Read by QxMD icon Read


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
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...
March 9, 2018: Expert Review of Anticancer Therapy
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
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
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
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
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
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
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
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
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
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
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
M Maekawa, A Watanabe, Y Iwayama, T Kimura, K Hamazaki, S Balan, H Ohba, Y Hisano, Y Nozaki, T Ohnishi, M Toyoshima, C Shimamoto, K Iwamoto, M Bundo, N Osumi, E Takahashi, A Takashima, T Yoshikawa
The risk of schizophrenia is increased in offspring whose mothers experience malnutrition during pregnancy. Polyunsaturated fatty acids (PUFAs) are dietary components that are crucial for the structural and functional integrity of neural cells, and PUFA deficiency has been shown to be a risk factor for schizophrenia. Here, we show that gestational and early postnatal dietary deprivation of two PUFAs-arachidonic acid (AA) and docosahexaenoic acid (DHA)-elicited schizophrenia-like phenotypes in mouse offspring at adulthood...
September 5, 2017: Translational Psychiatry
Julia J Scarisbrick
CD30-positive primary cutaneous T-cell lymphoma (CTCL) includes mycosis fungoides, anaplastic large-cell lymphoma and lymphomatoid papulosis type A. Brentuximab vedotin (BV) consists of an antibody targeting CD30 with a protease-cleavable linker to vedotin. CD30 binding allows internalization of BV inducing cell-cycle arrest and apoptosis. Response rates >75% with manageable adverse effects in refractory Hodgkin lymphoma and systemic anaplastic large-cell lymphoma led to accelerated approval for both. Phase II studies in CD30-expressing CTCL followed and showed similar efficacy, which was ratified in a Phase III trial of BV versus physician's choice (methotrexate or bexarotene) showing significant improved responses without increase in severe adverse effects although peripheral neuropathy is frequent...
August 14, 2017: Future Oncology
Yulia N Nosova, Ilia V Zenin, Varvara P Maximova, Ekaterina M Zhidkova, Kirill I Kirsanov, Ekaterina A Lesovaya, Anna A Lobas, Mikhail V Gorshkov, Olga N Kovaleva, Elena R Milaeva, Markus Galanski, Bernhard K Keppler, Alexey A Nazarov
We present the synthesis and cytotoxic potencies of new Pt(IV) complexes with bexarotene, an anticancer drug that induces cell differentiation and apoptosis via selective activation of retinoid X receptors. In these complexes bexarotene is positioned as an axial ligand. The complex of one bexarotene ligand attached to Pt(IV) oxaliplatin moiety was potent whereas its counterpart carrying two bexarotene ligands was inactive.
2017: Bioinorganic Chemistry and Applications
J P Nicolay, C Assaf
Adequate therapeutic management of cutaneous T-cell lymphoma (CTCL) requires the identification of the exact CTCL stage and entity within the current WHO classification. There is no curative therapy for CTCL yet, so that treatment currently aims at improving symptoms and quality of life as well as reducing relapse rates. The treatment has to be stage-adapted. Therapeutic options comprise skin-directed as well as systemic treatment. In early stages, phototherapy and local steroids are the first-line therapeutic options...
September 2017: Der Hautarzt; Zeitschrift Für Dermatologie, Venerologie, und Verwandte Gebiete
Osamu Shibahara, Masaki Watanabe, Shoya Yamada, Masaru Akehi, Takanori Sasaki, Akiya Akahoshi, Takahisa Hanada, Hiroyuki Hirano, Shunsuke Nakatani, Hiromi Nishioka, Yasuo Takeuchi, Hiroki Kakuta
The retinoid X receptor (RXR) partial agonist 1-[(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)amino]benzotriazole-5-carboxylic acid (1; CBt-PMN, Emax = 75%, EC50 = 143 nM) is a candidate for treatment of central nervous system (CNS) diseases such as Alzheimer's and Parkinson's diseases based on reports that RXR-full agonist 4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic acid (bexarotene) shows therapeutic effects on these disease in rodent models. Here, we synthesized carbon-11-labeled ([(11)C]1) as a tracer for positron emission tomography (PET) and used it in a PET imaging study to examine the brain uptake and biodistribution of 1...
August 24, 2017: Journal of Medicinal Chemistry
Daniel J Lewis, Simo Huang, Madeleine Duvic
Organ transplant recipients receiving immunosuppression have an increased risk of developing post-transplant lymphoproliferative diseases (PTLDs). Traditionally, PTLDs refer to Epstein-Barr virus (EBV)-induced B-cell lymphoma. However, post-transplant T-cell lymphoma may also occur and tends to have a poorer response to reduced immunosuppressive therapy. As such, additional therapy is often needed for post-transplant T-cell lymphoma, including post-transplant cutaneous T-cell lymphoma (PT-CTCL). We present only the third case of PT-CTCL occurring after liver transplantation...
September 2017: Dermatologic Therapy
Pham Dinh Quoc Huy, Nguyen Quoc Thai, Zuzana Bednarikova, Le Huu Phuc, Huynh Quang Linh, Zuzana Gazova, Mai Suan Li
In 2012, it was reported that anticancer drug bexarotene reduced amyloid plaque and improved mental functioning in a small sample of mice engineered to exhibit Alzheimer's like symptoms. It has been suggested that bexarotene stimulates expression of apolipoprotein E (ApoE) leading to intracellular clearance of amyloid beta (Aβ). However, the effect of bexarotene on clearance of plaques has not been seen in some mouse models. Two interesting questions include whether bexarotene can destroy Aβ fibrils via direct interaction with them and how this compound impacts the lag phase in the fibril growth process...
July 20, 2017: ACS Chemical Neuroscience
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"