Selective RAR agonists for acne vulgaris: A narrative review

Kassir, Martin; Karagaiah, Priyanka; Sonthalia, Sidharth; Katsambas, Andreas; Galadari, Hassan; Gupta, Mrinal; Lotti, Torello; Wollina, Uwe; Abdelmaksoud, Ayman; Grabbe, Stephan; Goldust, Mohamad

doi:10.1111/jocd.13340

Cited by 20 publications

(20 citation statements)

References 38 publications

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“…Retinoids are vitamin A-derived agonists of the retinoic acid receptors α, β, and γ (RAR-α, RAR-β, RAR-γ) [86,87]. Retinoic acid receptors are a group of nuclear hormone receptors that form into a homo/hetero-dimer upon ligand binding.…”

Section: Edcs and Retinoidsmentioning

confidence: 99%

“…Retinoic acid receptors are a group of nuclear hormone receptors that form into a homo/hetero-dimer upon ligand binding. This dimer complex then binds to nuclear responsive elements RARE (retinoic acid response element) or RXRE (retinoid X receptor response element) to activate transcription of gene expression [87]. As previously discussed, EDCs are known to participate in all aspects of nuclear hormone receptor function (See "Effects of EDCs on Endogenous Hormone Pathways").…”

Section: Edcs and Retinoidsmentioning

confidence: 99%

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Endocrine Disrupting Chemicals, Hormone Receptors, and Acne Vulgaris: A Connecting Hypothesis

Rao

Douglas

Hall

2021

Cells

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The relationship between endocrine disrupting chemicals (EDCs) and the pathogenesis of acne vulgaris has yet to be explored in the literature. Acne vulgaris is a chronic inflammatory skin disease of the pilosebaceous unit. The pathogenesis of acne involves several hormonal pathways, including androgens, insulin-like growth factor 1(IGF-1), estrogens, and corticosteroids. EDCs influence these pathways primarily through two mechanisms: altering endogenous hormone levels and interfering with hormone receptor function. This review article describes the mechanistic links between EDCs and the development of acne lesions. Highlighted is the contributory role of androgen receptor ligands, such as bisphenol A (BPA) and mono-2-ethylhexyl Phthalate (MEHP), via upregulation of lipogenic genes and resultant exacerbation of cholesterol synthesis. Additionally discussed is the protective role of phytoestrogen EDCs in counteracting androgen-induced sebocyte maturation through attenuation of PPARy transcriptional activity (i.e., resveratrol) and restoration of estrogen-regulated TGF-B expression in skin cells (i.e., genistein). Examination of the relationship between EDCs and acne vulgaris may inform adjunctive avenues of treatment such as limiting environmental exposures, and increasing low-glycemic, plant-rich foods in the diet. With a better understanding of the cumulative role that EDCs play in acne, clinicians can be better equipped to treat and ultimately improve the lives of their patients.

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Section: Edcs and Retinoidsmentioning

confidence: 99%

Section: Edcs and Retinoidsmentioning

confidence: 99%

Endocrine Disrupting Chemicals, Hormone Receptors, and Acne Vulgaris: A Connecting Hypothesis

Rao

Douglas

Hall

2021

Cells

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“…Recently was approved trifarotene, a fourth-generation representative. Trifarotene is a new selective RAR-γ agonist and has 20-fold higher selectivity versus RAR-α and RAR-β receptors [ 8 , 9 ].…”

Section: Introductionmentioning

confidence: 99%

Recent Advances Regarding the Therapeutic Potential of Adapalene

et al. 2020

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Adapalene (ADP) is a representative of the third retinoids generation and successfully used in first-line acne treatment. ADP binds to retinoic acid nuclear receptors. The comedolytic, anti-inflammatory, antiproliferative, and immunomodulatory are the known ADP effects. Its safety profile is an advantage over other retinoids. ADP recently was found to be effective in the treatment of several dermatological diseases and photoaging besides the utility in the treatment of acne vulgaris. New biological effects of adapalene with therapeutic potential are highlighted in this review paper. Thus, adapalene could be a valuable therapeutic drug into the treatment of several types of cancer. Additionally, some neurodegenerative diseases could be treated with a suitable formulation for intravenous administration. The antibacterial activity against methicillin-resistant Staphylococcus aureus of an analogue of ADP has been proven. In different therapeutic schemes, ADP is more effective in combination with other active substances. New topical combinations with adapalene include ketoconazole (antifungal), mometasone furoate (anti-inflammatory corticosteroid), nadifloxacin (fluoroquinolone), and alfa and beta hydroxy acids. Combination with oral drugs is a new trend that enhances the properties of topical formulations with adapalene. Several studies have investigated the effects of ADP in co-administration with azithromycin, doxycycline, faropenem, isotretinoin, and valganciclovir. Innovative formulations of ADP also aim to achieve a better bioavailability, increased efficacy, and reduced side effects. In this review, we have highlighted the current studies on adapalene regarding biological effects useful in various treatment types. Adapalene has not been exploited yet to its full biological potential.

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“…Tazarotene is a synthetic third-generation retinoid derived from vitamin A, which has proved to be beneficial in modulating keratinocyte proliferation and in reducing inflammation [14]. In particular, tazarotene effect is mediated by the up-regulation of the intracellular retinoic acid-binding protein-II expression [41]. This protein transactivates nuclear retinoic acid receptors (RARs), in particular RARβ and RARγ, by binding to specific DNA sequences on their promoter gene regions, thus leading to a reduced proliferation of normal and neoplastic cells and favoring cellular differentiation and apoptosis [41].…”

Section: Dermatophytesmentioning

confidence: 99%

Retinoids in Fungal Infections: From Bench to Bedside

et al. 2021

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Retinoids—a class of chemical compounds derived from vitamin A or chemically related to it—are used especially in dermatology, oncohematology and infectious diseases. It has been shown that retinoids—from their first generation—exert a potent antimicrobial activity against a wide range of pathogens, including bacteria, fungi and viruses. In this review, we summarize current evidence on retinoids’ efficacy as antifungal agents. Studies were identified by searching electronic databases (MEDLINE, EMBASE, PubMed, Cochrane, Trials.gov) and reference lists of respective articles from 1946 to today. Only articles published in the English language were included. A total of thirty-nine articles were found according to the criteria. In this regard, to date, In vitro and In vivo studies have demonstrated the efficacy of retinoids against a broad-spectrum of human opportunistic fungal pathogens, including yeast fungi that normally colonize the skin and mucosal surfaces of humans such as Candida spp., Rhodotorula mucilaginosa and Malassezia furfur, as well as environmental moulds such as Aspergillus spp., Fonsecae monofora and many species of dermatophytes associated with fungal infections both in humans and animals. Notwithstanding a lack of double-blind clinical trials, the efficacy, tolerability and safety profile of retinoids have been demonstrated against localized and systemic fungal infections.

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Selective RAR agonists for acne vulgaris: A narrative review

Cited by 20 publications

References 38 publications

Endocrine Disrupting Chemicals, Hormone Receptors, and Acne Vulgaris: A Connecting Hypothesis

Endocrine Disrupting Chemicals, Hormone Receptors, and Acne Vulgaris: A Connecting Hypothesis

Recent Advances Regarding the Therapeutic Potential of Adapalene

Retinoids in Fungal Infections: From Bench to Bedside

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