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Small-molecule activation of procaspase-3 to caspase-3 as a personalized anticancer strategy
Mutation and aberrant expression of apoptotic proteins are hallmarks of cancer. These changes prevent proapoptotic signals from being transmitted to executioner caspases, thereby averting apoptoticExpand
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PAC-1 activates procaspase-3 in vitro through relief of zinc-mediated inhibition.
The direct induction of apoptosis has emerged as a powerful anticancer strategy, and small molecules that either inhibit or activate certain proteins in the apoptotic pathway have great potential asExpand
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DNA as a target for anticancer compounds: methods to determine the mode of binding and the mechanism of action.
Small molecules that bind to DNA are extremely useful as biochemical tools for the visualization of DNA both in vitro and inside the cell. Additionally, the clinical significance of DNA-bindingExpand
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Poly(ADP-ribose) makes a date with death.
Poly(ADP-ribose) polymerase (PARP) enzymes catalyze the conversion of NAD(+) to polymers of poly(ADP-ribose) (PAR). Although its role in the DNA-damage response has long been recognized, recent workExpand
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Glucose conjugation for the specific targeting and treatment of cancer.
Cancers of diverse origins exhibit marked glucose avidity and high rates of aerobic glycolysis. Increased understanding of this dysfunctional metabolism known as the Warburg effect has led to anExpand
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Discovery of N-hydroxyindole-based inhibitors of human lactate dehydrogenase isoform A (LDH-A) as starvation agents against cancer cells.
Highly invasive tumor cells are characterized by a metabolic switch, known as the Warburg effect, from "normal" oxidative phosphorylation to increased glycolysis even under sufficiently oxygenatedExpand
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Dissecting glucose signalling with diversity-oriented synthesis and small-molecule microarrays
Small molecules that alter protein function provide a means to modulate biological networks with temporal resolution. Here we demonstrate a potentially general and scalable method of identifying suchExpand
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Predictive compound accumulation rules yield a broad-spectrum antibiotic
Most small molecules are unable to rapidly traverse the outer membrane of Gram-negative bacteria and accumulate inside these cells, making the discovery of much-needed drugs against these pathogensExpand
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Targeting RNA with small molecules.
5.1. Binding Sites of the Aminoglycosides 1185 5.2. Importance of Electrostatic Interactions 1185 5.3. Nonionic Interactions 1185 5.4. Pseudo-Base Pair Interactions 1186 5.5. Water-Mediated ContactsExpand
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Artificial activation of toxin-antitoxin systems as an antibacterial strategy.
Toxin-antitoxin (TA) systems are unique modules that effect plasmid stabilization via post-segregational killing of the bacterial host. The genes encoding TA systems also exist on bacterialExpand
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