The natural product berberine synergizes with osimertinib preferentially against MET-amplified osimertinib-resistant lung cancer via direct MET inhibition.
TLDR
In this paper, the authors showed that berberine was able to bind to the kinase domain of non-phosphorylated MET, occupy the front of the binding pocket, and interact with the activation loop, in a similar way as other known MET inhibitors do.About:
This article is published in Pharmacological Research.The article was published on 2022-01-01 and is currently open access. It has received 11 citations till now. The article focuses on the topics: Osimertinib & T790M.read more
Citations
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Protein tyrosine kinase inhibitor resistance in malignant tumors: molecular mechanisms and future perspective
TL;DR: In this article , the authors reviewed the drug resistance mechanisms of TKIs and the potential approaches to overcome TKI resistance, aiming to provide a theoretical basis for improving the efficacy of PTKIs.
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Anticancer Effects and Mechanisms of Berberine from Medicinal Herbs: An Update Review
Ruoxuan Xiong,Si-Yu Huang,Silan Wu,Dan Zhou,Zhi-jun Yang,Adila Saimaiti,Cai-Ning Zhao,Ao Shang,Yunjian Zhang,Ren-You Gan,Hua-Bin Li +10 more
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Multi-Target Potential of Berberine as an Antineoplastic and Antimetastatic Agent: A Special Focus on Lung Cancer Treatment
TL;DR: In this paper , a review of molecular insights of Berberine and its various derivative-induced antiproliferative and antimetastatic effects against lung cancer is presented, where the authors aim to provide a better understanding of molecular insight of the Alkaloid and its derivatives.
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Role of natural P-gp inhibitor in the effective delivery for chemotherapeutic agents
TL;DR: The significant objective of the present review is surfing through the impact of natural P-gp inhibitors having basic structures derived from the plant sources and how it inhibits the resistance of chemotherapeutic drugs together with how well it delivers chemotherapy medicines.
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The prospect of combination therapies with the third-generation EGFR-TKIs to overcome the resistance in NSCLC
Shiyu Li,Shuangli Zhu,H. Wei,Pengfei Zhu,Ying Jiao,Ming Yi,Juejun Gong,Kunpeng Zheng,Li Zhang +8 more
TL;DR: The third-generation EGFR-TKIs target T790M mutation and show potent anti-tumor efficacy, especially in central neural system response as discussed by the authors , but patients inevitably develop the acquired resistance to the first- or second-generative EGFRTKI after a period of treatment, and EGFR T790m mutation is the most common resistant mechanism.
References
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Global Cancer Statistics 2020: GLOBOCAN Estimates of Incidence and Mortality Worldwide for 36 Cancers in 185 Countries.
Hyuna Sung,Jacques Ferlay,Rebecca L. Siegel,Mathieu Laversanne,Isabelle Soerjomataram,Ahmedin Jemal,Freddie Bray +6 more
TL;DR: The GLOBOCAN 2020 estimates of cancer incidence and mortality produced by the International Agency for Research on Cancer (IARC) as mentioned in this paper show that female breast cancer has surpassed lung cancer as the most commonly diagnosed cancer, with an estimated 2.3 million new cases (11.7%), followed by lung cancer, colorectal (11 4.4%), liver (8.3%), stomach (7.7%) and female breast (6.9%), and cervical cancer (5.6%) cancers.
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Cancer Statistics, 2021.
TL;DR: In the United States, the cancer death rate has dropped continuously from its peak in 1991 through 2018, for a total decline of 31%, because of reductions in smoking and improvements in early detection and treatment as mentioned in this paper.
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Death Receptor Regulation and Celecoxib-Induced Apoptosis in Human Lung Cancer Cells
TL;DR: Celecoxib appears to induce apoptosis in human NSCLC through the extrinsic death receptor pathway through the small interfering RNA (siRNA) technology.
Journal Article
Differential Effects of Synthetic Nuclear Retinoid Receptor-selective Retinoids on the Growth of Human Non-Small Cell Lung Carcinoma Cells
Shi-Yong Sun,Ping Yue,Marcia I. Dawson,Braham Shroot,Serge Michel,William W. Lamph,Richard A. Heyman,Min Teng,Roshantha A.S. Chandraratna,Koichi Shudo,Waun Ki Hong,Reuben Lotan +11 more
TL;DR: There appeared to be no simple correlation among the histological type of the NSCLC, the levels of nuclear receptors or CRABPs, and the response of the cells to the growth-inhibitory effects of retinoids, but results suggest that several synthetic retinoid do exhibit inhibitory activity against NSCLCs, and some of them may be useful clinically.
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MET inhibitors for targeted therapy of EGFR TKI-resistant lung cancer
TL;DR: In this paper, the authors proposed combinatorial therapy with osimertinib and a MET or even a MEK inhibitor for resistant NSCLC carrying MET amplification and/or protein hyperactivation.
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