Abstract:
:Aryl Hydrocarbon Receptor (AhR) constitutes a major network hub of genomic and non-genomic signaling pathways, connecting host's immune cells to environmental factors. It shapes innate and adaptive immune processes to environmental stimuli with species-, cell- and tissue-type dependent specificity. Although an ever increasing number of studies has thrust AhR into the limelight as attractive target for the development of next-generation immunotherapies, concerns exist on potential safety issues associated with small molecule modulation of the receptor. Selective AhR modulators (SAhRMs) and rapidly metabolized AhR ligands (RMAhRLs) are two classes of receptor agonists that are emerging as interesting lead compounds to bypass AhR-related toxicity in favor of therapeutic effects. In this article, we discuss SAhRMs and RMAhRLs reported in literature, covering concepts underlying their definitions, specific binding modes, structure-activity relationships and AhR-mediated functions.
journal_name
Eur J Med Chemjournal_title
European journal of medicinal chemistryauthors
Dolciami D,Ballarotto M,Gargaro M,López-Cara LC,Fallarino F,Macchiarulo Adoi
10.1016/j.ejmech.2019.111842subject
Has Abstractpub_date
2020-01-01 00:00:00pages
111842eissn
0223-5234issn
1768-3254pii
S0223-5234(19)30994-8journal_volume
185pub_type
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