1.Comparison of Anticancer Effects of Histone Deacetylase Inhibitors CG-745 and Suberoylanilide Hydroxamic Acid in Non-small Cell Lung Cancer
Hyo Jin KIM ; Ui Ri AN ; Han Jee YOON ; Hyun LIM ; Ki Eun HWANG ; Young Suk KIM ; Hak Ryul KIM
Tuberculosis and Respiratory Diseases 2025;88(2):342-352
Background:
Histone deacetylase (HDAC) inhibition offers potential anticancer effects across diverse cancers due to HDAC's significant role in cancer development and progression. Consequently, we demonstrated the therapeutic efficacy of the novel HDAC inhibitor, CG-745, in comparison with existing inhibitors such as suberoylanilide hydroxamic acid (SAHA) in non-small cell lung cancer (NSCLC) cells.
Methods:
CG-745's effect on apoptosis and reactive oxygen species (ROS)-dependent mitochondrial dysfunction was investigated using annexin V assay, MitoSoX, and Western blot in human A549 and H460 cells. Additionally, HDAC expression was analyzed through real-time polymerase chain reaction. We also evaluated the inhibitory effect of CG-745 on epithelial-mesenchymal transition (EMT) induced by transforming growth factor β1 (TGF-β1) via Western blot, scratch analysis, and matrigel invasion analysis.
Results:
Compared to SAHA, CG-745 inhibited cell viability and mRNA expression of HDACs such as HDAC1, HDAC2, HDAC3, and HDAC8. It also induced apoptosis, ROS, and mitochondrial dysfunction in a concentration-dependent manner. CG-745 reversed EMT triggered by TGF-β1 in A549 and H460 cells, and curtailed the migration and invasion enhanced by TGF-β1. CG-745 has demonstrably inhibited EMT and induced apoptosis in NSCLC cells.
Conclusion
CG-745 may represent a novel therapeutic strategy for NSCLC treatment.
2.Comparison of Anticancer Effects of Histone Deacetylase Inhibitors CG-745 and Suberoylanilide Hydroxamic Acid in Non-small Cell Lung Cancer
Hyo Jin KIM ; Ui Ri AN ; Han Jee YOON ; Hyun LIM ; Ki Eun HWANG ; Young Suk KIM ; Hak Ryul KIM
Tuberculosis and Respiratory Diseases 2025;88(2):342-352
Background:
Histone deacetylase (HDAC) inhibition offers potential anticancer effects across diverse cancers due to HDAC's significant role in cancer development and progression. Consequently, we demonstrated the therapeutic efficacy of the novel HDAC inhibitor, CG-745, in comparison with existing inhibitors such as suberoylanilide hydroxamic acid (SAHA) in non-small cell lung cancer (NSCLC) cells.
Methods:
CG-745's effect on apoptosis and reactive oxygen species (ROS)-dependent mitochondrial dysfunction was investigated using annexin V assay, MitoSoX, and Western blot in human A549 and H460 cells. Additionally, HDAC expression was analyzed through real-time polymerase chain reaction. We also evaluated the inhibitory effect of CG-745 on epithelial-mesenchymal transition (EMT) induced by transforming growth factor β1 (TGF-β1) via Western blot, scratch analysis, and matrigel invasion analysis.
Results:
Compared to SAHA, CG-745 inhibited cell viability and mRNA expression of HDACs such as HDAC1, HDAC2, HDAC3, and HDAC8. It also induced apoptosis, ROS, and mitochondrial dysfunction in a concentration-dependent manner. CG-745 reversed EMT triggered by TGF-β1 in A549 and H460 cells, and curtailed the migration and invasion enhanced by TGF-β1. CG-745 has demonstrably inhibited EMT and induced apoptosis in NSCLC cells.
Conclusion
CG-745 may represent a novel therapeutic strategy for NSCLC treatment.
