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October 27, 2017

Isoform-Selective ATAD2 Chemical Probe with Novel Chemical Structure and Unusual Mode of Action

October 18, 2017|ACS Chemical Biology|Isoform-Selective ATAD2 Chemical Probe with Novel Chemical Structure and Unusual Mode of Action ATAD2 (ANCCA) is an epigenetic regulator and transcriptional cofactor, whose overexpression has been linked to the progress of various cancer types. Here, we report a DNA-encoded library screen leading to the discovery of BAY-850, a potent and isoform […]

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April 26, 2017

Structural insight into allosteric modulation of protease-activated receptor 2

April 26, 2017|Nature|Structural insight into allosteric modulation of protease-activated receptor 2 Protease-activated receptors (PARs) are a family of G-protein-coupled receptors (GPCRs) that are irreversibly activated by proteolytic cleavage of the N terminus, which unmasks a tethered peptide ligand that binds and activates the transmembrane receptor domain, eliciting a cellular cascade in response to inflammatory signals […]

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January 5, 2017

Discovery of a potent BTK inhibitor with a novel binding mode using parallel selections with a DNA-encoded chemical library.

2017 Jan. 5|Chembiochem.|Discovery of a potent BTK inhibitor with a novel binding mode using parallel selections with a DNA-encoded chemical library. We have identified and characterized novel potent inhibitors of Bruton’s tyrosine kinase (BTK) from a single DNA encoded library of over 110 million compounds using multiple parallel selection conditions…Analysis of the co-crystal structure of […]

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December 9, 2016

DNA-encoded chemistry: enabling the deeper sampling of chemical space.

Dec 9, 2016|Nat Rev Drug Discov.|DNA-encoded chemistry: enabling the deeper sampling of chemical space. DNA-encoded chemical library technologies are increasingly being adopted in drug discovery for hit and lead generation…This Review provides an overview of the development and applications of DNA-encoded chemistry, highlighting the challenges and future directions for the use of this technology. [Read […]

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November 18, 2016

Discovery of cofactor-specific, bactericidal Mycobacterium tuberculosis InhA inhibitors using DNA-encoded library technology.

Nov. 18, 2016|Proc Natl Acad Sci U S A.|Discovery of cofactor-specific, bactericidal Mycobacterium tuberculosis InhA inhibitors using DNA-encoded library technology. Millions of individuals are infected with and die from tuberculosis (TB) each year, and multidrug-resistant (MDR) strains of TB are increasingly prevalent…We describe here the use of DNA-encoded X-Chem (DEX) screening, combined with selection of […]

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June 10, 2015

Encoded Library Synthesis Using Chemical Ligation and the Discovery of sEH Inhibitors from a 334-Million Member Library.

Jun 10, 2015|Sci. Rep.|Encoded Library Synthesis Using Chemical Ligation and the Discovery of sEH Inhibitors from a 334-Million Member Library. A chemical ligation method for construction of DNA-encoded small-molecule libraries has been developed. Taking advantage of the ability of the Klenow fragment of DNA polymerase to accept templates with triazole linkages in place of phosphodiesters, […]

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June 1, 2015

Chemical ligation methods for the tagging of DNA-encoded chemical libraries.

June 2015|Curr Opin Chem Biol.|Chemical ligation methods for the tagging of DNA-encoded chemical libraries. The generation of DNA-encoded chemical libraries requires the unimolecular association of multiple encoding oligonucleotides with encoded chemical entities during combinatorial synthesis processes. This has traditionally been achieved using enzymatic ligation. We discuss a range of chemical ligation methods that provide alternatives […]

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February 24, 2014

Bigger is Better

February 24, 2014 | BioCentury | “Bigger is Better” “The vision is that when the library is big enough, molecules that are practically drug candidates will emerge from the primary screen.” [Read full article]

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