The retinoid X receptor agonist bexarotene (Targretin) synergistically enhances the growth inhibitory activity of cytotoxic drugs in non-small cell lung cancer cells

Hermann, T; Yen, Wan-Ching; Tooker, Patricia; Fan, B.; Roegner, K.; Negro‐Vilar, A.; Lamph, William W.; Bissonnette, Reid P.

doi:10.1016/j.lungcan.2005.05.008

Cited by 33 publications

(14 citation statements)

References 28 publications

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“…Treatment with LGD1069 (bexarotene) alone at 10 μM produced only minimal growth inhibition (≤ 25%) of Calu3, EKVX, H358M, H441, HOP62, HOP92, and SKMES1 non-small cell lung cancer (NSCLC) cell lines, and 30–50% inhibition of A427, A549, and H322M NSCLC cell lines although all lines expressed RXRβ and only SK-MES-1 failed to express RXRα [51]. However, co-treatment of the cells with LGD1069 (bexarotene) at 1 μM was able to reduce the IC 50 values of pacitaxel by 32–54% and vinorelbine by 18–48%.…”

Section: Rxr Ligandsmentioning

confidence: 99%

The retinoid X receptors and their ligands

Dawson

Xia

2012

Biochimica et Biophysica Acta (BBA) - Molecular and Cell Biolog

331

325

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This chapter presents an overview of the current status of studies on the structural and molecular biology of the retinoid X receptor subtypes α, β, and γ (RXRs, NR2B1–3), their nuclear and cytoplasmic functions, post-transcriptional processing, and recently reported ligands. Points of interest are the different changes in the ligand-binding pocket induced by variously shaped agonists, the communication of the ligand–bound pocket with the coactivator binding surface and the heterodimerization interface, and recently identified ligands that are natural products, those that function as environmental toxins or drugs that had been originally designed to interact with other targets, as well as those that were deliberately designed as RXR-selective transcriptional agonists, synergists, or antagonists. Of these synthetic ligands, the general trend in design appears to be away from fully aromatic rigid structures to those containing partial elements of the flexible tetraene side chain of 9-cis-retinoic acid.

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Section: Rxr Ligandsmentioning

confidence: 99%

The retinoid X receptors and their ligands

Dawson

Xia

2012

Biochimica et Biophysica Acta (BBA) - Molecular and Cell Biolog

331

325

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“…The combination index (CI) was calculated to evaluate the combination effect of chemotherapy and photothermal therapy. [ 23 ] The value of CI represents different meanings, while < 1 indicates synergism, > 1 means antagonism, and = 1 indicates additive effects.…”

Section: Methodsmentioning

confidence: 99%

MRI‐Visualized, Dual‐Targeting, Combined Tumor Therapy Using Magnetic Graphene‐Based Mesoporous Silica

Wang

Huang

Liang

et al. 2013

Small

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Targeting peptide-modified magnetic graphene-based mesoporous silica (MGMSPI) are synthesized, characterized, and developed as a multifunctional theranostic platform. This system exhibits many merits, such as biocompatibility, high near-infrared photothermal heating, facile magnetic separation, large T2 relaxation rates (r2), and a high doxorubicin (DOX) loading capacity. In vitro and in vivo results demonstrate that DOX-loaded MGMSPI (MGMSPID) can integrate magnetic resonance imaging, dual-targeting recognition (magnetic targeting and receptor-mediated active targeting), and chemo-photothermal therapy into a single system for a visualized-synergistic therapy of glioma. In addition, it is observed that the MGMSPID system has heat-stimulated, pH-responsive, sustained release properties. All of these characteristics would provide a robust multifunctional theranostic platform for visualized glioma therapy.

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“…We further showed that the combination of bexarotene and cytotoxic agents produces synergistic growth inhibition as well as prevents and overcomes acquired drug resistance in several preclinical cancer models (17)(18)(19)(20)(21). The encouraging preclinical results with bexarotene, alone or in combination with various cytotoxic agents, led us to further examine its role in treatment of solid tumors.…”

Section: Introductionmentioning

confidence: 91%

Bexarotene (LGD1069, Targretin), a Selective Retinoid X Receptor Agonist, Prevents and Reverses Gemcitabine Resistance in NSCLC Cells by Modulating Gene Amplification

Tooker

Yen

et al. 2007

Cancer Research

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Acquired drug resistance is a major obstacle in cancer therapy. As for many other drugs, this is also the case for gemcitabine, a nucleoside analogue with activity against nonsmall cell lung cancer (NSCLC). Here, we evaluate the ability of bexarotene to modulate the acquisition and maintenance of gemcitabine resistance in Calu3 NSCLC models. In the prevention model, Calu3 cells treated repeatedly with gemcitabine alone gradually developed resistance. However, with inclusion of bexarotene, the cells remained chemosensitive.

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The retinoid X receptor agonist bexarotene (Targretin) synergistically enhances the growth inhibitory activity of cytotoxic drugs in non-small cell lung cancer cells

Cited by 33 publications

References 28 publications

The retinoid X receptors and their ligands

The retinoid X receptors and their ligands

MRI‐Visualized, Dual‐Targeting, Combined Tumor Therapy Using Magnetic Graphene‐Based Mesoporous Silica

Bexarotene (LGD1069, Targretin), a Selective Retinoid X Receptor Agonist, Prevents and Reverses Gemcitabine Resistance in NSCLC Cells by Modulating Gene Amplification

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