3.Comparison of Anticancer Effects of Histone Deacetylase Inhibitors CG-745 and Suberoylanilide Hydroxamic Acid in Non-small Cell Lung Cancer
Hyo Jin KIM ; Ui Ri AN ; Han Jee YOON ; Hyun LIM ; Ki Eun HWANG ; Young Suk KIM ; Hak Ryul KIM
Tuberculosis and Respiratory Diseases 2025;88(2):342-352
Background:
Histone deacetylase (HDAC) inhibition offers potential anticancer effects across diverse cancers due to HDAC's significant role in cancer development and progression. Consequently, we demonstrated the therapeutic efficacy of the novel HDAC inhibitor, CG-745, in comparison with existing inhibitors such as suberoylanilide hydroxamic acid (SAHA) in non-small cell lung cancer (NSCLC) cells.
Methods:
CG-745's effect on apoptosis and reactive oxygen species (ROS)-dependent mitochondrial dysfunction was investigated using annexin V assay, MitoSoX, and Western blot in human A549 and H460 cells. Additionally, HDAC expression was analyzed through real-time polymerase chain reaction. We also evaluated the inhibitory effect of CG-745 on epithelial-mesenchymal transition (EMT) induced by transforming growth factor β1 (TGF-β1) via Western blot, scratch analysis, and matrigel invasion analysis.
Results:
Compared to SAHA, CG-745 inhibited cell viability and mRNA expression of HDACs such as HDAC1, HDAC2, HDAC3, and HDAC8. It also induced apoptosis, ROS, and mitochondrial dysfunction in a concentration-dependent manner. CG-745 reversed EMT triggered by TGF-β1 in A549 and H460 cells, and curtailed the migration and invasion enhanced by TGF-β1. CG-745 has demonstrably inhibited EMT and induced apoptosis in NSCLC cells.
Conclusion
CG-745 may represent a novel therapeutic strategy for NSCLC treatment.
4.Comparison of Anticancer Effects of Histone Deacetylase Inhibitors CG-745 and Suberoylanilide Hydroxamic Acid in Non-small Cell Lung Cancer
Hyo Jin KIM ; Ui Ri AN ; Han Jee YOON ; Hyun LIM ; Ki Eun HWANG ; Young Suk KIM ; Hak Ryul KIM
Tuberculosis and Respiratory Diseases 2025;88(2):342-352
Background:
Histone deacetylase (HDAC) inhibition offers potential anticancer effects across diverse cancers due to HDAC's significant role in cancer development and progression. Consequently, we demonstrated the therapeutic efficacy of the novel HDAC inhibitor, CG-745, in comparison with existing inhibitors such as suberoylanilide hydroxamic acid (SAHA) in non-small cell lung cancer (NSCLC) cells.
Methods:
CG-745's effect on apoptosis and reactive oxygen species (ROS)-dependent mitochondrial dysfunction was investigated using annexin V assay, MitoSoX, and Western blot in human A549 and H460 cells. Additionally, HDAC expression was analyzed through real-time polymerase chain reaction. We also evaluated the inhibitory effect of CG-745 on epithelial-mesenchymal transition (EMT) induced by transforming growth factor β1 (TGF-β1) via Western blot, scratch analysis, and matrigel invasion analysis.
Results:
Compared to SAHA, CG-745 inhibited cell viability and mRNA expression of HDACs such as HDAC1, HDAC2, HDAC3, and HDAC8. It also induced apoptosis, ROS, and mitochondrial dysfunction in a concentration-dependent manner. CG-745 reversed EMT triggered by TGF-β1 in A549 and H460 cells, and curtailed the migration and invasion enhanced by TGF-β1. CG-745 has demonstrably inhibited EMT and induced apoptosis in NSCLC cells.
Conclusion
CG-745 may represent a novel therapeutic strategy for NSCLC treatment.
