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BRD4 is an atypical kinase that phosphorylates Serine2 of the RNA Polymerase II carboxy-terminal domain
The bromodomain protein, BRD4, has been identified recently as a therapeutic target in acute myeloid leukemia, multiple myeloma, Burkitt’s lymphoma, NUT midline carcinoma, colon cancer, andExpand
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Synthetic GPI as a candidate anti-toxic vaccine in a model of malaria
The malaria parasite Plasmodium falciparum infects 5–10% of the world's population and kills two million people annually. Fatalities are thought to result in part from pathological reactionsExpand
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Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains.
The biological role played by non-BET bromodomains remains poorly understood, and it is therefore imperative to identify potent and highly selective inhibitors to effectively explore the biology ofExpand
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The kinetic isotope effect in the search for deuterated drugs.
The kinetic isotope effect has long been exploited by physical organic chemists to study reaction mechanisms due to its effect on reaction rates when cleavage of a C-isotope bond is rate determining.Expand
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Pharmacological evaluation of a novel phosphodiesterase 10A inhibitor in models of antipsychotic activity and cognition
In this study, we report the pharmacological effects of a novel PDE10A inhibitor, SEP-39. SEP-39 is a potent (1.0nM) inhibitor of human PDE10A in vitro, with good selectivity (>16000-fold) againstExpand
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GNE-886: A Potent and Selective Inhibitor of the Cat Eye Syndrome Chromosome Region Candidate 2 Bromodomain (CECR2).
The biological function of bromodomains, epigenetic readers of acetylated lysine residues, remains largely unknown. Herein we report our efforts to discover a potent and selective inhibitor of theExpand
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Inhibition of bromodomain-containing protein 9 for the prevention of epigenetically-defined drug resistance.
Bromodomain-containing protein 9 (BRD9), an epigenetic "reader" of acetylated lysines on post-translationally modified histone proteins, is upregulated in multiple cancer cell lines. To assess theExpand
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Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials.
In recent years, inhibition of the interaction between the bromodomain and extra-terminal domain (BET) family of chromatin adaptors and acetyl-lysine residues on chromatin has emerged as a promisingExpand
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Rapid synthesis of a glycosylphosphatidylinositol-based malaria vaccine using automated solid-phase oligosaccharide synthesis.
Described is an automated synthesis of hexasaccharide malarial toxin 1, currently under development as a malaria vaccine candidate. Using a combination of automated solid-phase methods andExpand
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