Výsledky vyhledávání - "Francisco Lopez-Tapia"

Akademický článek

Natural product preferentially targets redox and metabolic adaptations and aberrantly active STAT3 to inhibit breast tumor growth in vivo

Autor: Yinsong Zhu, Peibin Yue, Cody F. Dickinson, Justin K. Yang, Kyrstin Datanagan, Ning Zhai, Yi Zhang, Gabriella Miklossy, Francisco Lopez-Tapia, Marcus A. Tius, James Turkson

Publikováno v: Cell Death and Disease, Vol 13, Iss 12, Pp 1-14 (2022)

Abstract Dysregulated gene expression programs and redox and metabolic adaptations allow cancer cells to survive under high oxidative burden. These mechanisms also represent therapeutic vulnerabilities. Using triple-negative breast cancer (TNBC) as a

Externí odkaz: https://doaj.org/article/d34229ea9bfc4181a22308db8241c982

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Data from Hydroxamic Acid and Benzoic Acid–Based STAT3 Inhibitors Suppress Human Glioma and Breast Cancer Phenotypes In Vitro and In Vivo

Autor: James Turkson, Marcus A. Tius, Yuan Chen, Tyvette Hilliard, Chih-Hong Chen, Yifei Li, David Paladino, Francisco Lopez-Tapia, Peibin Yue

STAT3 offers an attractive target for cancer therapy, but small-molecule inhibitors with appealing pharmacologic properties have been elusive. Here, we report hydroxamic acid–based and benzoic acid–based inhibitors (SH5-07 and SH4-54, respectivel

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2685919e413c2073f3397cc0c16dd175
https://doi.org/10.1158/0008-5472.c.6507540

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Supplementary Figures S1-8 from Hydroxamic Acid and Benzoic Acid–Based STAT3 Inhibitors Suppress Human Glioma and Breast Cancer Phenotypes In Vitro and In Vivo

Autor: James Turkson, Marcus A. Tius, Yuan Chen, Tyvette Hilliard, Chih-Hong Chen, Yifei Li, David Paladino, Francisco Lopez-Tapia, Peibin Yue

Supplementary Figures S1-8. Fig. S1: EMSA analysis of Stat3 DNA-binding activity in vitro showing the effect of BP-1-102. Fig. S2: Effects of SH5-07, SH4-54 or BP-1-102 on Stat3 tyrosine and serine phosphorylation in tumor cells and on Stat3 DNA-bind

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0aad91b9f2cfc352b40b2cfe9ebd0cff
https://doi.org/10.1158/0008-5472.22408458.v1

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Abstract 5476: Novel azetidine-based STAT3 inhibitors induce misfolded protein response, endoplasmic reticulum stress and mitophagy, and inhibit breast tumor growth in vivo

Autor: Peibin Yue, Francisco Lopez-Tapia, Yinsong Zhu, Nagendra Verma, Felix Alonso-Valenteen, Simoun Mikhael, Lali Medina-Kauwe, Marcus Tius, James Turkson

Publikováno v: Cancer Research. 82:5476-5476

Anticancer drugs that directly target Signal Transducer and Activator of Transcription (Stat)3 have remained elusive. We present azetidine-based small molecules as a new class of potent Stat3 inhibitors. Compounds H172 and H182 have potency (IC50) of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::5867b7266b132fa46b6aa42f4db0d407
https://doi.org/10.1158/1538-7445.am2022-5476

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Abstract 5482: Natural product inhibitor of Stat3, G6PD, and TrxR1 functions induces an early oxidative stress and pyroptosis, and a late-stage DNA damage and cell cycle arrest to block tumor growth in human breast cancer models

Autor: Yinsong Zhu, Cody F. Dickinson, Justin Yang, Kyrstin Datanagan, Ning Zhai, Peibin Yue, Francisco Lopez-Tapia, Marcus A. Tius, James Turkson

Publikováno v: Cancer Research. 82:5482-5482

Bioactive natural products have led to new drugs or been the inspiration for developing new treatments. Signal transducer and activator of transcription (STAT)3 is a an oncogene that has been implicated in many human cancers. We report that the hirsu

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::ed993d5083d3fe1d4a6943d68393795f
https://doi.org/10.1158/1538-7445.am2022-5482

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Abstract 4792: Azetidine functionalized small-molecules potently inhibit STAT3 signaling and block tumor growth in human breast cancer xenografts

Autor: James Turkson, Christine Brotherton-Pleiss, Marcus A. Tius, Peibin Yue, Fu Wenzhen, Francisco Lopez-Tapia

Publikováno v: Cancer Research. 79:4792-4792

The development of inhibitors of Signal transducer and activator of transcription (STAT) 3 for clinical application has faced significant challenges and to date there are no suitable STAT3 small molecule inhibitors in the clinic. We report a novel cl

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::d0bdfc264cd8c2ed9f6e21d9251361d6
https://doi.org/10.1158/1538-7445.am2019-4792

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Abstract B137: Novel potent salicylic, benzoic, and benzohydroxamic acid-based small-molecule STAT3 inhibitors induce antitumor effects in breast cancer xenografts

Autor: Francisco Lopez-Tapia, Marcus A. Tius, Christine Brotherton-Pleiss, Peibin Yue, James Turkson

Publikováno v: Molecular Cancer Therapeutics. 17:B137-B137

We investigated the molecular determinants for the activity of the previously reported salicylic BP-1-102 (IC50 6.8 ± 2.5 μM), benzoic SH4-54 (IC50 4.4 ± 0.3 μM), and benzohydroxamic acid SH5-07 (IC50 3.9 ± 0.6 μM) small-molecule STAT3 inhibito

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::626e9fa9cbcb2e34dcd9bcbb9fc666de
https://doi.org/10.1158/1535-7163.targ-17-b137

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Abstract LB-058: Linker variation and structure-activity relationship analyses of salicylic, benzoic and hydroxamic acid-based small molecule Stat3 inhibitors

Autor: Christine Brotherton-Pleiss, Francisco Lopez-Tapia, James Turkson, Marcus A. Tius, Peibin Yue

Publikováno v: Cancer Research. 76:LB-058

Benzoic acid, salicylic acid and hydroxamic acid-based small molecules have been reported that inhibit Stat3 activation. However, the structural basis for their Stat3-inhibitory activities are not clearly defined. To investigate the molecular determi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::676f7d22d7afc1deb2197ef3f413bd82
https://doi.org/10.1158/1538-7445.am2016-lb-058

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