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Updated: Jul 10, 2025

Rapid Synthesis and Screening of Chemically Activated Transcription Factors with GFP-based Reporters
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Rapid Synthesis and Screening of Chemically Activated Transcription Factors with GFP-based Reporters

Published on: November 26, 2013

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核局所化と標的型転写制御を誘導する二機能小分子

William J Gibson1,2, Ananthan Sadagopan1,2, Veronika M Shoba1

  • 1Broad Institute of Harvard and MIT, 415 Main Street, Cambridge, Massachusetts 02142, United States.

Journal of the American Chemical Society
|November 22, 2023
PubMed
まとめ

研究者は細胞内のタンパク質の局所化を制御するために二機能分子を設計し,潜在的な癌および神経変性疾患の治療のために標的の核輸入を可能にしました.

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Nuclear receptors, or NRs, are unique transcription factors that regulate gene transcription and affect the cellular pathways involved in reproduction, development, or metabolism. Their ability to be stimulated by small lipophilic ligands and control vital cellular processes makes them ideal drug targets. Nearly 10-15% of currently prescribed drugs target these receptors.
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Signal Transduction: Overview

Cells respond to many types of information, often through receptor proteins positioned on the membrane. They respond to chemical signals, such as hormones, neurotransmitters, and other signaling molecules, initiating a series of molecular reactions to produce an appropriate response. This is called signal transduction. Cells also coordinate different responses elicited by the same signaling molecule via mediators, allowing molecular cross-talk.
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Eukaryotic Transcription Inhibitors

Certain biochemical processes, such as embryonic development and cell growth regulation, depend on the repression of specific genes. DNA binding proteins known as eukaryotic transcription inhibitors regulate the repression of gene expression in eukaryotes. The presence of these inhibitors at the required location and time in the cell is triggered by the presence of hormones and additional signals from other cells.
Eukaryotic transcription inhibitors usually contain two distinct domains, a...
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Master transcription regulators are regulatory proteins that are predominantly responsible for regulating the expression of multiple genes. Often these genes work in concert to drive a  complex process. Activation of a master transcription regulator can lead to a cascade of transcriptional activation necessary for that outcome. These regulators can directly bind to the regulatory sequences of the various genes involved, or they can indirectly regulate transcription by binding to regulatory...
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