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A three-hybrid approach to scanning the proteome for targets of small molecule kinase inhibitors.
The Y3H system described here may prove generally useful in the discovery of candidate drug targets in scanning the proteome for targets of kinase inhibitors. Expand
A proteome-wide CDK/CRK-specific kinase inhibitor promotes tumor cell death in the absence of cell cycle progression.
A small-molecule kinase inhibitor is described, which, besides inhibiting tumor cell cycle progression, exhibits potent cytotoxic activity toward noncycling tumor cells, but not nontransformed quiescent fibroblasts. Expand
Antifungal activity of a Candida albicans GGTase I inhibitor-alanine conjugate. Inhibition of Rho1p prenylation in C. albicans.
An alanine conjugate of a Candida albicans geranylgeranyl transferase I inhibitor was synthesized to facilitate its uptake into the fungal cell. The antifungal activity of CaGGTase-Ala conjugate isExpand
Formation of DNA-protein cross-links in mammalian cells by levuglandin E2.
The results suggest that LG adducts to DNA or protein are not repaired, but react further at sites on protein or DNA in close proximity to the initial adduction, forming cross-links in a slow phase of the process. Expand
MASPIT: three-hybrid trap for quantitative proteome fingerprinting of small molecule-protein interactions in mammalian cells.
During the course of this study, the pyrido[2,3-d]pyrimidine PD173955, a known SRC kinase inhibitor, was identified as a potent inhibitor of several ephrin receptor tyrosine kinases, which could perhaps be exploited in the design of inhibitors for this kinase subfamily. Expand
Formation and stability of pyrrole adducts in the reaction of levuglandin E2 with proteins.
The LG-derived protein-bound pyrrole may be a useful marker of oxidative lipid damage, and an immunoassay for this post-translational protein modification can be exploited as a mild, sensitive method for detecting and quantifying the generation of LGs in chronic inflammatory states. Expand
Structure-activity relationship studies of flavopiridol analogues.
Modifications of the 3-hydroxy-1-methylpiperidinyl (D ring) of flavopiridol and their effect on CDK inhibitory activity are reported. Expand
Levuglandin E2 inhibits mitosis and microtubule assembly.
It is shown that exogenous LGE2 enters cells and efficiently inhibits the first synchronous cell division of fertilized sea urchin eggs, attribute this inhibition to covalent modification of tubulin and thereby to inhibition of microtubule assembly. Expand
Total Synthesis of Iso[4]-levuglandin E2
Iso[4]-levuglandin E2 (iso[4]-LGE2, 5-acetyl-6-formyl-9-hydroxy-7(E),11(Z)-heptadecadienoic acid) is a structural isomer of levuglandin E2 (8-acetyl-9-formyl-12-hydroxy-5(Z),10(E)-heptadecadienoicExpand