TW37 enhances the pro-apoptosis and anti-migration ability of gefitinib in Non-Small Cell Lung Cancer

Chen, Xiaofan; Mao, Guangxian; Chen, Hua; Liu, Suyue; Wang, Sichao; Li, Xiaoqiang; Ye, Yiwang; Wu, Hao; Liu, Jixian

doi:10.14715/cmb/2018.64.4.2

Cited by 7 publications

(7 citation statements)

References 32 publications

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“…Currently, available diagnosis methods for lung cancer include chest radiographs, computed tomography (CT) scans and biopsy (5). In this scenario, to achieve better prognosis outcomes, identification of early lung cancer biomarkers or development of new diagnosis techniques that could detect lung cancer at earlier stage would be promising research directions (4,8).…”

Section: Introductionmentioning

confidence: 99%

Levels of serum bilirubin in small cell lung cancer and non-small cell lung cancer patients

Jiang

Shi

Yuan

et al. 2018

Cell Mol Biol (Noisy-le-grand)

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Elevated bilirubin has been associated with protection of cardiovascular and kidney systems, whereas decreased bilirubin may predispose respiratory diseases. However, whether serum bilirubin levels are associated with lung cancer remains unclear. Here, clinical and pathologic data of a cohort of 363 lung cancer patients along with 363 age-and gender-matched healthy subjects were collected. The association of serum bilirubin levels with lung cancer was analyzed. The levels of serum bilirubin were significantly lower in lung cancer patients. The aspartate transaminase and alkaline phosphatase levels were significantly higher in lung cancer. Multi-classification logistics regression analysis revealed low total bilirubin level [OR (95%CI), 1.12 (1.02-1.23)], aspartate transaminase [OR (95%CI), 1.12 (1.02-1.23)], and alanine transaminase [OR (95%CI), 1.12 (1.02-1.23)] were risk factors in lung cancer. Serum bilirubin levels were significantly changed among small cell lung cancer (SCLC), lung adenocarcinoma (LAC) and lung squamous cell carcinoma (LSC). Total bilirubin level, smoke history and heart disease were risk factors for subtypes. Compared with LSC, patients with smoke history had significant higher risk in LAC [OR (95% Confidence Interval, CI), 4. 49 (1.70, 11.96)]. Compared with LSC, patients with smoke history [OR (95%CI), 4.49 (1.70, 11.96)] and heart disease [OR (95%CI), 4.49 (1.70, 11.96)] had significant higher risk in SCLC. Compared with SCLC, patients with low total bilirubin [OR (95%CI), 1.12 (1.02-1.23)] and heart disease [OR (95%CI), 3.52(1.01-12.23)] had significant higher risk in LAC. Taken together, these results suggested low serum bilirubin levels are tightly associated with lung cancer, especially with LAC. Serum bilirubin levels might serve as a predictor for lung cancer patients clinically.

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Section: Introductionmentioning

confidence: 99%

Levels of serum bilirubin in small cell lung cancer and non-small cell lung cancer patients

Jiang

Shi

Yuan

et al. 2018

Cell Mol Biol (Noisy-le-grand)

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“…Interestingly, all the six anticancer drugs from the PPIs inhibitor category (category A) demonstrated the lowest IC 50 values against DENV NS2B/NS3 protease. Among them, four compounds, namely ABT263, ABT737, TW37, and AT101, are well-characterized Bcl-2 inhibitors [31][32][33][34][35] and exhibited the highest potency against the protease with decent IC 50 values of 0.86 ± 0.08, 1.15 ± 0.21, 0.89 ± 0.04, and 0.81 ± 0.08 μM, respectively (Table 1 and Figure 2).…”

Section: Determination Of Ic 50 Values Of Confirmed Hitsmentioning

confidence: 99%

Repurposing of investigational cancer drugs: Early phase discovery of dengue virus NS2B/NS3 protease inhibitors

