• 한국독성학회:학술대회논문집
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• 한국독성학회 2001년도 International Symposium on Signal transduction in Toxicology
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• pp.130-130
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• 2001

The commercially available paclitaxel product, Taxol$\circledR$ is currently formulated in a vehicle containing approximately a 1:1 v/v mixture of polyoxyethylated castor oil (Cremophor EL) and ethanol. Cremophor EL, a commonly used surfactant for lipophilic compounds, has been associated with many issues, such as adverse effects particularly following rapid administration, stability with the possibility for drug precipitation upon dilution, and filtering requirements.(omitted)

• Maxillofacial Plastic and Reconstructive Surgery
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• 제28권3호
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• pp.193-201
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• 2006

Squamous cell carcinoma(SCC) of head and neck(SCCHN) is the sixth most common human malignant tumor. However, despite advances in prevention and treatment of SCC, the five-year survival rates for patients remain still low. To improve the outcome for patients with SCCHN, novel treatment strategies are needed. Overexpression of the epidermal growth factor(EGF) and activation of its receptor(EGFR) are associated with progressive growth of SCCHN. Vascular endothelial growth factor(VEGF) signaling molecules are related with neoangiogenesis and vascular metastasis of SCC. In this study, we determined the therapeutic effect of AEE788(Novartis Pharma AG, Basel, Switzerland), which is a dual inhibitor of EGFR/ErbB2 and VEGFR tyrosine kinases, on human oral SCC. At first, we screened the expression of EGFR, c-ErbB2(HER-2) and VEGFR-2 in a series of human oral SCC cell lines. And then we evaluated the effects of AEE788 on the phosphorylation of EGFR and VEGFR-2 in a oral SCC cell line expressing EGFR/HER-2 and VEGFR-2. We also evaluated the effects of AEE788 alone, or with paclitaxel(Taxol) on the oral SCC cell growth and apoptosis. As a result, all oral SCC cells expressed EGFR and VEGFR-2. Treatment of oral SCC cells with AEE788 led to dose-dependent inhibition of EGFR and VEGFR-2 phosphorylation, growth inhibition, and induction of apoptosis. Moreover, AEE788 sensitizes the cells to paclitaxel-mediated toxicity and apoptosis. These data mean EGFR and VEGFR-2 can be reliable targets for molecular therapy of oral SCC, and therefore warrant clinical use of EGFR/VEGFR inhibition in the treatment of patients with recurrent or metastatic oral SCC.

• Bulletin of the Korean Chemical Society
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• 제34권6호
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• pp.1800-1808
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• 2013

Dual-responsive amphiphilic block copolymers were synthesized by combining enzymatic ring-opening polymerization (eROP) of ${\varepsilon}$-caprolactone (CL) and ATRP of N,N-dimethylamino-2-ethyl methacrylate (DMAEMA). The obtained block copolymers were characterized by gel permeation chromatography (GPC), $^1H$ NMR and FTIR-IR. The critical micelle concentration (CMC) of copolymer was determined by fluorescence spectra, it can be found that with hydrophilic block (PDMAEMA) increasing, CMC value of the polymer sample increased accordingly, and the CMC value was 0.012 mg/mL, 0.025 mg/mL and 0.037 mg/mL for $PCL_{50}$-b-$PDMAEMA_{68}$, $PCL_{50}$-b-$PDMAEMA_{89}$, $PCL_{50}$-b-$PDMAEMA_{112}$, $PCL_{50}$-b-$PDMAEMA_{89}$ was chosen as drug carrier to study in vitro release profile of anti-cancer drug (taxol). The temperature and pH dependence of the values of hydrodynamic diameter (Dh) of micelles, and self-assembly of the resulting block copolymers in water were evaluated by dynamic light scattering (DLS). The result showed that with the temperature increasing and pH decreasing, the Dh decreased. Drug-loaded nanoparticles were fabricated using paclitaxel as model. Transmission electron microscopy (TEM) and atomic force microscopy (AFM) had been explored to study the morphology of the hollow micelles and the nanoparticles, revealing well-dispersed spheres with the average diameters both around 80 nm. In vitro release kinetics of paclitaxel from the nanoparticles was also investigated in different conditions (pH and temperature, etc.), revealing that the drug release was triggered by temperature changes upon the lower critical solution temperature (LCST) at pH 7.4, and at $37^{\circ}C$ by an increase of pH.

