Результаты поиска

Adapalene suppressed the proliferation of melanoma cells by S-phase arrest and subsequent apoptosis via induction of DNA damage.

Malignant melanoma was the leading cause of mortality among the skin-associated cancer owing to its highly metastatic feature, increasing incidence and drug resistance requirement. Retinoids played important roles in the treatment of cancer via the activation of retinoid acid receptor (RAR) or retinoid X receptor (RXR). Our present study showed that the third-generation retinoid adapalene exhibited strong inhibitory effects on the proliferation of melanoma cells than other retinoids, such as all-trans-retinoic acid (ATRA), isotretinoin, acitretin and bexarotene, and adapalene exerted significa…

Review of treatment for alopecia totalis and alopecia universalis.

Alopecia areata (AA) is an autoimmune disease directed at the hair follicle. Although usually limited to patchy hair loss over the scalp (fo … mic therapy, immunosuppressive agents, TNFα inhibitors, and other therapies, such as sulfasalazine, bexarotene, JAK inhibitors, and simvastatin/ezetimibe. Although certain treatments showed significant hair regrowth, no treatment was completely effective. The most promising therapies with the highest quality data include diphenylcyclopropenone, squaric acid …

The retinoid X receptor: a nuclear receptor that modulates the sleep-wake cycle in rats.

RATIONALE: The nuclear receptor retinoid X receptor (RXR) belongs to a nuclear receptor superfamily that modulates diverse functions via homodimerization with itself or several other nuclear receptors, including PPARα. While the activation of PPARα by natural or synthetic agonists regulates the sleep-wake cycle, the role of RXR in the sleep modulation is unknown. OBJECTIVES: We investigated the effects of bexarotene (Bexa, a RXR agonist) or UVI 3003 (UVI, a RXR antagonist) on sleep, sleep homeostasis, levels of neurochemical related to sleep modulation, and c-Fos and NeuN expression. METHODS…

Anticancer Drug-induced Thyroid Dysfunction.

Cancer immunotherapy and targeted therapy, though less toxic than conventional chemotherapy, can increase the risk of thyroid dysfunction. I … diotherapeutic agent for tumours derived from neural crest cells, can cause primary hypothyroidism. Bexarotene can produce transient central hypothyroidism by altering the feedback effect of thyroid hormone on the pituitary gland. Thyroid dysfunction can be managed in the usual manner without a requirement for dose reduction or discontinuation of the implica …

CD8+ mycosis fungoides clinically masquerading as alopecia areata.

A 33-year-old female with a 7-year history of CD8-positive hypopigmented mycosis fungoides (MF) involving the trunk and extremities presente … ing the bulb portion of several hair follicles. Treatments for her MF lesions have included topical bexarotene, topical corticosteroids and phototherapy. Her alopecia has been treated with high potency topical corticosteroids and multiple intralesional triamcinolone injections with very minimal hair regrowth to date. Alopecia due to cutaneous lymphoma is an …

Evaluation of mortality, prognostic parameters, and treatment efficacy in mycosis fungoides.

BACKGROUND AND OBJECTIVES: Mycosis fungoides (MF), the most common primary cutaneous T-cell lymphoma, is characterized by a variable clinica … ease stage. Only single-agent interferon-α and phototherapy combined with interferon-α or retinoids/bexarotene achieved long-term disease control in MF. CONCLUSIONS: Our data support predictive validity of prognostic factors and models in MF and identified further potential parameters associated with poor survival. Prospective studies on prognostic indices …

Novel therapeutic approaches for cutaneous T cell lymphomas.

Introduction: Cutaneous T-cell lymphoma (CTCL) is a rare non-Hodgkin's lymphoma, characterized by malignant T cells infiltrating the skin. CTCL exhibits vast heterogeneity which complicates diagnosis and therapeutic strategies. Current CTCL treatment includes skin-directed therapies (such as topical corticosteroid, topical mechlorethamine, topical bexarotene, ultraviolet phototherapy and localized radiotherapy), total skin electron beam therapy and systemic therapies. Elucidation of molecular and signaling pathways underlying CTCL pathogenesis leads to identification of innovative and personal…

Management experience of advanced-stage mycosis fungoides/Sézary syndrome: a retrospective study from Spanish haematology referral units.

