common tertiary structure. The reactive site loop (RSL) of serpins is exposed at one end of the molecule for protease binding. Upon cleavage by a target protease, the RSL is inserted into the major $\beta$-sheet A, which is a necessary process for formation of a tight inhibitory complex. Various biochemical and structural studies suggest that the rate of the RSL insertion upon binding a target protease is critical for inhibitory activity, and it is thought that helix F region (thFs3A and helix F) located in front of $\beta$-sheet A, should be lifted for the loop insertion during complex formation.

• 통합자연과학논문집
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• 제5권1호
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• pp.32-37
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• 2012

Chemokine receptor antagonists have potential applications in field of drug discovery. Although the chemokine receptors are G-protein-coupled receptors, their cognate ligands are small proteins (8 to 12 kDa), and so inhibiting the ligand/receptor interaction has been challenging. The application of structure-based in-silico methods to drug discovery is still considered a major challenge, especially when the x-ray structure of the target protein is unknown. Such is the case with human CCR2 and CCR5, the most important members of the chemokine receptor family and also a potential drug target. Herein, we review the success stories of combined receptor modeling/mutagenesis approach to probe the allosteric nature of chemokine receptor binding by small molecule antagonists for CCR2 and CCR5 using Rhodopsin as template. We also urged the importance of recently available ${\beta}2$-andrenergic receptor as an alternate template to guide mutagenesis. The results demonstrate the usefulness and robustness of in-silico 3D models. These models could also be useful for the design of novel and potent CCR2 and CCR5 antagonists using structure based drug design.

• 고려인삼학회:학술대회논문집
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• 고려인삼학회 2006년도 춘계학술대회
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• pp.13-17
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• 2006

다양한 연구에 따르면, 고려인삼은 허약한 체질, 숙취, 폐경과 월경불순, 초기 당뇨병, 영양실조, 빈혈 및 단백질 부족, 간기능 악화, 각종 독성물질에 기인한 중독, 피로, 추위, 스트레스, 산후조리, 체력쇠퇴 등에 효능이 있음이 알려져 있다. 특히 고려인삼은 혈관 기능을 효과적으로 조절함으로 고혈압, 뇌졸중, 심근경색, 동맥경화, 관절염, 당뇨, 비만 등의 질환을 효과적으로 치료하거나 예방할 수 있는 효능이 있음이 최근 연구에 의하여 밝혀지고 있다. 그러나 고려인삼 약리효능의 표적분자(target molecule)나 생화학적 작용기전(biochemical mechanism)이 세포 및 분자 수준에서 규명되지 못하여 고려인삼이 의약품으로 인정받지 못하고 건강식품으로 분류되고 있어 소비가 한인 흑인 히스패닉 시장에 한정되고 있고, 최근에는 타 경쟁국 인삼에 비해 수출 경쟁력이 약화되고 있는 실정이다. 본 연구에서는 고려인삼 추출물과 효능성분이 혈관내피세포 기능조절에 미치는 효능 및 작용기전을 규명하여 고려인삼이 호발성 혈관질환에 대한 예방 및 치료 효능이 있음을 분자 및 유전자 수준에서 확인하고자 하였다.

• 대한의생명과학회지
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• 제18권3호
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• pp.210-217
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• 2012

Oncolytic viral vectors have shown good candidates for cancer treatment but have many limitations. To improve the therapeutic potential of oncolytic vaccinia virus, we developed a recombinant vaccinia virus expressing the 4-1BBL co-stimulatory molecule or CCL21. 4-1BBL and CCL21 expression was identified by FACS analysis and immunoblotting. rV-4-1BBL vaccination shows significant tumor regression compared to rV-LacZ, but rV-CCL21 shows rapid tumor growth compared to rV-LacZ in the poorly immunogenic B16 murine melanoma model. 4-1BBL expression resulted in the increase of the number of CD8+ T cells and especially the increase of effector (CD62L-CD44+) CD8+ T cells. These data suggest 4-1BBL may be the potential target for enhancement of tumor immunotherapy.