• Asian Pacific Journal of Cancer Prevention
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• 제16권13호
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• pp.5169-5173
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• 2015

To determine the efficacy of postoperative adjuvant chemotherapy with paclitaxel plus cisplatin (Taxol + DDP, TP therapy) for stage IIA esophageal squamous cell carcinoma (ESCC) and to investigate the expression of RUNX3 in lymph node metastasis-negative esophageal cancer and its relationship with medical prognosis, a retrospective summary of clinical treatment of 143 cases of stage IIA esophageal squamous cell carcinoma patients was made. The patients were divided into two groups, a surgery alone control group (52 patients) and a chemotherapy group that received postoperative TP therapy (91 patients). The disease-free and 5 year survival rates were compared between the groups and a multivariate analysis of prognostic factors was performed. The same analysis was performed for cases classified as RUNX3 positive and negative, with post-operative specimens assessed by immunohistochemistry. Although the disease-free and 5 year survival rates in control and chemotherapy groups did not significantly differ and there was no significance in RUNX3 negative cases, postoperative adjuvant chemotherapy in the chemotherapy group was shown to improve disease-free and 5 year survival rate compared to the control group in RUNX3 positive cases. On Cox regression multivariate analysis, postoperative adjuvant chemotherapy (P<0.01) was an independent prognostic factor for RUNX3 positive cases, suggesting that postoperative TP may be effective as adjuvant chemotherapy for stage IIA esophageal cancer patients with RUNX3 positive lesions.

• Journal of Gastric Cancer
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• 제5권4호
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• pp.252-259
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• 2005

위에 발생하는 원발성 소세포암은 매우 드물며 예후는 좋지 않아 초기에 발견되어도 60% 이상이 1년 이내에 사망한다. 본원 외과에서 수술치료를 받은 위소세포암 첫 번째 증례는 수술소견상 복막전이 소견 등으로 근치적 수술이 불가능하여 위공장문합술을 시행하였다. 수술 후 etoposide, cisplatin화학요법을 시행하고 6개월 뒤에 찍은 CT촬영상 복막전이, 림프절전이가 악화되어 paclitaxel, cisplatin으로 약제변경 하였으나 수술 후 14개월째 사망하였다. 두 번째 증례는 내시경 조직검사상 위선암과 소세포암의 복합 소견을 보였으며 CT 촬영상 복강동맥주위 림프절종대 및 간전이 소견이 발견되었다. TS-1과 cisplatin 선행화학요법 2차 시행 후 림프절 종대는 완전관해, 원발소 및 간전이소는 부분관해 소견을 보여 위전절제술 및 확대림프절 절제술을 시행하였다. 수술로 절제된 위 및 주변 림프절 35개의 조직검사상 암세포가 모두 사멸되었으며 위내 원 발병소는 심한 심유화변성 소견을 보여 수술 전 사용한 항암요법이 유의했다고 판단되었다. 이에 수술 후에도 동일 제제로 4차례 추가 투약을 하였다. 수술 후 6개월에 시행한 CT촬영상 간전이가 진행된 소견을 보여 간우엽 후부절제술을 시행하고 이후 ininotecan과 cisplatin을 이용한 항암화학요법을 5차례 시행하고 있으며 술 후 14개월째 생존 중이다. 세 번째 증례는 순수 소세포암으로 근치적 위아전절제술을 시행하였으며 수술 후 5차례에 걸쳐 TS-1, cisplatin 보조항암화학요법 시행하였고 수술 후 13개월째 재발 없이 생존 중이다.