5 research outputs found
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Light Controlled Modulation of Gene Expression by Chemical Optoepigenetic Probes
Epigenetic gene regulation is a dynamic process orchestrated by chromatin-modifying enzymes. Many of these master regulators exert their function through covalent modification of DNA and histone proteins. Aberrant epigenetic processes have been implicated in the pathophysiology of multiple human diseases. Small-molecule inhibitors have been essential to advancing our understanding of the underlying molecular mechanisms of epigenetic processes. However, the resolution offered by small molecules is often insufficient to manipulate epigenetic processes with high spatio-temporal control. Here, we present a novel and generalizable approach, referred to as ‘Chemo-Optical Modulation of Epigenetically-regulated Transcription’ (COMET), enabling high-resolution, optical control of epigenetic mechanisms based on photochromic inhibitors of human histone deacetylases using visible light. COMET probes may translate into novel therapeutic strategies for diseases where conditional and selective epigenome modulation is required
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Monoalkoxy BODIPYsî—¸A Fluorophore Class for Bioimaging
Small molecule fluorophores are indispensable
tools for modern
biomedical imaging techniques. In this report, we present the development
of a new class of BODIPY dyes based on an alkoxy-fluoro-boron-dipyrromethene
core. These novel fluorescent dyes, which we term MayaFluors, are
characterized by good aqueous solubility and favorable <i>in
vitro</i> physicochemical properties. MayaFluors are readily
accessible in good yields in a one-pot, two-step approach starting
from well-established BODIPY dyes, and allow for facile modification
with functional groups of relevance to bioconjugate chemistry and
bioorthogonal labeling. Biological profiling in living cells demonstrates
excellent membrane permeability, low nonspecific binding, and lack
of cytotoxicity