Saleem,

Kousar,

Jiskani

et al. 2023

Archiv der Pharmazie

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Dengue fever is a neglected vector‐borne disease and is more prevalent in Asia. Currently, no specific treatment is available. Given the time and cost of de novo drug discovery and development, an alternative option of drug repurposing is becoming an effective tool. We screened a library of 1127 pharmacologically active, metabolically stable, and structurally diverse small anticancer molecules to identify inhibitors of the dengue virus (DENV) NS2B/NS3 protease. Enzyme kinetics and inhibition data revealed four B‐cell lymphoma 2 inhibitors, that is, ABT263, ABT737, AT101, and TW37, as potent inhibitors of DENV NS2B/NS3 protease, with IC50 values of 0.86, 1.15, 0.81, and 0.89 µM, respectively. Mode of inhibition experiments and computational docking analyses indicated that ABT263 and ABT737 are competitive inhibitors, whereas AT101 and TW37 are noncompetitive inhibitors of the protease. With further evaluation, the identified inhibitors of the DENV NS2B/NS3 protease have the potential to be developed into specific anti‐dengue therapeutics.

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“…Danusertib, an aurora kinase inhibitor [82], was investigated in treating advanced solid tumors including NSCLC in phase I [83] and phase II [84] clinical studies, in which single-agent danusertib was well tolerated and showed marginal anti-tumor activity in common solid tumor types. TW-37, a small molecule inhibitor of B-cell lymphoma 2 (Bcl-2) family proteins [85], enhanced the pro-apoptosis and anti-migration ability of gefitinib in NSCLC [86]. TG-101348, an inhibitor of Janus kinase 2 (JAK2), reduced PD-L1 protein expression [87] and reversed erlotinib resistance in NSCLC cells [88].…”

Section: Carboplatinmentioning

confidence: 99%

Single B Cell Gene Co-Expression Networks Implicated in Prognosis, Proliferation, and Therapeutic Responses in Non-Small Cell Lung Cancer Bulk Tumors

Guo

2022

Cancers

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In NSCLC, there is a pressing need for immunotherapy predictive biomarkers. The processes underlying B-cell dysfunction, as well as their prognostic importance in NSCLC, are unknown. Tumor-specific B-cell gene co-expression networks were constructed by comparing the Boolean implication modeling of single-cell RNA sequencing of NSCLC tumor B cells and normal B cells. Proliferation genes were selected from the networks using in vitro CRISPR-Cas9/RNA interfering (RNAi) screening data in more than 92 human NSCLC epithelial cell lines. The prognostic and predictive evaluation was performed using public NSCLC transcriptome and proteome profiles. A B cell proliferation and prognostic gene co-expression network was present only in normal lung B cells and missing in NSCLC tumor B cells. A nine-gene signature was identified from this B cell network that provided accurate prognostic stratification using bulk NSCLC tumor transcriptome (n = 1313) and proteome profiles (n = 103). Multiple genes (HLA-DRA, HLA-DRB1, OAS1, and CD74) differentially expressed in NSCLC B cells, peripheral blood lymphocytes, and tumor T cells had concordant prognostic indications at the mRNA and protein expression levels. The selected genes were associated with drug sensitivity/resistance to 10 commonly used NSCLC therapeutic regimens. Lestaurtinib was discovered as a potential repositioning drug for treating NSCLC.

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TW37 enhances the pro-apoptosis and anti-migration ability of gefitinib in Non-Small Cell Lung Cancer

Cited by 7 publications

References 32 publications

Levels of serum bilirubin in small cell lung cancer and non-small cell lung cancer patients

Levels of serum bilirubin in small cell lung cancer and non-small cell lung cancer patients

Repurposing of investigational cancer drugs: Early phase discovery of dengue virus NS2B/NS3 protease inhibitors

Single B Cell Gene Co-Expression Networks Implicated in Prognosis, Proliferation, and Therapeutic Responses in Non-Small Cell Lung Cancer Bulk Tumors

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