• Bulletin of the Korean Chemical Society
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• 제34권7호
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• pp.2006-2010
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• 2013

Leukocyte common antigen-related phosphatase (LAR) has been considered a promising target for the development of therapeutics for neurological diseases. Here, we report the first example for a successful application of the structure-based virtual screening to identify the novel small-molecule LAR inhibitors. Five of these inhibitors revealed micromolar inhibitory activities with the associated $IC_{50}$ values ranging from 2 to 6 ${\mu}M$. Because the newly identified inhibitors were also screened for having desirable physicochemical properties as a drug candidate, they may serve as a starting point of the structure-activity relationship study to optimize the medical efficacy. Structural features relevant to the stabilization of the new inhibitors in the active site of LAR are discussed in detail.

• Bulletin of the Korean Chemical Society
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• 제34권6호
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• pp.1668-1672
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• 2013

We developed a standoff Raman detection system for explosive molecules (EMs). Our system was composed of reflective telescope with 310 mm diameter lens, 532 nm pulse laser, and Intensified Charge-Coupled Device (ICCD) camera. In order to remove huge background noise coming from ambient light, laser pulses with nanosecond time width were fired to target sample and ICCD was gated to open only during the time when the scattered Raman signal from the sample arrived at ICCD camera. We performed standoff experiments with military EMs by putting the detector at 10, 20 and 30 m away from the source. The standoff results were compared with the confocal Raman results. Based on our standoff experiments, we were able to observe the peaks in the range of 1200 and $1600cm^{-1}$, where vibrational modes of nitro groups were appeared. The wave numbers and shapes of these peaks may serve as good references in detecting and identifying various EMs.

• 대한의생명과학회지
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• 제10권2호
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• pp.75-84
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• 2004

Massive identification of differentially expressed patterns has been used as a tool to detect genes that are involved in disease related process. We employed circular single stranded sense molecules as probe DNA for a DNA chip. The circular single stranded DNAs derived from 1,152 unigene cDNA clones were purified in a high throughput mode from the culture supernatant of bacterial transformants containing recombinant phagemids and arrayed onto silanized slide glasses. The DNA chip was examined for its utility in detection of differential expression profile by using cDNA hybridization. Hybridization of the single stranded probe DNA were performed with Cy3- or Cy5-labeled target cDNA preparations at $60^\circ$C. Dot scanning performed with the hybridized slide showed 29 up-regulated and 6 down-regulated genes in a cancerous liver tissue when compared to those of adjacent noncancerous liver tissue. These results indicate that the circular single stranded sense molecules can be employed as probe DNA of arrays in order to obtain a precious panel of differentially expressed genes.

• Journal of Photoscience
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• 제10권3호
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• pp.237-240
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• 2003

The tetradecameric peptide (K47-K60) near the NH$_2$-terminal region of epithelial-cell adhesion molecule (Ep-CAM) was chosen as antigenic site and a polyclonal antibody was generated, which could recognize Ep-CAM from the mouse colon tissue or the colon cancer cell, CT-26, in Western blot analysis. Then, the fluorescein isothiocyanate (FITC), a fluorescence dye, was conjugated with the affinity purified Ep-CAM antibody using thiocyanate and the amino groups of FITC and antibody, respectively. The molar ratio of FITC to antibody was estimated approximately 1.86 to 1.00 by measuring the optical densities at 492 nm and 280 nm. Ep-CAM antibody-FITC conjugate was then used for immunohistochemistry of the CT-26 cells. Judging from the shapes formed by fluorescence, the Ep-CAM antibody could delivered FITC to the surface of cells in which Ep-CAM was expressed. This result implies that Ep-CAM antibody could be also used for the tissue-specific delivery of the photosensitizer to the target protein via antigen-antibody interaction.

• 센서학회지
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• 제27권5호
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• pp.275-279
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• 2018

In this study, we introduce a sensing platform based on a plasmonic metasurface absorber (MA) with a vertical nanogap for the ultrasensitive detection of monolayer molecules. The vertical nanogap of the MA, where the extremely high near-field is uniformly distributed and exposed to the external environment, is formed by an under-cut structure between a metallic cross nanoantenna and the mirror layer. The accessible sensing area and the enhanced near-field of the MA further enhance the sensitivity of surface-enhanced infrared absorption for the target molecule of 1-octadecanethiol. To provide strong coupling between the molecular vibrations and plasmonic resonance, the design parameters of the MA with a vertical nanogap are numerically designed.