5.Comparison of Anticancer Effects of Histone Deacetylase Inhibitors CG-745 and Suberoylanilide Hydroxamic Acid in Non-small Cell Lung Cancer
Hyo Jin KIM ; Ui Ri AN ; Han Jee YOON ; Hyun LIM ; Ki Eun HWANG ; Young Suk KIM ; Hak Ryul KIM
Tuberculosis and Respiratory Diseases 2025;88(2):342-352
Background:
Histone deacetylase (HDAC) inhibition offers potential anticancer effects across diverse cancers due to HDAC's significant role in cancer development and progression. Consequently, we demonstrated the therapeutic efficacy of the novel HDAC inhibitor, CG-745, in comparison with existing inhibitors such as suberoylanilide hydroxamic acid (SAHA) in non-small cell lung cancer (NSCLC) cells.
Methods:
CG-745's effect on apoptosis and reactive oxygen species (ROS)-dependent mitochondrial dysfunction was investigated using annexin V assay, MitoSoX, and Western blot in human A549 and H460 cells. Additionally, HDAC expression was analyzed through real-time polymerase chain reaction. We also evaluated the inhibitory effect of CG-745 on epithelial-mesenchymal transition (EMT) induced by transforming growth factor β1 (TGF-β1) via Western blot, scratch analysis, and matrigel invasion analysis.
Results:
Compared to SAHA, CG-745 inhibited cell viability and mRNA expression of HDACs such as HDAC1, HDAC2, HDAC3, and HDAC8. It also induced apoptosis, ROS, and mitochondrial dysfunction in a concentration-dependent manner. CG-745 reversed EMT triggered by TGF-β1 in A549 and H460 cells, and curtailed the migration and invasion enhanced by TGF-β1. CG-745 has demonstrably inhibited EMT and induced apoptosis in NSCLC cells.
Conclusion
CG-745 may represent a novel therapeutic strategy for NSCLC treatment.
6.The efficacy and safety of DW1601 in patients with acute bronchitis: a multi-center, randomized, double-blind, phase III clinical trial
Young Seok LEE ; Seong Yong LIM ; Kyung Hoon MIN ; Do Jin KIM ; Kwang Ha YOO ; Tae-Bum KIM ; Hak-Ryul KIM ; Jae Jeong SHIM
The Korean Journal of Internal Medicine 2022;37(6):1195-1204
Background/Aims:
DW1601, an oral fixed dose combination syrup composed of DW16011 and Pelargonium sidoides, was developed to enhance the symptom relief effect in patients with acute bronchitis. We evaluated the efficacy and safety of DW1601 compared to DW16011 or P. sidoides for treatment of acute bronchitis using a randomized, double-blind, placebocontrolled, multi-centre trial design.
Methods:
A total of 204 patients with acute bronchitis was randomized 1:1:1 to receive DW1601 (n = 67), DW16011 (n = 70), or P. sidoides (n = 64) for 7 days. The primary outcome was efficacy of DW1601 compared to DW16011 or P. sidoides in reducing the total bronchitis severity score (BSS) at day 4 of treatment. Secondary endpoints were changes in total and symptomspecific BSS, response rate and patient satisfaction rate. Safety analysis was assessed at day 7.
Results:
At 4 days after medication, decrease of total BSS from baseline was significantly greater in the DW1601 group than in the DW16011 group (–3.51 ± 0.18 vs. –2.65 ± 0.18, p = 0.001) or P. sidoides group (–3.56 ± 0.18 vs. –2.64 ± 0.19, p < 0.001). In addition, the BSS total score at day 7 and the BSS cough and sputum component scores at days 4 and 7 were significantly more improved with DW1601 treatment compared with the DW16011 group or P. sidoides group. Participants treated with DW1601 showed higher rates of response and satisfaction than control groups (response rate, DW1601, 100% vs. DW16011, 85.7% vs. P. sidoides, 85.9%; satisfaction rate, DW1601, 92.6% vs. DW16011, 82.9% vs. P. sidoides, 81.2%). Significant adverse events were not observed in the DW1601 group.
