Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation
…, EJ Roberts, D Vassiliadis, ML Burr, AGS Preston… - Science, 2020 - science.org
The two tandem bromodomains of the BET (bromodomain and extraterminal domain) proteins
enable chromatin binding to facilitate transcription. Drugs that inhibit both bromodomains …
enable chromatin binding to facilitate transcription. Drugs that inhibit both bromodomains …
[HTML][HTML] HIV-1 and microvesicles from T cells share a common glycome, arguing for a common origin
L Krishnamoorthy, JW Bess Jr, AB Preston… - Nature chemical …, 2009 - nature.com
HIV-1 is a master at deceiving the immune system and usurping host biosynthetic machinery.
Although HIV-1 is coated with host-derived glycoproteins, only glycosylation of viral gp120 …
Although HIV-1 is coated with host-derived glycoproteins, only glycosylation of viral gp120 …
Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 2. Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives
SM Westaway, AGS Preston, MD Barker… - Journal of medicinal …, 2016 - ACS Publications
Following the discovery of cell penetrant pyridine-4-carboxylate inhibitors of the KDM4 (JMJD2)
and KDM5 (JARID1) families of histone lysine demethylases (eg, 1), further optimization …
and KDM5 (JARID1) families of histone lysine demethylases (eg, 1), further optimization …
The optimization of a novel, weak bromo and extra terminal domain (BET) bromodomain fragment ligand to a potent and selective second bromodomain (BD2) …
…, AM Michon, D Mitchell, A Preston… - Journal of Medicinal …, 2020 - ACS Publications
The profound efficacy, yet associated toxicity of pan-BET inhibitors is well documented. The
possibility of an ameliorated safety profile driven by significantly selective (>100-fold) …
possibility of an ameliorated safety profile driven by significantly selective (>100-fold) …
Design and Synthesis of a Highly Selective and In Vivo-Capable Inhibitor of the Second Bromodomain of the Bromodomain and Extra Terminal Domain Family of …
A Preston, S Atkinson, P Bamborough… - Journal of Medicinal …, 2020 - ACS Publications
Pan-bromodomain and extra terminal domain (BET) inhibitors interact equipotently with the
eight bromodomains of the BET family of proteins and have shown profound efficacy in a …
eight bromodomains of the BET family of proteins and have shown profound efficacy in a …
Discovery of a highly selective BET BD2 inhibitor from a DNA-encoded library technology screening hit
…, C Messenger, A Phillipou, A Preston… - Journal of Medicinal …, 2021 - ACS Publications
Second-generation bromodomain and extra terminal (BET) inhibitors, which selectively target
one of the two bromodomains in the BET proteins, have begun to emerge in the literature. …
one of the two bromodomains in the BET proteins, have begun to emerge in the literature. …
[PDF][PDF] Hepcidin-mediated hypoferremia disrupts immune responses to vaccination and infection
Background How specific nutrients influence adaptive immunity is of broad interest. Iron
deficiency is the most common micronutrient deficiency worldwide and imparts a significant …
deficiency is the most common micronutrient deficiency worldwide and imparts a significant …
Cell penetrant inhibitors of the KDM4 and KDM5 families of histone lysine demethylases. 1. 3-Amino-4-pyridine carboxylate derivatives
SM Westaway, AGS Preston, MD Barker… - Journal of Medicinal …, 2016 - ACS Publications
Optimization of KDM6B (JMJD3) HTS hit 12 led to the identification of 3-((furan-2-ylmethyl)amino)pyridine-4-carboxylic
acid 34 and 3-(((3-methylthiophen-2-yl)methyl)amino)pyridine-4-…
acid 34 and 3-(((3-methylthiophen-2-yl)methyl)amino)pyridine-4-…
Plasma iron controls neutrophil production and function
Low plasma iron (hypoferremia) induced by hepcidin is a conserved inflammatory response
that protects against infections but inhibits erythropoiesis. How hypoferremia influences …
that protects against infections but inhibits erythropoiesis. How hypoferremia influences …
Use of quality improvement strategies among small to medium-size US primary care practices
…, DJ Cohen, RL Ward, A Preston… - The Annals of Family …, 2018 - Annals Family Med
PURPOSE Improving primary care quality is a national priority, but little is known about the
extent to which small to medium-size practices use quality improvement (QI) strategies to …
extent to which small to medium-size practices use quality improvement (QI) strategies to …