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Equivalency challenge: Evaluation of Lipodox® as the generic equivalent for Doxil® in a human ovarian cancer orthotropic mouse model.
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Homogeneous and Functional Group Tolerant Ring-Closing Metathesis for DNA-Encoded Chemical Libraries
TLDR
This work addresses reaction heterogeneity, poor pH control, and catalyst decomposition in the ring-closing metathesis of DNA–chemical conjugates with a RCM reaction system that includes a novel aqueous solvent combination to enable reaction homogeneity, an acidic buffer system which masks traditionally problematic functional groups, and a decomposition-resistant catalyst which maximizes conversion to the cyclized product.
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Discovery of potent thrombin inhibitors from a protease-focused DNA-encoded chemical library
TLDR
A protease-focused DNA-encoded chemical library was designed that utilizes chemotypes known to engage conserved catalytic protease residues, and a DNA-compatible method for guanidinylation of amines and reduction of nitriles is developed.
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Discovery and characterization of bromodomain 2–specific inhibitors of BRDT
  • Zhifeng Yu, A. Ku, M. Matzuk
  • Biology, Chemistry
    Proceedings of the National Academy of Sciences
  • 26 February 2021
TLDR
This drug discovery campaign on BRDT, a validated spermatogenic-specific contraceptive target, yielded rapid discovery of potent and specific inhibitors of the second bromodomain of BRDT that have unique binding characteristics to BR DT-BD2 relative to BRDT-BD1.
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Identifying OXA-48 Carbapenemase Inhibitors using DNA-Encoded Chemical Libraries.
TLDR
Despite the low in vivo activity, CDD-97 provides new insights into OXA-48 inhibition and demonstrates the potential of using DNA-encoded chemistry technology to rapidly identify β-lactamase binders and studyβ-lacticamase inhibition, leading to clinically useful inhibitors.
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DNA-encoded chemistry technology yields expedient access to SARS-CoV-2 Mpro inhibitors
TLDR
An affinity-based screen of 4 billion DNA-encoded molecules en masse was used to identify a potent class of virus-specific inhibitors of the SARS-CoV-2 main protease (Mpro) without extensive and time-consuming medicinal chemistry.
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mTORC2 Signaling is Required for Liver Regeneration in a Cholestatic Liver Injury Murine Model.
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Identifying Oxacillinase-48 Carbapenemase InhibitorsUsing DNA-Encoded Chemical Libraries
TLDR
Despite the low in vivo activity, CDD-97 provides new insights into OXA-48 inhibition and demonstrates the potential of using DNA-encoded chemistry technology to rapidly identify β-lactamase binders and to studyβ-lacticamase inhibition, leading to clinically useful inhibitors.
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Design and construction of a stereochemically diverse piperazine-based DNA-encoded chemical library.
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Corrigendum to 'Equivalency challenge: evaluation of Lipodox® as the generic equivalent for Doxil® in a human ovarian cancer orthotropic mouse model' [Gynecol. Oncol. 141 (2016) 357-363].
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