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Bexarotene

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https://www.readbyqxmd.com/read/29762675/rxr-ligands-modulate-thyroid-hormone-signaling-competence-in-young-xenopus-laevis-tadpoles
#1
Brenda J Mengeling, Michael L Goodson, J David Furlow
Appropriate thyroid hormone (TH) signaling through thyroid hormone receptors (TRs) is essential for vertebrate development. Amphibian metamorphosis is initiated and sustained through the action of TH on TRs which are conserved across vertebrates. TRs heterodimerize with retinoid-X receptors (RXRs) on thyroid hormone-response elements (TREs) in the genome, yet in most cell line and adult animal studies, RXR ligands do not affect expression of TR target genes. We used a quantitative, precocious metamorphosis assay to interrogate the effects of the RXR agonist bexarotene (Bex) and the RXR antagonist UVI 3003 (UVI) on T3-induced resorption phenotypes in Xenopus laevis tadpoles one-week post-fertilization...
May 11, 2018: Endocrinology
https://www.readbyqxmd.com/read/29717863/binding-of-bexarotene-to-the-amyloid-precursor-protein-transmembrane-domain-in-liposomes-alters-its-%C3%AE-helical-conformation-but-inhibits-%C3%AE-secretase-non-selectively
#2
Frits Kamp, Holger A Scheidt, Edith Winkler, Gabriele Basset, Hannes Heinel, James M Hutchison, Loren M LaPointe, Charles R Sanders, Harald Steiner, Daniel Huster
Bexarotene is a pleiotropic molecule that has been proposed as an amyloid-β (Aβ)-lowering drug for the treatment of Alzheimer´s disease (AD). It acts by upregulation of an apolipoprotein E (apoE)-mediated Aβ clearance mechanism. However, whether or not bexarotene induces removal of Aβ plaques in mouse models of AD has been controversial. Here, we show by NMR and CD spectroscopy that bexarotene directly interacts with and stabilizes the transmembrane domain α-helix of the amyloid precursor protein (APP) in a region where cholesterol binds...
May 2, 2018: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29704526/a-novel-gene-expression-analytics-based-approach-to-structure-aided-design-of-rexinoids-for-development-as-next-generation-cancer-therapeutics
#3
Bentley J Hanish, Jennifer F Hackney Price, Ichiro Kaneko, Ning Ma, Arjan van der Vaart, Carl E Wagner, Peter W Jurutka, Pamela A Marshall
Rexinoids are powerful ligands that bind to retinoid-X-receptors (RXRs) and show great promise as therapeutics for a wide range of diseases, including cancer. However, only one rexinoid, bexarotene (Targretin TM) has been successfully transitioned from the bench to the clinic and used to treat cutaneous T-cell lymphoma (CTCL). Our goal is to develop novel potent rexinoids with a less untoward side effect profile than bexarotene. To this end, we have synthesized a wide array of rexinoids with EC50 values and biological activity similar to bexarotene...
April 25, 2018: Steroids
https://www.readbyqxmd.com/read/29688151/bexarotene-attenuates-early-brain-injury-via-inhibiting-micoglia-activation-through-ppar%C3%AE-after-experimental-subarachnoid-hemorrhage
#4
Li Tu, Xiu-Lin Yang, Qian Zhang, Qian Wang, Tian Tian, Dan Liu, Xiang Qu, Jin-Yong Tian
Objectives Early brain injury (EBI) is considered to be one of the main causes of poor outcome in subarachnoid hemorrhage (SAH) patients. Bexarotene is an agonist of retinoid X receptor and plays a protective role in central nervous system diseases. However, the exact role of bexarotene in SAH has not been reported. Therefore, the present study was to determine whether bexarotene administration attenuate EBI after SAH in mice and to explore the underlying mechanism. Methods SAH was induced in C57BL/6 mice by endovascular perforation...
April 24, 2018: Neurological Research
https://www.readbyqxmd.com/read/29681823/successful-treatment-of-advanced-primary-cutaneous-peripheral-t-cell-lymphoma-with-oral-bexarotene-monotherapy
#5
Yota Sato, Taku Fujimura, Yumi Kambayashi, Akira Hashimoto, Setsuya Aiba
Bexarotene is a third-generation retinoid X receptor-selective retinoid that is widely used for the early treatment of advanced-stage cutaneous T-cell lymphomas. In this report, we describe a case of successful treatment of advanced primary cutaneous peripheral T-cell lymphoma not otherwise specified (PTCL-NOS) with oral bexarotene monotherapy. After the administration of oral bexarotene at a dose of 300 mg/m2 /day, all skin lesions and lymph nodes regressed, and complete remission was achieved for 1 year. Our case suggested that bexarotene monotherapy could be one of the possible therapies for the treatment of primary cutaneous PTCL-NOS...
