scholarly journals Identification of a potent kinase inhibitor targeting EML4-ALK fusion protein in non-small cell lung cancer

MedChemComm ◽  
2017 ◽  
Vol 8 (10) ◽  
pp. 1914-1918
Author(s):  
Lian-Xiang Luo ◽  
Ying Li ◽  
Yu-Zhen Niu ◽  
Yu-Wei Wang ◽  
Qian-Qian Wang ◽  
...  

Herein, we reported 5067-0952, a potent ALK inhibitor with pharmacological efficacy in non-small cell lung cancers harboring the ALK fusion oncogene.

Author(s):  
Sajad Khan ◽  
Shahid Ali ◽  
Muhammad

Background:Lung cancers or (Bronchogenic-Carcinomas) are the disease in certain parts of the lungs in which irresistible multiplication of abnormal cells leads to the inception of a tumor. Lung cancers consisting of two substantial forms based on the microscopic appearance of tumor cells are: Non-Small-Cell-Lung-Cancer (NSCLC) (80 to 85%) and Small-Cell-Lung-Cancer (SCLC) (15 to 20%).Discussion:Lung cancers are existing luxuriantly across the globe and the most prominent cause of death in advanced countries (USA & UK). There are many causes of lung cancers in which the utmost imperative aspect is the cigarette smoking. During the early stage, there is no perspicuous sign/symptoms but later many symptoms emerge in the infected individual such as insomnia, headache, pain, loss of appetite, fatigue, coughing etc. Lung cancers can be diagnosed in many ways, such as history, physical examination, chest X-rays and biopsy. However, after the diagnosis and confirmation of lung carcinoma, various treatment approaches are existing for curing of cancer in different stages such as surgery, radiation therapy, chemotherapy, and immune therapy. Currently, novel techniques merged that revealed advancements in detection and curing of lung cancer in which mainly includes: microarray analysis, gene expression profiling.Conclusion:Consequently, the purpose of the current analysis is to specify and epitomize the novel literature pertaining to the development of cancerous cells in different parts of the lung, various preeminent approaches of prevention, efficient diagnostic procedure, and treatments along with novel technologies for inhibition of cancerous cell growth in advance stages.


Lung Cancer ◽  
2014 ◽  
Vol 85 (2) ◽  
pp. 245-250 ◽  
Author(s):  
Julian R. Molina ◽  
Nathan R. Foster ◽  
Thanyanan Reungwetwattana ◽  
Garth D. Nelson ◽  
Andrew V. Grainger ◽  
...  

2021 ◽  
Vol 49 (5) ◽  
pp. 030006052110165
Author(s):  
Naiwang Tang ◽  
Bin Hu ◽  
Yin Zhang ◽  
Zhiwei Chen ◽  
Ronghuan Yu

Background Small-cell lung cancer (SCLC) accounts for approximately 15% to 20% of all lung cancers, and it is the leading cause of tumor-related deaths globally. This study explored the molecular mechanisms underlying the development of SCLC. Methods The correlations of phosphoinositide-dependent kinase-1 (PDPK1), p-Akt, and Hedgehog expression with patient characteristics were analyzed using SCLC specimens, and their expression was measured in BEAS-2B cells (control) and the SCLC cell lines H82, H69, H446, H146, and H526. Transfection experiments were performed to inhibit or activate gene expression in cells. We then measured the proliferation and migration of H146 cells. Results PDPK1, p-Akt, and Hedgehog expression was significantly higher in SCLC tissues, and their expression was correlated with patient characteristics. p-Akt expression was significantly correlated with Hedgehog expression. In H146 cells, PDPK1 and p-Akt were significantly upregulated. Silencing of PDPK1 or Akt and inhibition of Hedgehog significantly inhibited the proliferation and migration of H146 cells. PDPK1 and Akt affected Hedgehog expression, but Hedgehog did not affect PDPK1 or p-Akt expression. Conclusions The interaction between the PDPK1–Akt pathway and the Hedgehog pathway influences the prognosis, growth, and migration of SCLC.


2012 ◽  
Vol 66 (3) ◽  
pp. 221-227 ◽  
Author(s):  
Xueying Yang ◽  
Jing Di ◽  
Yang Zhang ◽  
Suning Zhang ◽  
Jibin Lu ◽  
...  

Open Medicine ◽  
2021 ◽  
Vol 16 (1) ◽  
pp. 1160-1167
Author(s):  
Xing Chai ◽  
Xinru Zhang ◽  
Wenqian Li ◽  
Jin Chai

Abstract Lung cancer is the most common cause of cancer-related death. Non-small cell lung cancer (NSCLC) and small cell lung cancer (SCLC) are the two major histological categories of lung cancers. Drug resistance is a great challenge for cancer treatment, and histological transformation from NSCLC to SCLC is one of the mechanisms underlying drug resistance in NSCLC patients. SCLC-transformed patients show combined characteristics of NSCLC and SCLC; however, they lack timely diagnoses and effective treatment strategies. Thus, we reviewed the clinical characteristics of SCLC transformation patients with a literature search to enhance clinical consciousness, diagnosis, and personalized treatment for patients with it.


Author(s):  
Jennifer W. Carlisle ◽  
R. Donald Harvey

The number of therapeutic options available for patients with advanced non–small-cell lung cancer has been led by deeper understanding of molecular drivers, immune function, and fundamental biology. In this article, we describe the relevant clinical pharmacologic characteristics of three broad classes of existing and investigational treatments, with a focus on mechanisms of action, adverse event profiles, pharmacokinetic and pharmacodynamic properties, and known and predicted resistance pathways. Specifically, within the kinase inhibitor class, agents directed against the RET, MET, and KRAS pathways are reviewed. Additionally, the first antibody-drug conjugates that target HER2 and HER3 are in trials and will ideally be available for patients soon. Finally, proteolysis-targeting chimeras approach pathway inhibition through enzyme degradation rather than target inhibition and are a promising platform for new agents in non–small-cell lung cancer and across cancer types. Each of these classes requires knowledge of clinical pharmacologic principles in development and use to ensure patient care in clinics and trials is optimized and personalized, including dosing and scheduling strategies, potential drug interactions, use in special populations, and monitoring parameters. Ideally, oncologists will continue to have new agents available across the non–small-cell lung cancer treatment spectrum to offer to a patient group that, until relatively recently, had few options.


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