Calixarbutin: A novel calixarene-based potential water-soluble anti-tyrosinase agent with high ...

Since melanocytes are the origin of melanoma and some skin disorders such as melasma, they are important cells from the perspective of medicinal chemistry. Therefore, a medication that can simultaneously overcome these diseases will be a successful potential therapeutic agent. Arbutin with phenolic structure is a powerful natural anti-tyrosinase agent. Hence, the phenolic structure of this drug, prompted us to design its novel calix[4]arene-based cluster. Therefore, the present study reports the synthesis and in vitro bio-activities of cyclic tetramer of arbutin in comparison to its simple drug unit as the reference medication. The in vitro biological results showed amplified anti-tyrosinase (6-fold) and anti-melanoma (27-fold) activities, in addition to more aqueous solubility (8-fold) for this cluster in relation to arbutin. Therefore, compared to arbutin, more bioactive cluster can be considered as a novel water-soluble melanogenesis inhibitor with high anti-melanoma activity.
Source: Iranian Journal of Pharmaceutical Research - Category: Drugs & Pharmacology Source Type: research

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Abstract PURPOSE: Few studies have investigated the relationship between vitiligo and risks of various types of cancers, especially those other than skin cancer. Conventional observational studies are susceptible to potential confounders and inverse causation. With a Mendelian randomization approach, we were able to evaluate the causality between vitiligo and different cancer risks. METHODS: 37 vitiligo-related single-nucleotide polymorphisms identified by the published genome-wide association studies were used as instrumental variables in our study. Summary data of individual-level genetic information were o...
Source: Clinical Breast Cancer - Category: Cancer & Oncology Authors: Tags: J Cancer Res Clin Oncol Source Type: research
People with melanoma who take immune checkpoint inhibitors are less likely to develop colitis if they are taking vitamin D supplements at treatment initiation, a study published in the journal Cancer has suggested
Source: The Pharmaceutical Journal - Category: Drugs & Pharmacology Source Type: research
Understanding tumor resistance to T cell immunotherapies is critical to improve patient outcomes. Our study revealed a role for transcriptional suppression of the tumor-intrinsic HLA class I (HLA-I) antigen processing and presentation machinery (APM) in therapy resistance. Low HLA-I APM mRNA levels in melanoma metastases before immune checkpoint blockade (ICB) correlated with nonresponsiveness to therapy and poor clinical outcome. Patient-derived melanoma cells with silenced HLA-I APM escaped recognition by autologous CD8+ T cells. However, targeted activation of the innate immunoreceptor RIG-I initiated de novo HLA-I APM ...
Source: Journal of Clinical Investigation - Category: Biomedical Science Authors: Source Type: research
Aberrant DNA methylation is an epigenetic hallmark of melanoma and hypomethylating drugs with immunomodulatory activity are currently investigated in clinical trials. DNA methyltransferase 1 (DNMT1) is the major maintenance methyltransferase but its expression in melanocytic tumors is unknown. We analyzed DNMT1 expression in primary melanocytes, melanoma cell lines and 83 melanocytic tumors and explored its association with proliferation, mutational status and response to BRAF and MEK inhibition.
Source: American Journal of Pathology - Category: Pathology Authors: Tags: Regular Article Source Type: research
ACS Chemical BiologyDOI: 10.1021/acschembio.0c00222
Source: ACS Chemical Biology - Category: Chemistry Authors: Source Type: research
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Source: Pathology Research and Practice - Category: Pathology Source Type: research
AbstractSentinel lymph node biopsy is a technique to identify the first lymph node (or nodes) draining a tumor. The underlying principle is that as the first site of cancer spread, evaluation of the sentinel node will be most predictive for wider nodal involvement. The introduction of sentinel node biopsy revolutionized the surgical management of cutaneous melanoma and breast cancer, becoming a key component in the management of such patients. For over 20  years, thoracic surgeons have similarly worked to apply this technique to lung cancer but have thus far not had the same impact on lung surgery. In this review, we ...
Source: General Thoracic and Cardiovascular Surgery - Category: Cardiovascular & Thoracic Surgery Source Type: research
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Source: Journal of Dermatological Treatment - Category: Dermatology Tags: J Dermatolog Treat Source Type: research
We present a large, multi-institutional study on thick melanoma, evaluating for factors prognostic of survival.
Source: Surgery - Category: Surgery Authors: Source Type: research
ConclusionsAccumulated(int)PD-1 in T cells may contribute to enhanced immune evasion in AMM. Evaluation of intracellular PD-1 expression would be useful for better management of nivolumab-treated AMM patients in view of predicting treatment response and the incidence of irAE. Our findings further support the necessity of periodical administration of nivolumab for treating AMM.
Source: International Journal of Clinical Oncology - Category: Cancer & Oncology Source Type: research
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