January 2018: Case Reports in Oncology
https://www.readbyqxmd.com/read/29642873/bexarotene-inhibits-the-viability-of-non-small-cell-lung-cancer-cells-via-slc10a2-ppar%C3%AE-pten-mtor-signaling-pathway
#6
Xinghao Ai, Feng Mao, Shengping Shen, Yang Shentu, Jiejun Wang, Shun Lu
BACKGROUND: Thirty to 40 % of non-small cell lung cancer (NSCLC) patients developed higher hypertriglyceridemia in the process of treatment with bexarotene. And bioinformatics studies discovered that the expression of slc10a2 was increased in high-grade hypertriglyceridemia patients. So, we will explore the mechanism which may involve in this process. METHODS: We constructed slc10a2 overexpressed A549 cells and H1299 cells as cell models, normal A549 cells and H1299 cells as control...
April 11, 2018: BMC Cancer
https://www.readbyqxmd.com/read/29599065/the-retinoid-x-receptor-agonist-9-cis-uab30-inhibits-cutaneous-t-cell-lymphoma-proliferation-through-the-skp2-p27kip1-axis
#7
Chu-Fang Chou, Yu-Hua Hsieh, Clinton J Grubbs, Venkatram R Atigadda, James A Mobley, Reinhard Dummer, Donald D Muccio, Isao Eto, Craig A Elmets, W Timothy Garvey, Pi-Ling Chang
BACKGROUND: Bexarotene (Targretin® ) is currently the only FDA approved retinoid X receptor (RXR) -selective agonist for the treatment of cutaneous T-cell lymphomas (CTCLs). The main side effects of bexarotene are hypothyroidism and elevation of serum triglycerides (TGs). The novel RXR ligand, 9-cis UAB30 (UAB30) does not elevate serum TGs or induce hypothyroidism in normal subjects. OBJECTIVES: To assess preclinical efficacy and mechanism of action of UAB30 in the treatment of CTCLs and compare its action with bexarotene...
March 15, 2018: Journal of Dermatological Science
https://www.readbyqxmd.com/read/29562115/development-of-new-bexarotene-loaded-mesoporous-silica-systems-for-topical-pharmaceutical-formulations
#8
Aurelia Vasile, Maria Ignat, Mirela Fernanda Zaltariov, Liviu Sacarescu, Iulian Stoleriu, Dan Draganescu, Mihai Dumitras, Lacramioara Ochiuz
The present study reports the first time use of MCM-41 mesoporous silica as highly efficient carrier for bexarotene - an antineoplastic agent specific for cutaneous T-cell lymphoma treatment. Bexarotene is highly toxic and poor-water soluble, having low bioavailability in the conventional pharmaceutical forms. Comparative uptake of bexarotene on amino-functionalized silica host at various functionalization degrees is discussed in details taking into account all structural features, of matrix as well as properties of the drug molecules...
March 2018: Acta Chimica Slovenica
https://www.readbyqxmd.com/read/29521139/emerging-roles-of-bexarotene-in-the-prevention-treatment-and-anti-drug-resistance-of-cancers
#9
Danyang Shen, Xiaoming Yu, Yan Wu, Yuanlei Chen, Gonghui Li, Feng Cheng, Liqun Xia
Retinoic acid X receptors play key roles in tumor cell proliferation, differentiation, apoptosis and angiogenesis via transcriptional regulation. Bexarotene is a specific RXRs agonist which has been granted by FDA approval for the clinical treatment of cutaneous T cell lymphoma (CTCL). Its cancer prevention and treatment potentials in various tumors have been under investigation over the past decade. Areas covered: This review summarizes the efficacy and underlying mechanisms of bexarotene for the treatment of multiple cancers based on the launched clinical trials as well as the basic studies...
May 2018: Expert Review of Anticancer Therapy
https://www.readbyqxmd.com/read/29448961/nuclear-receptor-agonist-driven-modification-of-inflammation-and-amyloid-pathology-enhances-and-sustains-cognitive-improvements-in-a-mouse-model-of-alzheimer-s-disease
#10
Brad T Casali, Erin G Reed-Geaghan, Gary E Landreth
BACKGROUND: Alzheimer's disease (AD) is a highly prevalent neurodegenerative disorder characterized by pathological hallmarks of beta-amyloid plaque deposits, tau pathology, inflammation, and cognitive decline. Treatment remains a clinical obstacle due to lack of effective therapeutics. Agonists targeting nuclear receptors, such as bexarotene, reversed cognitive deficits regardless of treatment duration and age in murine models of AD. While bexarotene demonstrated marked efficacy in decreasing plaque levels following short-term treatment, prolonged treatment did not modulate plaque burden...
