Targeting Aryl hydrocarbon receptor for next-generation immunotherapies: Selective modulators (SAhRMs) versus rapidly metabolized ligands (RMAhRLs).

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 Chem

authors

Dolciami D,Ballarotto M,Gargaro M,López-Cara LC,Fallarino F,Macchiarulo A

doi

10.1016/j.ejmech.2019.111842

subject

Has Abstract

pub_date

2020-01-01 00:00:00

pages

111842

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(19)30994-8

journal_volume

185

pub_type

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