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Article Abstract
Psoriasis is a chronic inflammatory disease that affects the quality of life of patients. The aromatic hydrocarbon receptor (AHR) plays a pivotal role in maintaining the skin barrier integrity. In this study, we conducted a comprehensive analysis of the structure-activity relationship of Tapinarof analogues. Among them, showed low cytotoxicity (>40 μM) and potent AHR agonist activity with an EC value of 2.01 nM, which was 14-fold stronger than that of Tapinarof (28.93 nM). exhibited the ability to elevate the transcript levels of key AHR downstream pathway target genes, including CYP1A1 and CYP1B1. Upon topical application, significantly ameliorated imiquimod (IMQ)-induced psoriasis-like cutaneous manifestations and repaired the barrier function of skin, concurrently downregulating the expression levels of CD206, CD36, IL-18, and MCP-1. These findings suggested that represents a potential alternative to Tapinarof for the topical psoriasis treatment.
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| http://dx.doi.org/10.1021/acs.jmedchem.5c01060 | DOI Listing |
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Design, Optimization, and Biological Evaluation of Novel Tapinarof Analogues as AHR Agonists for Topical Psoriasis Treatment.
J Med Chem
September 2025
Hubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation, School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China.
Psoriasis is a chronic inflammatory disease that affects the quality of life of patients. The aromatic hydrocarbon receptor (AHR) plays a pivotal role in maintaining the skin barrier integrity. In this study, we conducted a comprehensive analysis of the structure-activity relationship of Tapinarof analogues.
View Article and Find Full Text PDFTherapeutic Advancements in Psoriasis and Psoriatic Arthritis.
J Clin Med
February 2025
Center for Dermatology Research, Department of Dermatology, Wake Forest University School of Medicine, Winston-Salem, NC 27157, USA.
Within the past few years, many new therapies have emerged for psoriasis and psoriatic arthritis (PsA). Current topical therapies-including corticosteroids, vitamin D analogs, tapinarof, and roflumilast-remain the mainstay for mild disease, while oral systemic and biologic options are for moderate to severe cases. Biologics-such as Tumor necrosis factor-alpha (TNF-alpha), Interleukin 12/23 (IL-12/23), Interleukin-17 (IL-17), and Interleukin-23 (IL-23)-have revolutionized care by providing highly effective and safer alternatives.
View Article and Find Full Text PDFA comparison of the safety and efficacy of tapinarof and roflumilast topical therapies in the management of mild-to-moderate plaque psoriasis.
Skin Res Technol
September 2024
Rutgers Robert Wood Johnson Medical School, New Brunswick, New Jersey, USA.
Article Synopsis
- - Psoriasis is an inflammatory skin disease treated with topical medications like steroids and vitamin D analogs; new treatments such as tapinarof and roflumilast have shown promise with their unique anti-inflammatory effects.
- - A review of recent studies identified strong efficacy and manageable side effects for both tapinarof and roflumilast in mild-to-moderate plaque psoriasis, with tapinarof having more frequent, mild side effects, while roflumilast had less frequent but more severe adverse events.
- - Both treatments allow for once-daily dosing which could improve patient adherence, but cost is a concern; further research is needed to compare their effectiveness, safety, and overall cost-effectiveness.
Tapinarof and its structure-activity relationship for redox chemistry and phototoxicity on human skin keratinocytes.
Free Radic Biol Med
October 2024
Department of Medical Chemistry and Biochemistry, Faculty of Medicine and Dentistry, Palacky University, Hněvotínská 3, 775 15, Olomouc, Czech Republic. Electronic address:
Tapinarof (3,5-dihydroxy-4-isopropylstilbene) is a therapeutic agent used in the treatment of psoriasis (VTAMA®). In this study, we examined the redox behaviour, (photo)stability, (photo)toxicity and (bio)transformation of tapinarof in the context of a structure-activity relationship study. Selected derivatives of the structurally related tapinarof were investigated, namely resveratrol, pterostilbene, pinosylvin and its methyl ether.
View Article and Find Full Text PDFAn update on topical therapies for psoriasis.
Curr Opin Rheumatol
July 2024
St Vincent's University Hospital, Elm Park.
Purpose Of Review: Topical therapies are a mainstay of treatment for mild psoriasis and may be a useful adjunct in treatment of moderate-to-severe psoriasis. This review summarizes recent advances in topical therapies for psoriasis and currently available treatments.
Recent Findings: Topical aryl hydrocarbon receptor modulators (tapinarof) and topical phosphodiesterase-4 inhibitors (roflumilast) have been proven effective in randomized controlled trials for psoriasis.