February 15, 2018: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/29287960/discovering-alkylamide-derivatives-of-bexarotene-as-new-therapeutic-agents-against-triple-negative-breast-cancer
#11
Luxi Chen, Chao Long, Jennifer Nguyen, Dhiraj Kumar, Jiyong Lee
Triple-negative breast cancer (TNBC) has been reported to be correlated with high expression of proliferation markers as well as constitutive activation of metastasis-relevant signaling pathways. For many years, breast cancer researchers have been investigating specific and effective methods to treat or to control the development of TNBC, but promising therapeutic options remain elusive. In this study, we have demonstrated that alkylamide derivatives of bexarotene DK-1-150 and DK-1-166 induce apoptotic cell death in TNBC cell lines without causing cytotoxicity in the normal mammary epithelial cell line...
December 16, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29282975/correction-to-bexarotene-does-not-clear-amyloid-beta-plaques-but-delays-fibril-growth-molecular-mechanisms
#12
Pham Dinh Quoc Huy, Nguyen Quoc Thai, Zuzana Bednarikova, Le Huu Phuc, Huynh Quang Linh, Zuzana Gazova, Mai Suan Li
No abstract text is available yet for this article.
December 28, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29212711/ppar%C3%AE-activation-by-bexarotene-promotes-neuroprotection-by-restoring-bioenergetic-and-quality-control-homeostasis
#13
Audrey S Dickey, Dafne N Sanchez, Martin Arreola, Kunal R Sampat, Weiwei Fan, Nicolas Arbez, Sergey Akimov, Michael J Van Kanegan, Kohta Ohnishi, Stephen K Gilmore-Hall, April L Flores, Janice M Nguyen, Nicole Lomas, Cynthia L Hsu, Donald C Lo, Christopher A Ross, Eliezer Masliah, Ronald M Evans, Albert R La Spada
Neurons must maintain protein and mitochondrial quality control for optimal function, an energetically expensive process. The peroxisome proliferator-activated receptors (PPARs) are ligand-activated transcription factors that promote mitochondrial biogenesis and oxidative metabolism. We recently determined that transcriptional dysregulation of PPARδ contributes to Huntington's disease (HD), a progressive neurodegenerative disorder resulting from a CAG-polyglutamine repeat expansion in the huntingtin gene. We documented that the PPARδ agonist KD3010 is an effective therapy for HD in a mouse model...
December 6, 2017: Science Translational Medicine
https://www.readbyqxmd.com/read/29191068/an-exploratory-cost-effectiveness-analysis-of-systemic-treatments-for-cutaneous-t-cell-lymphoma
#14
Larisa Geskin, Daniel C Malone
PURPOSE: To conduct an exploratory cost-effectiveness analysis of systemic treatment options for more advanced cutaneous T-cell lymphoma (CTCL). METHODS: A cost-effectiveness model compared systemic bexarotene, denileukin diftitox, interferon-α, methotrexate, pralatrexate, romidepsin, vorinostat, and extracorporeal photopheresis (ECP) treatment of CTCL. Treatment effectiveness data were extracted from published studies and/or US product labeling. Overall response, the primary effectiveness measure, was defined as the proportion of patients achieving complete or partial response...
December 18, 2017: Journal of Dermatological Treatment
https://www.readbyqxmd.com/read/29188497/bexarotene-a-selective-rxr%C3%AE-agonist-reverses-hypotension-associated-with-inflammation-and-tissue-injury-in-a-rat-model-of-septic-shock
#15
Bahar Tunctan, Sefika P Kucukkavruk, Meryem Temiz-Resitoglu, Demet S Guden, Ayse N Sari, Seyhan Sahan-Firat
Peroxisome proliferator-activated receptors (PPARs) are nuclear receptors that can activate or inhibit the expression of many target genes by forming a heterodimer complex with the retinoid X receptor (RXR). The aim of this study was to investigate effects of bexarotene, a selective RXRα agonist, on the changes in renal, cardiac, hepatic, and pulmonary expression/activity of inducible nitric oxide synthase (iNOS) and cytochrome P450 (CYP) 4F6 in relation to PPARα/β/γ-RXRα heterodimer formation in a rat model of septic shock...
February 2018: Inflammation
https://www.readbyqxmd.com/read/29127736/liver-x-receptor-activation-inhibits-sglt2-mediated-glucose-transport-in-human-renal-proximal-tubular-cells
#16
Pattira Chonlaket, Teerasak Wongwan, Sunhapas Soodvilai
What is the central question of this study? The liver X receptor (LXR) has been reported to regulate several membrane transporters. It is imperative to investigate whether LXR activation regulates SGLT2-mediated glucose transport in human renal proximal tubular cells. What is the main finding and its importance? Liver X receptor activation inhibits SGLT2 transport function in normal and high-glucose conditions via reduction of SGLT2 protein expression. Liver X receptors (LXRs) are members of a nuclear receptor family consisting of two isoforms, LXRα and LXRβ...
