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Showing 25 to 36 of 75 entries
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Structure-based identification of a new IAP-targeting compound that induces cancer cell death inducing NF-κB pathway.

Computational and structural biotechnology journal

Cossu F, Camelliti S, Lecis D, Sorrentino L, Majorini MT, Milani M, Mastrangelo E.
PMID: 34938412
Comput Struct Biotechnol J. 2021 Nov 26;19:6366-6374. doi: 10.1016/j.csbj.2021.11.034. eCollection 2021.

Inhibitors of apoptosis proteins (IAPs) are validated onco-targets, as their overexpression correlates with cancer onset, progression, diffusion and chemoresistance. IAPs regulate cell death survival pathways, inflammation, and immunity. Targeting IAPs, by impairing their protein-protein interaction surfaces, can affect events...

Exploratory window-of-opportunity trial to investigate the tumor pharmacokinetics/pharmacodynamics of the IAP antagonist Debio 1143 in patients with head and neck cancer.

Clinical and translational science

Gomez-Roca C, Even C, Le Tourneau C, Basté N, Delord JP, Sarini J, Vergez S, Temam S, Hoffmann C, Rochaix P, Borcoman E, Gavillet B, Rouits E, Ménétrey A, Brichory F, Purcea D, Vuagniaux G, Zanna C.
PMID: 33742767
Clin Transl Sci. 2022 Jan;15(1):55-62. doi: 10.1111/cts.13002. Epub 2021 Nov 11.

Inhibitor of apoptosis proteins (IAPs) regulate apoptosis and modulate NF-κB signaling thereby driving expression of genes involved in immune/inflammatory responses. The orally available IAP antagonist Debio 1143 has potential to enhance tumor response to chemoradiotherapy and/or immunotherapy. Patients with...

Osthole induces lung cancer cell apoptosis through inhibition of inhibitor of apoptosis family proteins.

Oncology letters

Xu XM, Zhang ML, Zhang Y, Zhao L.
PMID: 27895730
Oncol Lett. 2016 Nov;12(5):3779-3784. doi: 10.3892/ol.2016.5170. Epub 2016 Sep 22.

In the present study, we investigated the effects and mechanisms of Osthole on the apoptosis of non-small cell lung cancer (NSCLC) cells and its synergistic effect with Embelin. Our results revealed that treatment with both Osthole and Embelin inhibited...

Overlap of NatA and IAP substrates implicates N-terminal acetylation in protein stabilization.

Science advances

Mueller F, Friese A, Pathe C, da Silva RC, Rodriguez KB, Musacchio A, Bange T.
PMID: 33523899
Sci Adv. 2021 Jan 15;7(3). doi: 10.1126/sciadv.abc8590. Print 2021 Jan.

SMAC/DIABLO and HTRA2 are mitochondrial proteins whose amino-terminal sequences, known as inhibitor of apoptosis binding motifs (IBMs), bind and activate ubiquitin ligases known as inhibitor of apoptosis proteins (IAPs), unleashing a cell's apoptotic potential. IBMs comprise a four-residue, loose...

Nucleolin-aptamer therapy in retinoblastoma: molecular changes and mass spectrometry-based imaging.

Molecular therapy. Nucleic acids

Subramanian N, Srimany A, Kanwar JR, Kanwar RK, Akilandeswari B, Rishi P, Khetan V, Vasudevan M, Pradeep T, Krishnakumar S.
PMID: 27574784
Mol Ther Nucleic Acids. 2016 Aug 30;5(8):e358. doi: 10.1038/mtna.2016.70.

Retinoblastoma (RB) is an intraocular childhood tumor which, if left untreated, leads to blindness and mortality. Nucleolin (NCL) protein which is differentially expressed on the tumor cell surface, binds ligands and regulates carcinogenesis and angiogenesis. We found that NCL...

Exploratory window-of-opportunity trial to investigate the tumor pharmacokinetics/pharmacodynamics of the IAP antagonist Debio 1143 in patients with head and neck cancer.

Clinical and translational science

Gomez-Roca C, Even C, Le Tourneau C, Basté N, Delord JP, Sarini J, Vergez S, Temam S, Hoffmann C, Rochaix P, Borcoman E, Gavillet B, Rouits E, Ménétrey A, Brichory F, Purcea D, Vuagniaux G, Zanna C.
PMID: 33742767
Clin Transl Sci. 2021 Mar 20; doi: 10.1111/cts.13002. Epub 2021 Mar 20.

Inhibitor of apoptosis proteins (IAPs) regulate apoptosis and modulate NF-κB signaling thereby driving expression of genes involved in immune/inflammatory responses. The orally available IAP antagonist Debio 1143 has potential to enhance tumor response to chemoradiotherapy and/or immunotherapy. Patients with...