BACKGROUND: Advanced-stage mycosis fungoides/Sézary syndrome (aMF/SS) has a dismal outcome. The only curative treatment is allogeneic stem c … cent of patients received systemic therapy. The median number of therapies was three (range: 1-9). Bexarotene (21%), CHOP-like chemotherapy (10%) and methotrexate (9%) were the more common treatments. The overall survival at a median follow-up of 28 months (range: 8-65 months) for aMF/SS was 56.9%. Survival probability was more favourable for MF (p < 0.02). …

Overview of cutaneous T-cell lymphoma: prognostic factors and novel therapeutic approaches.

The cutaneous T-cell lymphomas (CTCL) comprise a heterogeneous group of entities. The WHO classification distinguishes indolent low-risk ent … egimens are palliative with no demonstrated survival benefit. Among the novel therapies for CTCL is bexarotene, a retinoid X-receptor (RXR)-selective agonist, which has demonstrated efficacy in advanced refractory CTCL. Other novel agents include the interleukin (IL)-2 fusion toxin (ONTAK), pentostatin (a potent adenosine deaminase inhibitor), histone deacet …

Amino acid transporter SLC38A3 mediates bone cancer pain in rats via the PI3K/AKT/TRPV1 signaling pathway.

Bone cancer pain (BCP), one of the most intractable symptoms in patients with cancer, remains poorly understood and lacks effective therapeu … g pathway corresponds with BCP-related pain behaviors and expression patterns of SLC38A3 and TRPV1. Bexarotene alleviates BCP in rats by suppressing the aberrant overexpression of SLC38A3, thereby blocking the PI3K/AKT signaling pathway-mediated upregulation of TRPV1. These findings indicate that SLC38A3, through its downstream PI3K/AKT-TRPV1 axis, may serve …

Mechanisms related to the pathophysiology and management of central hypothyroidism.

Central hypothyroidism (CH) is defined as hypothyroidism due to insufficient stimulation of the thyroid gland by TSH, for which secretion or activity can be impaired at the hypothalamic or pituitary levels. Patients with CH frequently present with multiple other pituitary hormone deficiencies. In addition to classic CH induced by hypothalamic-pituitary tumors or Sheehan syndrome, novel causes include traumatic brain injury or subarachnoid hemorrhage, bexarotene (a retinoid X receptor agonist) therapy, neonates being born to mothers with insufficiently controlled Graves disease, and lymphocytic…

Choices in the treatment of cutaneous T-cell lymphoma.

Mycosis fungoides is responsive to treatment in the early stages; patients have a long duration of survival but are rarely cured of the dise … nd its toxic effects can usually be controlled using prophylactic therapies. The synthetic retinoid bexarotene (Targretin) is taken orally and produces high response rates in CTCL, with a good long-term tolerability profile. Conventional systemic chemotherapies produce rapid responses and high response rates in CTCL, but these are generally of short duration …

Dual Anti-inflammatory Actions of a Novel Retinoid X Receptor Agonist Derived from a Natural Compound in Microglial Cells.

Microglia-mediated neuroinflammation plays a critical role in the onset and progression of Alzheimer's disease. In a previous study, we synt … of 6OHA on BV-2 microglial cells following 2 h of LPS exposure. Similar to the existing RXR agonist bexarotene (Bex), 6OHA treatment (0.1 and 1 μM) resulted in a dose-dependent decrease in the mRNA levels of proinflammatory mediators, including interleukin-1β (Il1b), Il6, and inducible nitric oxide synthase. However, these effects on proinflammatory mediator …

Селективный ретиноид X рецептор агонизм способствует функциональному восстановлению и миелиническому ремонту в экспериментальном аутоиммунном энцефаломиелите.

