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Inhibition of DNA methylation and reactivation of silenced genes by zebularine.
TLDR
Zebularine is a stable DNA demethylating agent and the first drug in its class able to reactivate an epigenetically silenced gene by oral administration. Expand
Structural basis of actin recognition and arginine ADP-ribosylation by Clostridium perfringens ι-toxin
TLDR
The crystal structure of actin-Ia in complex with the nonhydrolyzable NAD analog βTAD suggests a common reaction mechanism for ADPRTs and might be of use in rational drug design to block toxin-substrate recognition. Expand
Exotoxin A–eEF2 complex structure indicates ADP ribosylation by ribosome mimicry
TLDR
Four structures of a catalytically active complex between a fragment of Pseudomonas aeruginosa exotoxin A and its protein substrate, translation elongation factor 2 (eEF2), which suggest the requirement of diphthamide for ADP ribosylation for diphtheria toxin may be explained. Expand
2-Substitution of adenine nucleotide analogues containing a bicyclo[3.1.0]hexane ring system locked in a northern conformation: enhanced potency as P2Y1 receptor antagonists.
TLDR
The most potent molecule at the hP2Y(1) receptor was an (N)-methanocarba N(6)-methyl-2-iodo analogue 12, which displayed a K(i) value in competition for binding of [(3)H]5 of 0.79 nM and aK(B) value of 1.74 nM for inhibition of PLC. Expand
Metabolic activation of zebularine, a novel DNA methylation inhibitor, in human bladder carcinoma cells.
TLDR
The complex metabolism of Zeb and its limited DNA incorporation suggest that these are the reasons why it is less potent than either 5-azacytidine or 5-aza-2'-deoxycytidine and requires higher doses for equivalent inhibition of DNMT. Expand
Epigenetic therapy with 3-deazaneplanocin A, an inhibitor of the histone methyltransferase EZH2, inhibits growth of non-small cell lung cancer cells.
TLDR
The results indicated that an epigenetic therapy that pharmacologically targets EZH2 via DZNep may constitute a novel approach to treatment of NSCLCs. Expand
3-Deazaneplanocin: a new and potent inhibitor of S-adenosylhomocysteine hydrolase and its effects on human promyelocytic leukemia cell line HL-60.
TLDR
3-deazaneplanocin may have therapeutic potential as an anticancer or antiviral drug and be competitive with the substrate adenosine. Expand
The Lipophilicity of Phorbol Esters as a Critical Factor in Determining the Pattern of Translocation of Protein Kinase C δ Fused to Green Fluorescent Protein*
TLDR
The results indicate that lipophilicity of phorbol esters is a critical factor contributing to differential PKC δ localization and thereby potentially to their different biological activities. Expand
Zebularine: A Unique Molecule for an Epigenetically Based Strategy in Cancer Chemotherapy
TLDR
The increased electrophilic character of its simple aglycon endows the molecule with unique biologic properties as a potent inhibitor of both cytidine deaminase and DNA cytosine methyltransferase, making zebularine a promising antitumor agent that shows activity both in vitro and in experimental animals. Expand
Host immune defense peptide LL-37 activates caspase-independent apoptosis and suppresses colon cancer.
TLDR
It is reported that LL-37 activates a p53-mediated, caspase-independent apoptotic cascade that contributes to suppression of colon cancer and triggers AIF/EndoG-mediated apoptosis in colon cancer cells. Expand
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