Conclusions
DW1601 is superior to DW16011 or P. sidoides in improving symptoms of acute bronchitis.
7.Birt-Hogg-Dubé Syndrome Associated with a Renal Tumor
Su Jin OH ; Ki Eun HWANG ; Eun Taik JEONG ; Hak Ryul KIM ; Keum Ha CHOI ; Dae Woong RYU
Korean Journal of Medicine 2019;94(4):379-382
Birt-Hogg-Dubé syndrome (BHD) is a rare autosomal dominant disorder characterized by the formation of hair follicle tumors, kidney tumors, and pulmonary cysts with recurrent spontaneous pneumothorax. A 44-year-old woman visited Wonkwang University Hospital with mild dyspnea. A chest X-ray on admission revealed pneumothorax in both lung fields. Chest computed tomography (CT) revealed both pneumothorax and multiple, irregularly shaped, variable-sized cysts in both lung fields. Upon physical examination, white dome-shaped papules were observed on the face. Histological examination of the skin lesion confirmed fibrofolliculoma, and genetic studies revealed a folliculin gene mutation. Abdominal CT revealed a 1-cm small solid renal mass at the lower pole of the right kidney. We surgically removed the renal tumor, and a histological diagnosis of oncocytoma was made. Here, we report a case of BHD that demonstrated all three clinical manifestations; this is the first case report of its kind in Korea.
Adenoma, Oxyphilic
;
Adult
;
Birt-Hogg-Dube Syndrome
;
Diagnosis
;
Dyspnea
;
Estrone
;
Female
;
Hair Follicle
;
Humans
;
Kidney
;
Kidney Neoplasms
;
Korea
;
Lung
;
Physical Examination
;
Pneumothorax
;
Skin
;
Thorax
;
Tomography, X-Ray Computed
8.Comparison of cobas EGFR Mutation Test v2 and PANAMutyper-R-EGFR for Detection and Semi-Quantification of Epidermal Growth Factor Receptor Mutations in Plasma and Pleural Effusion Supernatant
A Lum HAN ; Hak Ryul KIM ; Keum Ha CHOI ; Ki Eun HWANG ; Mengyu ZHU ; Yuya HUANG ; Moxin WU ; Young Jin LEE ; Min Cheol PARK ; Ji Hyun CHO ; Do Sim PARK
Annals of Laboratory Medicine 2019;39(5):478-487
BACKGROUND: Plasma epidermal growth factor receptor (EGFR) mutation tests are less invasive than tissue EGFR mutation tests. We determined which of two kits is more efficient: cobas EGFR Mutation test v2 (cobasv2; Roche Molecular Systems, Pleasanton, CA, USA) or PANAMutyper-R-EGFR (Mutyper; Panagene, Daejeon, Korea). We also evaluated whether pleural effusion supernatant (PE-SUP) samples are assayable, similar to plasma samples, using these two kits. METHODS: We analyzed 156 plasma and PE-SUP samples (31 paired samples) from 116 individuals. We compared the kits in terms of accuracy, assessed genotype concordance (weighted κ with 95% confidence intervals), and calculated Spearman's rho between semi-quantitatively measured EGFR-mutant levels (SQIs) measured by each kit. We also compared sensitivity using 47 EGFR-mutant harboring samples divided into more-dilute and less-dilute samples (dilution ratio: ≥ or <1:1,000). RESULTS: cobasv2 tended to have higher accuracy than Mutyper (73% vs 69%, P=0.53), and PE-SUP samples had significantly higher accuracy than plasma samples (97% vs 55–71%) for both kits. Genotype concordance was 98% (κ=0.92, 0.88–0.96). SQIs showed strong positive correlations (P<0.0001). In less-dilute samples, accuracy and sensitivity did not differ significantly between kits. In more-dilute samples, cobasv2 tended to have higher sensitivity than Mutyper (43% vs 20%, P=0.07). CONCLUSIONS: The kits have similar performance in terms of EGFR mutation detection and semi-quantification in plasma and PE-SUP samples. cobasv2 tends to outperform Mutyper in detecting less-abundant EGFR-mutants. PE-SUP samples are assayable using either kit.