Доказательства того, что ремонт миелина имеет решающее значение для функционального восстановления при множественном склерозе (МС), привели к идентификации бенсаротина (БХТ). Этот клинически многообещающий ремиелионирующий агент активирует множество подтипов ядерного гормонального рецептора, связанных с ремонтом миелина. Однако BXT вызывает неприемлемую гиперлипидемию. Напротив, IRX4204 избирательно активирует ретиноид X рецептор (RXR). Учитывая неопровержимые связи между активацией RXR и увеличением миелинового ремонта, мы использовали IRX4204 для исследования воздействия только агонизма RXR

Совпадение в аннотации оригинала
Evidence that myelin repair is crucial for functional recovery in multiple sclerosis (MS) led to the identification of bexarotene (BXT). This clinically promising remyelinating agent activates multiple nuclear hormone receptor subtypes implicated in myelin repair. However, BXT produces unacceptable hyperlipidemia. In contrast, IRX4204 selectively activates t…

Structural and Mechanistic Insights into the Main Protease (Mpro) Dimer Interface Destabilization Inhibitor: Unveiling New Therapeutic Avenues against SARS-CoV-2.

SARS-CoV-2 variant recurrence has emphasized the imperative prerequisite for effective antivirals. The main protease (Mpro) of SARS-CoV-2 is crucial for viral replication, making it one of the prime and promising antiviral targets. Mpro features several druggable sites, including active sites and allosteric sites near the dimerization interface, that regulate its catalytic activity. This study identified six highly efficacious antiviral SARS-CoV-2 compounds (WIN-62577, KT185, bexarotene, ledipasvir, diacerein, and simepervir) using structure-based virtual screening of compound libraries agains…

Clinical characterization of mycosis fungoides with abnormal light reactions induced by narrow-band UVB therapy: A review of a single-center experience.

Narrow-band UVB (NB-UVB) therapy at a wavelength of 311 nm is often used to treat mycosis fungoides (MF). However, we occasionally encounter cases of erythema induced by low doses of NB-UVB, known as an abnormal light reaction (ALR). We investigated the incidence of ALR in patients with MF and the association between ALR and clinical and laboratory findings. Forty patients (30 men and 10 women) with MF (excluding patients treated with bexarotene or etretinate) who received NB-UVB therapy at the Department of Dermatology, University of Toyama, from January to December 2022 were analyzed. ALR wa…

Novel pharmacotherapy targeting the positive symptoms of schizophrenia.

INTRODUCTION: The severity of positive symptoms in schizophrenia is associated with poor prognosis. About one-third of schizophrenia patient … rbide, propentofylline, sodium nitroprusside; metabolic regulators: diazoxide, allopurinol; others: bexarotene, raloxifene [in women]). The effectiveness of the latter compounds indicates that other biological systems, such as immunity or metabolism can be object of future research to identify pharmacological targets for positive symptoms of schizophrenia. M …

[Mycosis fungoides bullosa: A rare clinical presentation].

INTRODUCTION: Mycosis fungoides (MF) is the most common form of cutaneous lymphoma and usually manifests as erythematous and scaly patches o … d was ruled out by additional exams. Our patient was successively treated with combined interferon, bexarotene and methotrexate, followed by vorinostat, resulting in partial remission. DISCUSSION: Cases of bullous MF are very rare. In the literature, the clinical presentation is heterogeneous, with tense or flaccid bullae that can occur on unaffected skin o …

Rapid Evolving Unilateral Indurated Oozing Facial Plaques in a Patient with Head-and-Neck Cancer: Peripheral T-Cell Lymphoma Not Otherwise Specified (NOS).

BACKGROUND: The sudden development of facial plaques and nodules may be an alarming clinical sign for underlying malignancies. Nevertheless, … face and isotretinoin was stopped. Skin biopsy suggested mycosis fungoid and an oral treatment with bexarotene was started. After limited response for another eight weeks, he returned later with massive facial swelling, nodules and impetiginization. Another skin biopsy was performed to exclude diagnostic error or investigate possible disease progression. Mic …