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About liver disease

Nuclear receptors

Nuclear receptors are a class of recognized therapeutic targets already exploited by the pharmaceutical industry.

At Genfit, as world-leading experts in gene regulation and nuclear receptors, we leverage the potential of these therapeutic targets to develop next generation treatments.

As transcription factors, nuclear receptors are intracellular receptors that participate in numerous fundamental physiological mechanisms. For example, they regulate key biological functions such as lipid and glucose metabolism, as well as the proliferation and differentiation of certain cell types.

gene-mod

Nuclear receptors as therapeutic targets

The nuclear receptors are important for homeostatic control and for adaptation to environmental variation. They thus participate in the molecular mechanisms whose dysregulation is associated with metabolic diseases (dyslipidemia, diabetes), inflammatory diseases, and certain types of cancer.

The therapeutic potential of certain nuclear receptors is already exploited by the pharma industry, such that they are the molecular target of approximately 13% of authorized medications (for example, estrogens, glucocorticoids, androgens, vitamin D, fibrates). The orphan nuclear receptors, for which no natural ligand has been identified, represent another potential source of therapeutic targets.

ROR and Rev-Erb, examples of key nuclear receptors targeted at Genfit

The nuclear receptors ROR (α, β, γ) and Rev-Erb (α, β) are implicated in key physiological processes such as the regulation of lipid and glucose metabolism. They also participate in the regulation of certain inflammatory responses. The identification and characterization of synthetic ligands for these nuclear receptors thus represents a therapeutic opportunity for the treatment of certain metabolic and inflammatory diseases.

Based on the understanding of the physiopathological implications of ROR and Rev-Erb in diseases of interest for Genfit, we are exploring two novel therapeutic approaches related to RORγ and Rev-Erbα respectively.

Programs
TGFTX1

In the TGFTX1 program, Genfit has selected RORγt (RORgamma-t), a key Nuclear Receptor that directs IL-17 mediated immunity and represents an attractive and widely recognized target to treat inflammatory and auto-immune diseases.

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