Cancers, Vol. 11, Pages 1245: Novel Carbazole-Piperazine Hybrid Small Molecule Induces Apoptosis by Targeting BCL-2 and Inhibits Tumor Progression in Lung Adenocarcinoma in Vitro and Xenograft Mice Model

Cancers, Vol. 11, Pages 1245: Novel Carbazole-Piperazine Hybrid Small Molecule Induces Apoptosis by Targeting BCL-2 and Inhibits Tumor Progression in Lung Adenocarcinoma in Vitro and Xenograft Mice Model Cancers doi: 10.3390/cancers11091245 Authors: Mongre Mishra Prakash Jung Lee Kumari Hong Lee Lung cancer is a type of deadly cancer and a leading cause of cancer associated death worldwide. BCL-2 protein is considered as an imperative target for the treatment of cancer due to their significant involvement in cell survival and death. A carbazole-piperazine hybrid molecule ECPU-0001 was designed and synthesized as a potent BCL-2 targeting agent with effective anticancer cancer activity. Interaction of ECPU-001 has been assessed by docking, molecular dynamics (MD) simulation, and thermal shift assay. Further, in vitro and in vivo anticancer activity was executed by cytotoxicity assay, FACS, colony formation and migration assay, western blotting, immunocyto/histochemistry and xenograft nude mice model. Molecular docking and MD simulation study confirmed that ECPU-0001 nicely interacts with the active site of BCL-2 by displaying a Ki value of 5.72 µM and binding energy (ΔG) of –8.35 kcal/mol. Thermal shift assay also validated strong interaction of this compound with BCL-2. ECPU-0001 effectively exerted a cytotoxic effect against lung adenocarnoma cells A459 with an IC50 value of 1.779 µM. Molecular mechanism of...
Source: Cancers - Category: Cancer & Oncology Authors: Tags: Article Source Type: research

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Cancers, Vol. 11, Pages 1411: Programmed Death–Ligand 1 and Vimentin: A Tandem Marker as Prognostic Factor in NSCLC Cancers doi: 10.3390/cancers11101411 Authors: Julien Ancel Philippe Birembaut Maxime Dewolf Anne Durlach Béatrice Nawrocki-Raby Véronique Dalstein Gonzague Delepine Silvia Blacher Gaëtan Deslée Christine Gilles Myriam Polette In non-metastatic non-small-cell lung cancer (NSCLC), outcomes remain poor. Adjuvant chemotherapies provide a limited improvement in disease-free survival. Recent exploratory studies on early-stage NSCLC show that immunotherapy ...
Source: Cancers - Category: Cancer & Oncology Authors: Tags: Article Source Type: research
A trio of genetic pathway inhibiting compounds shrunk lung tumors in mice and human cancer cells caused by a mutation in the KRAS gene, suggesting a new treatment method for adenocarcinomas.
Source: Health News - UPI.com - Category: Consumer Health News Source Type: news
AbstractObjectivesThe aim of this study is to evaluate the surgical results of clinical N1 disease and to clarify the high-risk clinical N1 subgroup.MethodsBetween 1990 and 2012, 137 patients who were clinically diagnosed as having N1 disease were enrolled. Their medical records were reviewed to assess clinical characteristics, radiologic findings, pathologic results, postoperative outcomes, recurrence patterns, and survival. Logistic regression analysis was used to identify independent predictive factors for pathologic N2 upstaging. To determine which factors were significantly associated with survival, a multivariate ana...
Source: General Thoracic and Cardiovascular Surgery - Category: Cardiovascular & Thoracic Surgery Source Type: research
KRAS represents an excellent therapeutic target in lung cancer, the most commonly mutated form of which can now be blocked using KRAS-G12C mutant-specific inhibitory trial drugs. Lung adenocarcinoma cells harboring KRAS mutations have been shown previously to be selectively sensitive to inhibition of mitogen-activated protein kinase kinase (MEK) and insulin-like growth factor 1 receptor (IGF1R) signaling. Here, we show that this effect is markedly enhanced by simultaneous inhibition of mammalian target of rapamycin (mTOR) while maintaining selectivity for the KRAS-mutant genotype. Combined mTOR, IGF1R, and MEK inhibition i...
Source: Science Translational Medicine - Category: Biomedical Science Authors: Tags: Research Articles Source Type: research
In this study, we assessed sCD27 levels in patients with advanced lung cancer and determined their correlation with survival and clinicopathologic parameters. METHODS: Serum samples were collected from patients with advanced lung cancer, and sCD27 was quantified via enzyme-linked immunosorbent assay. The association between sCD27 levels and clinicopathologic status and patient survival was retrospectively analyzed. RESULTS: Of 96 patients analyzed, 73 had adenocarcinoma, 7 had squamous cell carcinoma, and 15 had small cell carcinoma. Median serum sCD27 level was 36.54 U/mL (range, undetectable-104.47); this is lo...
Source: Oncology - Category: Cancer & Oncology Authors: Tags: Oncology Source Type: research
-Vila Rafael Rosell BRAF V600 mutations have been found in 1–2% of non-small-cell lung cancer (NSCLC) patients, with Food and Drug Administration (FDA) approved treatment of dabrafenib plus trametinib and progression free survival (PFS) of 10.9 months. However, 50–80% of BRAF mutations in lung cancer are non-V600, and can be class II, with intermediate to high kinase activity and RAS independence, or class III, with impaired kinase activity, upstream signaling dependence, and consequently, sensitivity to receptor tyrosine kinase (RTK) inhibitors. Plasma cell-free DNA (cfDNA) of 185 newly diagnosed...
Source: Cancers - Category: Cancer & Oncology Authors: Tags: Article Source Type: research
CONCLUSION: ERGIC3 silencing in combination with BFA treatment could additively inhibit lung cancer cell growth. This finding might shed a light on new adjuvant therapy for lung adenocarcinoma. PMID: 31530266 [PubMed - as supplied by publisher]
Source: Current Cancer Drug Targets - Category: Cancer & Oncology Authors: Tags: Curr Cancer Drug Targets Source Type: research
Lung cancer is the leading cause of cancer-related mortality worldwide [1]. Despite advancements in diagnostic modalities and surgical techniques in recent decades, the recurrence rate of lung cancer after curative resection is still high at up to 30 –55% [2].
Source: Lung Cancer - Category: Cancer & Oncology Authors: Source Type: research
Conclusion Gefitinib, erlotinib, and afatinib have similar effectiveness in advanced stage N SCLC with EGFR mutation positive. Afatinib tends to be associated with longer PFS but further investigation is required. DOI: 10.3779/j.issn.1009-3419.2019.09.02
Source: Chinese Journal of Lung Cancer - Category: Cancer & Oncology Source Type: research
Conclusion Patients who has lower mutation abundance with EGFR sensitive mutations after TKI treatment may have a longer survival period (P
Source: Chinese Journal of Lung Cancer - Category: Cancer & Oncology Source Type: research
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