Literature DB >> 32576582

Lys05 - A Promising Autophagy Inhibitor in the Radiosensitization Battle: Phosphoproteomic Perspective.

Martin Ondrej1, Lucie Cechakova1, Ivo Fabrik2, Jana Klimentova2, Ales Tichy3.   

Abstract

BACKGROUND: Autophagy is a crucial factor contributing to radioresistance during radiotherapy. Although Lys05 has proven its ability to improve the results of radiotherapy through the inhibition of autophagy, molecular mechanisms of this inhibition remain elusive. We aimed to describe the molecular mechanisms involved in Lys05-induced inhibition of autophagy.
MATERIALS AND METHODS: Radioresistant human non-small cell lung carcinoma cells (H1299, p53-negative) and methods of quantitative phosphoproteomics were employed to define the molecular mechanisms involved in Lys05-induced inhibition of autophagy.
RESULTS: We confirmed that at an early stage after irradiation, autophagy was induced, whereas at a later stage after irradiation, it was inhibited. The early-stage induction of autophagy was characterized mainly by the activation of biosynthetic and metabolic processes through up- or down-regulation of the critical autophagic regulatory proteins Sequestosome-1 (SQSTM1) and proline-rich AKT1 substrate 1 (AKT1S1). The late-stage inhibition of autophagy was attributed mainly to down-regulation of Unc-51 like autophagy-activating kinase 1 (ULK1) through phosphorylation at Ser638.
CONCLUSION: This work contributes to emerging phosphoproteomic insights into autophagy-mediated global signaling in lung cancer cells, which might consequently facilitate the development of precision medicine therapeutics. Copyright
© 2020, International Institute of Anticancer Research (Dr. George J. Delinasios), All rights reserved.

Entities:  

Keywords:  Lys05; Phosphoproteomics; autophagy; inhibitor; lung cancer

Mesh:

Substances:

Year:  2020        PMID: 32576582      PMCID: PMC7367607          DOI: 10.21873/cgp.20196

Source DB:  PubMed          Journal:  Cancer Genomics Proteomics        ISSN: 1109-6535            Impact factor:   4.069


  35 in total

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4.  Rapid detergent removal from peptide samples with ethyl acetate for mass spectrometry analysis.

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Journal:  Curr Protoc Protein Sci       Date:  2010-02

5.  Phosphorylation of PRAS40 on Thr246 by PKB/AKT facilitates efficient phosphorylation of Ser183 by mTORC1.

Authors:  Emmani B M Nascimento; Marieke Snel; Bruno Guigas; Gerard C M van der Zon; Jan Kriek; J Antonie Maassen; Ingrid M Jazet; Michaela Diamant; D Margriet Ouwens
Journal:  Cell Signal       Date:  2010-02-06       Impact factor: 4.315

6.  Prevention of amino acid conversion in SILAC experiments with embryonic stem cells.

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7.  Autophagy inhibitor Lys05 has single-agent antitumor activity and reproduces the phenotype of a genetic autophagy deficiency.

Authors:  Quentin McAfee; Zhihui Zhang; Arabinda Samanta; Samuel M Levi; Xiao-Hong Ma; Shengfu Piao; John P Lynch; Takeshi Uehara; Antonia R Sepulveda; Lisa E Davis; Jeffrey D Winkler; Ravi K Amaravadi
Journal:  Proc Natl Acad Sci U S A       Date:  2012-05-07       Impact factor: 11.205

8.  Combining radiation with autophagy inhibition enhances suppression of tumor growth and angiogenesis in esophageal cancer.

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Journal:  Mol Med Rep       Date:  2015-04-16       Impact factor: 2.952

9.  Radiosensitization of human leukemic HL-60 cells by ATR kinase inhibitor (VE-821): phosphoproteomic analysis.

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10.  Autophagy inhibition enhances radiosensitivity of Eca‑109 cells via the mitochondrial apoptosis pathway.

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  1 in total

Review 1.  Inhibiting Cytoprotective Autophagy in Cancer Therapy: An Update on Pharmacological Small-Molecule Compounds.

Authors:  Lijuan Zhang; Yuxuan Zhu; Jiahui Zhang; Lan Zhang; Lu Chen
Journal:  Front Pharmacol       Date:  2022-08-11       Impact factor: 5.988

  1 in total

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