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Clinical targeting of HIV capsid protein with a long-acting small molecule
TLDR
The small molecule GS-6207, which disrupts the function of the HIV capsid protein, shows potential as a long-acting therapeutic agent for the treatment and prevention of HIV infection.
Structural, Biochemical, and Biophysical Characterization of Idelalisib Binding to Phosphoinositide 3-Kinase δ*
TLDR
The data show that idelalisib is a potent and selective inhibitor of the kinase activity of PI3Kδ, and a crystal structure of idELalisib bound to the p110δ subunit ofPI3K δ furthers the understanding of the binding interactions that confer the potency and selectivity of the compound.
Discovery of Orally Efficacious Phosphoinositide 3-Kinase δ Inhibitors with Improved Metabolic Stability.
TLDR
This work led to the discovery of 35, a highly selective inhibitor of PI3Kδ which displays an excellent pharmacokinetic profile and is efficacious in a rodent model of rheumatoid arthritis.
Discovery of a Phosphoinositide 3-Kinase (PI3K) β/δ Inhibitor for the Treatment of Phosphatase and Tensin Homolog (PTEN) Deficient Tumors: Building PI3Kβ Potency in a PI3Kδ-Selective Template by
TLDR
This work led to the discovery of a highly selective PI3Kβ/δ inhibitor displaying excellent pharmacokinetic profile and efficacy in a human PTEN-deficient LNCaP prostate carcinoma xenograft tumor model.
The characterization of idelalisib binding to PI 3 K δ 1 Structural , biochemical and biophysical characterization of idelalisib binding to phosphoinositide 3-kinase delta *
TLDR
The data show that idelalisib is a potent and selective inhibitor of the kinase activity of PI3Kδ, and several additional biochemical and biophysical assays showed that the compound binds reversibly and non-covalently to the Kinase.
Screening and Identification of a Novel Class of TGF-β Type 1 Receptor Kinase Inhibitor
TLDR
Kinetic analysis revealed that compound 8 inhibited AlK5 via mixed-type inhibition, suggesting that it may bind to ALK5 differently than other published adenosine triphosphate site inhibitors.
2,4,6-Triaminopyrimidine as a Novel Hinge Binder in a Series of PI3Kδ Selective Inhibitors.
TLDR
This medicinal chemistry effort culminated in the identification of 52, a potent and highly selective inhibitor of PI3Kδ that demonstrates efficacy in a rat model of arthritis.
Atropisomerism by Design: Discovery of a Selective and Stable Phosphoinositide 3-Kinase (PI3K) β Inhibitor.
TLDR
A case in which torsional scan studies guided the thoughtful creation of a restricted axis of rotation between two heteroaromatic systems of a phosphoinositide 3-kinase (PI3K) β inhibitor, generating a pair of atropisomeric compounds with significantly different pharmacological and pharmacokinetic profiles.
Optimized High-Throughput Screen for Hepatitis C Virus Translation Inhibitors
TLDR
A high-throughput assay to identify compounds that selectively block translation initiation from the HCV internal ribosome entry site (HCV IRES) found no selective HCVIRES inhibitors but did discover a new scaffold of general translation inhibitor.
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