Epidermal Growth Factor
;
Genotype
;
Plasma
;
Pleural Effusion
;
Receptor, Epidermal Growth Factor
9.Birt-Hogg-Dubé Syndrome Associated with a Renal Tumor
Su Jin OH ; Ki Eun HWANG ; Eun Taik JEONG ; Hak Ryul KIM ; Keum Ha CHOI ; Dae Woong RYU
Korean Journal of Medicine 2019;94(4):379-382
Birt-Hogg-Dubé syndrome (BHD) is a rare autosomal dominant disorder characterized by the formation of hair follicle tumors, kidney tumors, and pulmonary cysts with recurrent spontaneous pneumothorax. A 44-year-old woman visited Wonkwang University Hospital with mild dyspnea. A chest X-ray on admission revealed pneumothorax in both lung fields. Chest computed tomography (CT) revealed both pneumothorax and multiple, irregularly shaped, variable-sized cysts in both lung fields. Upon physical examination, white dome-shaped papules were observed on the face. Histological examination of the skin lesion confirmed fibrofolliculoma, and genetic studies revealed a folliculin gene mutation. Abdominal CT revealed a 1-cm small solid renal mass at the lower pole of the right kidney. We surgically removed the renal tumor, and a histological diagnosis of oncocytoma was made. Here, we report a case of BHD that demonstrated all three clinical manifestations; this is the first case report of its kind in Korea.
10.Computed tomography morphologic features of pulmonary adenocarcinoma with brain/bone metastasis.
Ki Eun HWANG ; Su Jin OH ; Chul PARK ; Se Jeong JEON ; Jeong Mi LEE ; Byong Ki CHA ; Kwon Ha YOON ; Eun Taik JEONG ; Hak Ryul KIM
The Korean Journal of Internal Medicine 2018;33(2):340-346
BACKGROUND/AIMS: Brain and bone metastases are common in patients with lung cancer. The development of metastasis is associated with poor survival in lung cancer patients. Although tumor morphologic features on radiographs are routinely assessed for differentiation between benign and malignant lung nodules, they are not used to predict metastasis. We assessed morphologic features of pulmonary adenocarcinomas with brain/bone metastasis on computed tomography (CT) to identify related factors for metastasis. METHODS: We performed a retrospective analysis of initial chest CT findings (size, type of contour, percentage of necrosis, enhancement, presence or absence of calcification, and air cavity) from 2009 to 2010 of patients with brain or bone metastasis and compared the findings with those of patients without metastases. RESULTS: In total, 128 patients were included (78 men, 52 women; mean age 69 years; range, 36 to 87). Nineteen patients had brain metastases and 32 had bone metastases. Morphologic features associated with brain metastasis included size ≥ 50 mm (odds ratio [OR], 3.37; 95% confidence interval [CI], 1.24 to 9.17; p = 0.013), necrosis ≥ 30% (OR, 4.51; 95% CI, 1.62 to 12.55; p =0.002), and presence of calcification (OR, 3.97; 95% CI, 1.16 to 13.55; p = 0.035). Morphologic features associated with bone metastasis included necrosis ≥ 30% (OR, 4.639; 95% CI, 1.98 to 10.82; p < 0.001) and T 3 to 4 stage (OR, 2.53; 95% CI, 1.07 to 6.00; p = 0.031). CONCLUSIONS: We found that necrosis ≥ 30% was associated with pulmonary adenocarcinoma with brain and bone metastasis at initial chest CT morphologic feature. To validate these results, further research should be conducted.
Adenocarcinoma*
;
Brain
;
Female
;
Humans
;
Lung
;
Lung Neoplasms
;
Male
;
Necrosis
;
Neoplasm Metastasis*
;
Retrospective Studies
;
Tomography, X-Ray Computed

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