Nuclear Receptors: Coactivators and Transcriptional Modulation

Description

This lecture delves into the role of coactivators in modulating transcriptional activity by loosening histone complexes from DNA, exposing additional regions for transcription machinery. It explains histone acetylation, the structure of bromodomains, and the activation of transcription. The lecture also covers ERa antagonists, the membrane ER signaling pathway, tissue-specific actions of selective estrogen receptor modulators, and tissue-specific nuclear receptor signaling.

Official source

https://mediaspace.epfl.ch/media/0_q2iuyk5q

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Related concepts (25)

Selective androgen receptor modulator

Selective Androgen Receptor Modulators or SARMs are a class of androgen receptor ligands that were developed with the intention of maintaining some of the desirable effects of androgens, such as preventing osteoporosis and muscle loss while reducing risks of undesirable conditions such as prostate cancer. In the late 1990s, the first nonsteroidal SARM, an analog of bicalutamide, was discovered at Imperial Chemical Industries.

Selective receptor modulator

In the field of pharmacology, a selective receptor modulator or SRM is a type of drug that has different effects in different tissues. A SRM may behave as an agonist in some tissues while as an antagonist in others. Hence selective receptor modulators are sometimes referred to as tissue selective drugs or mixed agonists / antagonists. This tissue selective behavior is in contrast to many other drugs that behave either as agonists or antagonists regardless of the tissue in question.

Selective glucocorticoid receptor modulator

Selective glucocorticoid receptor modulators (SEGRMs) and selective glucocorticoid receptor agonists (SEGRAs) formerly known as dissociated glucocorticoid receptor agonists (DIGRAs) are a class of experimental drugs designed to share many of the desirable anti-inflammatory, immunosuppressive, or anticancer properties of classical glucocorticoid drugs but with fewer side effects such as skin atrophy. Although preclinical evidence on SEGRAMs’ anti-inflammatory effects are culminating, currently, the efficacy of these SEGRAMs on cancer are largely unknown.

Histone acetyltransferase

Histone acetyltransferases (HATs) are enzymes that acetylate conserved lysine amino acids on histone proteins by transferring an acetyl group from acetyl-CoA to form ε-N-acetyllysine. DNA is wrapped around histones, and, by transferring an acetyl group to the histones, genes can be turned on and off. In general, histone acetylation increases gene expression. In general, histone acetylation is linked to transcriptional activation and associated with euchromatin.

Selective estrogen receptor modulator

Selective estrogen receptor modulators (SERMs), also known as estrogen receptor agonist/antagonists (ERAAs), are a class of drugs that act on the estrogen receptor (ER). A characteristic that distinguishes these substances from pure ER agonists and antagonists (that is, full agonists and silent antagonists) is that their action is different in various tissues, thereby granting the possibility to selectively inhibit or stimulate estrogen-like action in various tissues.