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Induction of mitochondrial dysfunction as a strategy for targeting tumour cells in metabolically compromised microenvironments
The small molecule VLX600 is identified as a drug that is preferentially active against quiescent cells in colon cancer 3-D microtissues and displays tumour growth inhibition in vivo, suggesting that tumours in metabolically compromised microenvironments have a limited ability to respond to decreased mitochondrial function.
IL-15 activates mTOR and primes stress-activated gene expression leading to prolonged antitumor capacity of NK cells.
Findings highlight the importance of mTOR-regulated metabolic processes for immune cell functions and argue for implementation of IL-15 in adoptive NK-cell cancer therapy.
Three-Dimensional Cell Culture-Based Screening Identifies the Anthelmintic Drug Nitazoxanide as a Candidate for Treatment of Colorectal Cancer
It is reported that the FDA-approved anthelmintic drug nitazoxanide could be a potential candidate for advancement into cancer clinical trials and it is shown that all five compounds inhibit mitochondrial respiration, suggesting that cancer cells in low glucose concentrations depend on oxidative phosphorylation rather than solely glycolysis.
Irreversible inhibition of cytosolic thioredoxin reductase 1 as a mechanistic basis for anticancer therapy
- W. Stafford, Xiaoxiao Peng, Elias S. J. Arnér
- Biology, ChemistryScience Translational Medicine
- 14 February 2018
Targeting of the TXN pathway alone and selective inhibition of the cytosolic selenocysteine-containing enzyme TXN reductase 1 (TXNRD1) are evaluated to display the therapeutic anticancer potential of irreversibly targeting cytosol TXNRD 1 using small molecules and present potent and selective TXNRd1 inhibitors.
Repurposing of auranofin: Thioredoxin reductase remains a primary target of the drug.
Induction of tumor cell apoptosis by a proteasome deubiquitinase inhibitor is associated with oxidative stress.
- S. Brnjic, M. Mazurkiewicz, S. Linder
- Biology, ChemistryAntioxidants & redox signaling
- 24 November 2014
The data show that enhanced oxidative stress and ER stress are major determinants of the strong apoptotic response elicited by the 19S DUB inhibitor b-AP15.
Drug Development Targeting the Ubiquitin–Proteasome System (UPS) for the Treatment of Human Cancers
This review systematically categorizes all current reported small molecule inhibitors of the various essential components of the UPS, including ubiquitin-activating enzymes (E1s, E2s, and E3s), and discusses the immunoproteasome which is considered as a prospective therapeutic target of the next generation of proteasome inhibitors in cancer therapies.
Autophagy Is a Protective Mechanism for Human Melanoma Cells under Acidic Stress*
- M. Marino, P. Pellegrini, A. De Milito
- Biology, ChemistryThe Journal of Biological Chemistry
- 3 July 2012
Observations indicate that induction of autophagy may represent an adaptation mechanism for cancer cells exposed to an acidic environment, and strengthen the validity of therapeutic strategies targeting tumor pH regulation and Autophagy in progressive malignancies.
Estrogen Receptor β as a Therapeutic Target in Breast Cancer Stem Cells
- Ran Ma, G. Karthik, J. Hartman
- Biology, MedicineJournal of the National Cancer Institute
- 10 February 2017
ERβ is identified as a mediator of estrogen action in BSCs and a novel target for endocrine therapy.
The 19S Deubiquitinase Inhibitor b-AP15 Is Enriched in Cells and Elicits Rapid Commitment to Cell Death
It is concluded that the strong enrichment of b-AP15 in cells and a rapid commitment to apoptosis/cell death are factors that likely contribute to the strong antitumor activity of this compound.