Huarui Cui
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View article: Small-Molecule Approaches to Target Transcription Factors
Small-Molecule Approaches to Target Transcription Factors Open
Dysregulated transcription factor activity is a defining feature of various cancer types. As such, targeting oncogenic transcriptional dependency has long been pursued as a potential therapeutic approach. However, transcription factors hav…
View article: Design of Highly Fluorinated Peptides for Cell-based <sup>19</sup>F NMR
Design of Highly Fluorinated Peptides for Cell-based <sup>19</sup>F NMR Open
The design of imaging agents with high fluorine content is essential for overcoming the challenges associated with signal detection limits in 19F MRI-based molecular imaging. In addition to perfluorocarbon and fluorinated polymers, fluorin…
View article: A Structure-based Design Approach for Generating High Affinity BRD4 D1-Selective Chemical Probes
A Structure-based Design Approach for Generating High Affinity BRD4 D1-Selective Chemical Probes Open
Chemical probes for epigenetic proteins are essential tools for dissecting the molecular mechanisms for gene regulation and therapeutic development. The bromodomain and extra-terminal (BET) proteins are master transcriptional regulators. D…
View article: Super enhancer regulation of cytokine-induced chemokine production in alcoholic hepatitis
Super enhancer regulation of cytokine-induced chemokine production in alcoholic hepatitis Open
Alcoholic hepatitis (AH) is associated with liver neutrophil infiltration through activated cytokine pathways leading to elevated chemokine expression. Super-enhancers are expansive regulatory elements driving augmented gene expression. He…
View article: 4-Methyl-1,2,3-Triazoles as <i>N</i>-Acetyl-Lysine Mimics Afford Potent BET Bromodomain Inhibitors with Improved Selectivity
4-Methyl-1,2,3-Triazoles as <i>N</i>-Acetyl-Lysine Mimics Afford Potent BET Bromodomain Inhibitors with Improved Selectivity Open
The bromodomain and extra terminal (BET) protein family recognizes acetylated lysines within histones and transcription factors using two N-terminal bromodomains, D1 and D2. The protein-protein interactions between BET bromodomains, acetyl…
View article: Endothelial p300 Promotes Portal Hypertension and Hepatic Fibrosis Through C‐C Motif Chemokine Ligand 2–Mediated Angiocrine Signaling
Endothelial p300 Promotes Portal Hypertension and Hepatic Fibrosis Through C‐C Motif Chemokine Ligand 2–Mediated Angiocrine Signaling Open
Background and Aims During liver fibrosis, liver sinusoidal endothelial cells (LSECs) release angiocrine signals to recruit inflammatory cells into the liver. p300, a master regulator of gene transcription, is associated with pathological …
View article: Quantifying the Selectivity of Protein–Protein and Small Molecule Interactions with Fluorinated Tandem Bromodomain Reader Proteins
Quantifying the Selectivity of Protein–Protein and Small Molecule Interactions with Fluorinated Tandem Bromodomain Reader Proteins Open
Multidomain bromodomain-containing proteins regulate gene expression via chromatin binding, interactions with the transcriptional machinery, and by recruiting enzymatic activity. Selective inhibition of members of the bromodomain and extra…
View article: Selective N‐Terminal BET Bromodomain Inhibitors by Targeting Non‐Conserved Residues and Structured Water Displacement**
Selective N‐Terminal BET Bromodomain Inhibitors by Targeting Non‐Conserved Residues and Structured Water Displacement** Open
Bromodomain and extra‐terminal (BET) family proteins, BRD2‐4 and T, are important drug targets; however, the biological functions of each bromodomain remain ill‐defined. Chemical probes that selectively inhibit a single BET bromodomain are…
View article: Potent and Selective N-Terminal BRD4 Bromodomain Inhibitors by Targeting Non-Conserved Residues and Structured Water Displacement
Potent and Selective N-Terminal BRD4 Bromodomain Inhibitors by Targeting Non-Conserved Residues and Structured Water Displacement Open
This manuscript focuses on the structure-based design of selective inhibitors of the first bromodomain of BRD4. This manuscript uses describes organic synthesis to make inhibitors, and biophysical analysis to evaluate their inhibitor poten…
View article: Potent and Selective N-Terminal BRD4 Bromodomain Inhibitors by Targeting Non-Conserved Residues and Structured Water Displacement
Potent and Selective N-Terminal BRD4 Bromodomain Inhibitors by Targeting Non-Conserved Residues and Structured Water Displacement Open
This manuscript focuses on the structure-based design of selective inhibitors of the first bromodomain of BRD4. This manuscript uses describes organic synthesis to make inhibitors, and biophysical analysis to evaluate their inhibitor poten…
View article: Systematically Mitigating the p38α Activity of Triazole-based BET Inhibitors
Systematically Mitigating the p38α Activity of Triazole-based BET Inhibitors Open
The Bromodomain and Extra Terminal (BET) family of proteins recognize post-translational N-ε-acetylated lysine modifications, regulating transcription as "reader" proteins. Bromodomain inhibitors are interesting targets for the development…
View article: Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase–Bromodomain Inhibitor
Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase–Bromodomain Inhibitor Open
As regulators of transcription, epigenetic proteins that interpret post-translational modifications to N-terminal histone tails are essential for maintaining cellular homeostasis. When dysregulated, "reader" proteins become drivers of dise…