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Crystal structures of the two major aggrecan degrading enzymes, ADAMTS4 and ADAMTS5
Aggrecanases are now believed to be the principal proteinases responsible for aggrecan degradation in osteoarthritis. Given their potential as a drug target, we solved crystal structures of the twoExpand
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(1-(4-(Naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine: a wingless beta-catenin agonist that increases bone formation rate.
A high-throughput screening campaign to discover small molecule leads for the treatment of bone disorders concluded with the discovery of a compound with a 2-aminopyrimidine template that targetedExpand
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Natural products as probes of cell biology: 20 years of didemnin research
The discovery of the didemnin family of marine depsipeptides launched an exciting and intriguing chapter in natural product chemistry. The unusual structure of the didemnin congeners has led toExpand
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Inhibition of protein synthesis by didemnin B: how EF-1alpha mediates inhibition of translocation.
The antineoplastic cyclic depsipeptide didemnin B (DB) inhibits protein synthesis in cells and in vitro. The stage at which DB inhibits protein synthesis in cells is not known, althoughExpand
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Synthesis of New Didemnin B Analogs for Investigations of Structure/Biological Activity Relationships
Modifications were introduced in the side chain of didedemnin B to af- ford several analogs (1f-1j) for biological testing in order to identi- fy the features responsible for the bioactivity of theExpand
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Synthesis and biological evaluation of ((4-keto)-phenoxy)methyl biphenyl-4-sulfonamides: a class of potent aggrecanase-1 inhibitors.
The prevention of aggrecan (a key component of cartilage) cleavage via the inhibition of aggrecanase-1 may provide a unique opportunity to stop the progression of cartilage degradation inExpand
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Inhibition of protein synthesis by didemnins: cell potency and SAR.
Synthetic and naturally occurring didemnins are potent and specific inhibitors of protein synthesis in vitro. Structure-activity analysis indicates a requirement for the intact macrocycle; however,Expand
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Riluzole prodrugs for melanoma and ALS: design, synthesis, and in vitro metabolic profiling.
Riluzole (1) is an approved therapeutic for the treatment of ALS and has also demonstrated anti-melanoma activity in metabotropic glutamate GRM1 positive cell lines, a mouse xenograft assay and humanExpand
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