PPARα agonist fenofibrate relieves acquired resistance to gefitinib in non-small cell lung cancer by promoting apoptosis via PPARα/AMPK/AKT/FoxO1 pathway

Wang, Meisa; Han, Qiu-shuang; Jia, Zhirong; Chen, Chuan-sheng; Qiao, Chun‐Feng; Liu, Qianqian; Zhang, Yameng; Wang, Kai-wei; Wang, Jie; Xiao, Kang; Ding, Xiaowen

doi:10.1038/s41401-021-00638-z

Cited by 22 publications

(16 citation statements)

References 33 publications

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“… 401 This induction was observed for ABCA1 / Abca1 mRNA 268 , 315 , 343 , 401 , 405 as well as ABCA1 protein levels, 268 , 337 , 343 , 395 , 405 , 409 and was functionally confirmed by increased cholesterol efflux. 268 , 315 A connection between the PPAR and LXR pathways has also been drawn, 268 , 326 , 327 , 337 , 400 highlighting the importance of both pathways for ABCA1 / Abca1 induction. Furthermore, fenofibrate had a positive impact on both the LXR-α and AMPK pathways 400 Certain PPAR agonists have been used as standard inducers of Abca1 , e.g.…”

Section: Part I: Status Quomentioning

confidence: 91%

“… 268 , 315 A connection between the PPAR and LXR pathways has also been drawn, 268 , 326 , 327 , 337 , 400 highlighting the importance of both pathways for ABCA1 / Abca1 induction. Furthermore, fenofibrate had a positive impact on both the LXR-α and AMPK pathways 400 Certain PPAR agonists have been used as standard inducers of Abca1 , e.g. , pioglitazone 407 and rosiglitazone.…”

Section: Part I: Status Quomentioning

confidence: 91%

“…Another well-known approach to induce ABCA1 involves the PPAR pathway ( Figure 3 ). 268 , 272 , 295 , 309 , 315 , 321 , 326 , 327 , 337 , 343 , 395 , 400 - 409 Certain PPAR/Ppar inducers and/or PPAR activators have been described above, as these modulators also have effects on the LXR pathway. 321 , 361 , 372 , 373 , 377 …”

Section: Part I: Status Quomentioning

confidence: 99%

“…Several drugs and drug-like PPAR agonists were revealed to induce ABCA1 / Abca1 mRNA and/or ABCA1 protein content, including the PPAR-α agonists fenofibrate, 326 , 400 , 404 pemafibrate (K-877), 405 Wy14643, 268 , 343 and RPR-5, 268 as well as the PPAR-γ agonists efatutazone, 337 pioglitazone, 272 , 309 , 326 , 395 , 407 pitavastatin, 343 prostaglandin J2 (PG-J2), 268 , 327 rosiglitazone ( Figure 2 ), 268 , 309 , 315 , 408 , 409 troglitazone, 268 and GW7845, 315 but also the broad-spectrum PPAR-α, PPAR-β, and PPAR-γ agonist bezafibrate 268 , 327 and the multitarget PPAR-α, PPAR-γ, and PPAR-δ agonist tetradecylthioacetic acid. 401 This induction was observed for ABCA1 / Abca1 mRNA 268 , 315 , 343 , 401 , 405 as well as ABCA1 protein levels, 268 , 337 , 343 , 395 , 405 , 409 and was functionally confirmed by increased cholesterol efflux.…”

Section: Part I: Status Quomentioning

confidence: 99%

“…Finally, the antineoplastic agent gefitinib reduced ABCA1 protein content in various non-small cell lung cancer cell lines. 400 …”

Section: Part I: Status Quomentioning

confidence: 99%

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Strategies to gain novel Alzheimer’s disease diagnostics and therapeutics using modulators of ABCA transporters

Pahnke

Bascuñana

Brackhan

et al. 2021

Free Neuropathology

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Adenosine-triphosphate-(ATP)-binding cassette (ABC) transport proteins are ubiquitously present membrane-bound efflux pumps that distribute endo- and xenobiotics across intra- and intercellular barriers. Discovered over 40 years ago, ABC transporters have been identified as key players in various human diseases, such as multidrug-resistant cancer and atherosclerosis, but also neurodegenerative diseases, such as Alzheimer’s disease (AD). Most prominent and well-studied are ABCB1, ABCC1, and ABCG2, not only due to their contribution to the multidrug resistance (MDR) phenotype in cancer, but also due to their contribution to AD. However, our understanding of other ABC transporters is limited, and most of the 49 human ABC transporters have been largely neglected as potential targets for novel small-molecule drugs. This is especially true for the ABCA subfamily, which contains several members known to play a role in AD initiation and progression. This review provides up-to-date information on the proposed functional background and pathological role of ABCA transporters in AD. We also provide an overview of small-molecules shown to interact with ABCA transporters as well as potential in silico , in vitro , and in vivo methodologies to gain novel templates for the development of innovative ABC transporter-targeting diagnostics and therapeutics.

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Section: Part I: Status Quomentioning

confidence: 91%

Section: Part I: Status Quomentioning

confidence: 91%

Section: Part I: Status Quomentioning

confidence: 99%

Section: Part I: Status Quomentioning

confidence: 99%

“…Finally, the antineoplastic agent gefitinib reduced ABCA1 protein content in various non-small cell lung cancer cell lines. 400 …”

Section: Part I: Status Quomentioning

confidence: 99%

See 3 more Smart Citations

Strategies to gain novel Alzheimer’s disease diagnostics and therapeutics using modulators of ABCA transporters

Pahnke

Bascuñana

Brackhan

et al. 2021

Free Neuropathology

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Preclinical evidence using synthetic compounds and natural products indicates that AMPK represents a potential pharmacological target for the therapy of pulmonary diseases

Yang,

Rubin,

et al. 2024

Medicinal Research Reviews

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Adenosine 5′‐monophosphate (AMP)‐activated protein kinase (AMPK) is a highly conserved eukaryotic enzyme discovered as a key regulator of cellular energy homeostasis, with anti‐inflammation, antioxidative stress, anticancer, and antifibrosis beneficial effects. AMPK is dysregulated in human pulmonary diseases such as acute lung injury, nonsmall cell lung cancer, pulmonary fibrosis, chronic obstructive pulmonary disease, and asthma. This review provides an overview of the beneficial role of natural, synthetic, and Chinese traditional medicines AMPK modulators in pulmonary diseases, and highlights the role of the AMPK signaling pathway in the lung, emphasizing the importance of finding lead compounds and drugs that can target and modulate AMPK to treat the lung diseases.

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Lipid-lowering drugs and cancer: an updated perspective

Alizadehasl,

Alavi,

Boudagh

et al. 2023

Pharmacol. Rep

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PPARα agonist fenofibrate relieves acquired resistance to gefitinib in non-small cell lung cancer by promoting apoptosis via PPARα/AMPK/AKT/FoxO1 pathway

Cited by 22 publications

References 33 publications

Strategies to gain novel Alzheimer’s disease diagnostics and therapeutics using modulators of ABCA transporters

Strategies to gain novel Alzheimer’s disease diagnostics and therapeutics using modulators of ABCA transporters

Preclinical evidence using synthetic compounds and natural products indicates that AMPK represents a potential pharmacological target for the therapy of pulmonary diseases

Lipid-lowering drugs and cancer: an updated perspective

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