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Synthesis and Anti-Cancer Activity of the Novel Selective Glucocorticoid Receptor Agonists of the Phenylethanolamine Series.
Int J Mol Sci
August 2024
Department of Chemical Carcinogenesis, Institute of Carcinogenesis, N.N. Blokhin National Medical Research Center for Oncology, Kashirskoe Shosse 24-15, Moscow 115478, Russia.
Article Synopsis
- Glucocorticoids (GCs) are commonly used to treat blood cancers but can cause various side effects due to how they interact with glucocorticoid receptors (GRs).
- Selective GR agonists (SEGRAs) like CpdA aim to enhance the beneficial anticancer effects while minimizing side effects; however, CpdA faces challenges with chemical instability.
- The newly developed derivative, CpdA-03, shows improved stability and GR affinity, demonstrating significant anticancer activity in lymphoma models, with a tripling reduction in tumor volume compared to conventional treatments.
Synephrine and Its Derivative Compound A: Common and Specific Biological Effects.
Int J Mol Sci
December 2023
Department of Chemical Carcinogenesis, N.N. Blokhin National Medical Research Center of Oncology, 115478 Moscow, Russia.
This review is focused on synephrine, the principal phytochemical found in bitter orange and other medicinal plants and widely used as a dietary supplement for weight loss/body fat reduction. We examine different aspects of synephrine biology, delving into its established and potential molecular targets, as well as its mechanisms of action. We present an overview of the origin, chemical composition, receptors, and pharmacological properties of synephrine, including its anti-inflammatory and anti-cancer activity in various in vitro and animal models.
View Article and Find Full Text PDFBoswellic acids and their derivatives as potent regulators of glucocorticoid receptor actions.
Arch Biochem Biophys
November 2020
Department of Biochemistry and Biotechnology, University of Thessaly, Larissa, Greece. Electronic address:
Glucocorticoid (GCs) hormones exert their actions via their cognate steroid receptors the Glucocorticoid Receptors (GR), by genomic or non-genomic mechanisms of actions. GCs regulate many cellular functions among them growth, metabolism, immune response and apoptosis. Due to their cell type specific induction of apoptosis GCs are used for the treatment of certain type of cancer.
View Article and Find Full Text PDFExperimental Glucocorticoid Receptor Agonists for the Treatment of Asthma: A Systematic Review.
J Exp Pharmacol
August 2020
Department of Medicine and Surgery, Respiratory Disease and Lung Function Unit, University of Parma, Parma, Italy.
Inhaled corticosteroids (ICSs) are considered the cornerstone of asthma treatment. Despite the solid evidence documenting the efficacy and safety of ICSs at the level of the airways, their use can be affected by pulmonary and systemic adverse events (AEs) when administered chronically and/or at high doses. Thus, there is a pharmacological and medical need for new glucocorticoid (GC) receptor (GR) ligands with a more favorable therapeutic index, in order to overcome the shortcomings of currently available ICSs.
View Article and Find Full Text PDFTopical 'dual-soft' glucocorticoid receptor agonist for dermatology.
Bioorg Med Chem Lett
September 2020
AstraZeneca, Laboratory Animal Sciences, Drug Safety and Metabolism, IMED Biotech Unit, Pepparedsleden 1, Mölndal, Sweden.
Steroidal glucocorticoids (GR agonists) have been widely used for the topical treatment of skin disorders, including atopic dermatitis. They are a very effective therapy, but they are associated with both unwanted local effects in the skin (skin thinning/atrophy) and systemic side effects. These effects can limit the long-term utility of potent steroids.
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