February 1, 2018: Experimental Physiology
https://www.readbyqxmd.com/read/29102679/cutaneous-t-cell-lymphomas-focusing-on-novel-agents-in-relapsed-and-refractory-disease
#17
REVIEW
Lisa Argnani, Alessandro Broccoli, Pier Luigi Zinzani
Patients with relapsed or refractory cutaneous T-cell lymphoma (CTCL) display a dismal prognosis and their therapy represents an unmet medical need, as the best treatment strategy is yet to be determined. Exciting data on novel targeted agents are now emerging from recently concluded and ongoing clinical trials in patients with relapsed and refractory CTCL. Three FDA approved compounds are used as single agents including the oral retinoid bexarotene and histone deacetylase inhibitors romidepsin and vorinostat...
December 2017: Cancer Treatment Reviews
https://www.readbyqxmd.com/read/29044016/drug-induced-hypothyroidism
#18
Leonardo F L Rizzo, Daniela L Mana, Héctor A Serra
The thyroid axis is particularly prone to interactions with a wide variety of drugs, whose list increases year by year. Hypothyroidism is the most frequent consequence of drug-induced thyroid dysfunction. The main mechanisms involved in the development of primary hypothyroidism are: inhibition of the synthesis and/or release of thyroid hormones, immune mechanisms related to the use of interferon and other cytokines, and the induction of thyroiditis associated with the use of tyrosine kinase inhibitors and drugs blocking the receptors for vascular endothelial growth factor...
2017: Medicina
https://www.readbyqxmd.com/read/28981706/insights-into-interplay-between-rexinoid-signaling-and-myogenic-regulatory-factor-associated-chromatin-state-in-myogenic-differentiation
#19
Munerah Hamed, Saadia Khilji, Katherine Dixon, Alexandre Blais, Ilya Ioshikhes, Jihong Chen, Qiao Li
While skeletal myogenesis is tightly coordinated by myogenic regulatory factors including MyoD and myogenin, chromatin modifications have emerged as vital mechanisms of myogenic regulation. We have previously established that bexarotene, a clinically approved agonist of retinoid X receptor (RXR), promotes the specification and differentiation of skeletal muscle lineage. Here, we examine the genome-wide impact of rexinoids on myogenic differentiation through integral RNA-seq and ChIP-seq analyses. We found that bexarotene promotes myoblast differentiation through the coordination of exit from the cell cycle and the activation of muscle-related genes...
November 2, 2017: Nucleic Acids Research
https://www.readbyqxmd.com/read/28961843/global-patterns-of-care-in-advanced-stage-mycosis-fungoides-sezary-syndrome-a-multicenter-retrospective-follow-up-study-from-the-cutaneous-lymphoma-international-consortium
#20
P Quaglino, M Maule, H M Prince, P Porcu, S Horwitz, M Duvic, R Talpur, M Vermeer, M Bagot, J Guitart, E Papadavid, J A Sanches, E Hodak, M Sugaya, E Berti, P Ortiz-Romero, N Pimpinelli, O Servitje, A Pileri, P L Zinzani, T Estrach, R Knobler, R Stadler, M T Fierro, S Alberti Violetti, I Amitay-Laish, C Antoniou, C Astrua, S Chaganti, F Child, A Combalia, S Fabbro, P Fava, V Grandi, C Jonak, E Martinez-Escala, M Kheterpal, E J Kim, C McCormack, T Miyagaki, D Miyashiro, S Morris, C Muniesa, V Nikolaou, G Ognibene, F Onida, S Osella-Abate, S Porkert, C Postigo-Llorente, C Ram-Wolff, S Ribero, K Rogers, M Sanlorenzo, R Stranzenbach, N Spaccarelli, A Stevens, D Zugna, A H Rook, L J Geskin, R Willemze, S Whittaker, R Hoppe, J Scarisbrick, Y Kim
Background: Advanced-stage mycosis fungoides (MF)/Sézary syndrome (SS) patients are weighted by an unfavorable prognosis and share an unmet clinical need of effective treatments. International guidelines are available detailing treatment options for the different stages but without recommending treatments in any particular order due to lack of comparative trials. The aims of this second CLIC study were to retrospectively analyze the pattern of care worldwide for advanced-stage MF/SS patients, the distribution of treatments according to geographical areas (USA versus non-USA), and whether the heterogeneity of approaches has potential impact on survival...
October 1, 2017: Annals of Oncology: Official Journal of the European Society for Medical Oncology
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