REV-ERB and ROR nuclear receptors as drug targets
نویسندگان
چکیده
منابع مشابه
Cross-Talk among RORal and the Rev-erb Family of Orphan Nuclear Receptors
We have cloned Rev-erbfi, a novel isoform of the Rev-erba orphan nuclear receptor. The DNA binding domains of Rev-erba and fl are highly related to each other and to the retinoic acid related orphan receptor (ROR)/RZR subfamily of nuclear receptors. Indeed, we find that all three receptors bind as monomers to the sequence AATGT-AGGTCA. Whereas RORal constitutively activates transcription throug...
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Nuclear hormone receptors (NRs) function as ligand dependent DNA binding proteins that translate physiological/nutritional signals into gene regulation. Dysfunctional NR signaling leads to many disorders in reproduction, inflammation, and metabolism. The opportunity to identify novel regulatory pathways in the context of human health and disease drives the challenge to unravel the biological fu...
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The circadian clock acts at the genomic level to coordinate internal behavioural and physiological rhythms via the CLOCK–BMAL1 transcriptional heterodimer. Although the nuclear receptors REV-ERB-a and REV-ERB-b have been proposed to form an accessory feedback loop that contributes to clock function, their precise roles and importance remain unresolved. To establish their regulatory potential, w...
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Nuclear receptors (NRs) are ideal targets for drug discovery. Not only do they control a myriad of biological and disease processes, but they are also regulated by small lipophilic molecules that can be easily exchanged with a drug of choice. All 48 of the NR genes in the human genome have been identified, many of their structures have been solved and their ligands identified. Their mechanism o...
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Nuclear receptors are a large superfamily of transcription factors involved in important physiological functions such as control of embryonic development, organ physiology, cell differentiation and homeostasis [1–3]. Apart from the normal physiology, nuclear receptors have been identified to play a role inmany pathological processes, such as cancer, diabetes, rheumatoid arthritis, asthma or hor...
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ژورنال
عنوان ژورنال: Nature Reviews Drug Discovery
سال: 2014
ISSN: 1474-1776,1474-1784
DOI: 10.1038/nrd4100