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(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells
Significance Protein methyltransferases constitute an emerging but undercharacterized class of therapeutic targets with diverse roles in normal human biology and disease. Small-molecule “chemicalExpand
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Identification of a Chemical Probe for Bromo and Extra C-Terminal Bromodomain Inhibition through Optimization of a Fragment-Derived Hit
The posttranslational modification of chromatin through acetylation at selected histone lysine residues is governed by histone acetyltransferases (HATs) and histone deacetylases (HDACs). TheExpand
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Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit.
The acetyl post-translational modification of chromatin at selected histone lysine residues is interpreted by an acetyl-lysine specific interaction with bromodomain reader modules. Here we report theExpand
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Covalent inhibitors of interleukin-2 inducible T cell kinase (itk) with nanomolar potency in a whole-blood assay.
We wish to report a strategy that targets interleukin-2 inducible T cell kinase (Itk) with covalent inhibitors. Thus far, covalent inhibition of Itk has not been disclosed in the literature.Expand
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Pyridone-conjugated monobactam antibiotics with gram-negative activity.
Herein we describe the structure-aided design and synthesis of a series of pyridone-conjugated monobactam analogues with in vitro antibacterial activity against clinically relevant Gram-negativeExpand
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Siderophore receptor-mediated uptake of lactivicin analogues in gram-negative bacteria.
Multidrug-resistant Gram-negative pathogens are an emerging threat to human health, and addressing this challenge will require development of new antibacterial agents. This can be achieved through anExpand
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Selective Targeting of Bromodomains of the Bromodomain-PHD Fingers Family Impairs Osteoclast Differentiation
Histone acetyltransferases of the MYST family are recruited to chromatin by BRPF scaffolding proteins. We explored functional consequences and the therapeutic potential of inhibitors targetingExpand
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Synthesis of Chiral Azabicycles from Pyroglutaminols.
The stereocontrolled synthesis of a range of substituted bicyclic morpholine and piperazine derivatives is reported from substituted pyroglutaminols via an intramolecular SN2 cyclization as the keyExpand
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Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance
PFI-3, a novel inhibitor targeting the bromodomains of essential components of the BAF/PBAF complex, affects the differentiation of ESC and TSC. Mammalian SWI/SNF [also called Brg/Brahma-associatedExpand
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Novel monobactams utilizing a siderophore uptake mechanism for the treatment of gram-negative infections.
Novel siderophore-linked monobactams with in vitro and in vivo anti-microbial activity against MDR Gram-negative pathogens are described.
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