Sulforaphane Protects Against Ethanol-Induced Apoptosis in Human Neural Crest Cells Through Diminishing Ethanol-Induced Hypermethylation at the Promoters of the Genes Encoding the Inhibitor of Apoptosis Proteins.

Frontiers in cell and developmental biology

Li Y, Fan H, Yuan F, Lu L, Liu J, Feng W, Zhang HG, Chen SY.
PMID: 33634123
Front Cell Dev Biol. 2021 Feb 09;9:622152. doi: 10.3389/fcell.2021.622152. eCollection 2021.

The neural crest cell (NCC) is a multipotent progenitor cell population that is sensitive to ethanol and is implicated in the Fetal Alcohol Spectrum Disorders (FASD). Studies have shown that sulforaphane (SFN) can prevent ethanol-induced apoptosis in NCCs. This...

Role of RIPK1 in SMAC mimetics-induced apoptosis in primary human HIV-infected macrophages.

Scientific reports

Caballero RE, Dong SXM, Gajanayaka N, Ali H, Cassol E, Cameron WD, Korneluk R, Tremblay MJ, Angel JB, Kumar A.
PMID: 34824340
Sci Rep. 2021 Nov 25;11(1):22901. doi: 10.1038/s41598-021-02146-w.

Macrophages serve as viral reservoirs due to their resistance to apoptosis and HIV-cytopathic effects. We have previously shown that inhibitor of apoptosis proteins (IAPs) confer resistance to HIV-Vpr-induced apoptosis in normal macrophages. Herein, we show that second mitochondrial activator...

Anti-apoptotic signaling as a cytoprotective mechanism in mammalian hibernation.

PeerJ

Rouble AN, Hefler J, Mamady H, Storey KB, Tessier SN.
PMID: 23638364
PeerJ. 2013 Feb 12;1:e29. doi: 10.7717/peerj.29. Print 2013.

In the context of normal cell turnover, apoptosis is a natural phenomenon involved in making essential life and death decisions. Apoptotic pathways balance signals which promote cell death (pro-apoptotic pathways) or counteract these signals (anti-apoptotic pathways). We proposed that...

Up regulation of Bax and down regulation of Bcl2 during 3-NC mediated apoptosis in human cancer cells.

Cancer cell international

Naseri MH, Mahdavi M, Davoodi J, Tackallou SH, Goudarzvand M, Neishabouri SH.
PMID: 26074734
Cancer Cell Int. 2015 May 28;15:55. doi: 10.1186/s12935-015-0204-2. eCollection 2015.

BACKGROUND: Recently, we have reported the induction of apoptosis by 2-amino-4-(3-nitrophenyl)-3-cyano-7-(dimethylamino)-4H-chromene (3-NC) in HepG2, T47D and HCT116 cells with low nano molar IC50 values. In this study, anti-proliferative effects of modified 4-aryle-4H-chromenes derivatives; 2-amino-4-(3-bromophenyl)-3-cyano-7-(dimethylamino)-4H-chromene (3-BC), 2-amino-4-(3-trifluoromethylphenyl)-3-cyano-7-(dimethylamino)-4H-chromene (3-TFC) and 2-amino-4-(4,5-methylenedioxyphenyl)-3-cyano-7-(dimethylamino)-4H-chromene...

Selective IAP inhibition results in sensitization of unstimulated but not CD40-stimulated chronic lymphocytic leukaemia cells to TRAIL-induced apoptosis.

Pharmacology research & perspectives

Zhuang J, Laing N, Oates M, Lin K, Johnson G, Pettitt AR.
PMID: 25505620
Pharmacol Res Perspect. 2014 Dec;2(6):e00081. doi: 10.1002/prp2.81. Epub 2014 Sep 01.

Despite recent advances in therapy, chronic lymphocytic leukaemia (CLL) remains incurable and new treatment strategies are therefore urgently required. Inhibitor of apoptosis proteins (IAPs) are over-expressed in CLL, suggesting both a role in disease pathogenesis and the potential for...

Debio 1143, an antagonist of multiple inhibitor-of-apoptosis proteins, activates apoptosis and enhances radiosensitization of non-small cell lung cancer cells in vitro.

American journal of cancer research

Liu N, Tao Z, Blanc JM, Zaorsky NG, Sun Y, Vuagniaux G, Dicker AP, Lu B.
PMID: 25520882
Am J Cancer Res. 2014 Nov 19;4(6):943-51. eCollection 2014.

Inhibitors of apoptosis (IAPs) limit the effectiveness of radiation in non-small cell lung cancer (NSCLC). Debio 1143 (D1143) is an antagonist of IAPs. The purpose of this study was to investigate the potential of D1143 as a radiosensitizer in...

Showing 25 to 36 of 75 entries