Zenodo (CERN European Organization for Nuclear Research), Dec 31, 1998
Fluoresc:ent quaternary salts derived from proflavin (PI) harbouring long alkyl chains, organize ... more Fluoresc:ent quaternary salts derived from proflavin (PI) harbouring long alkyl chains, organize into unilamellar bilayer vesicles of diameter ll-18 nm in water and form mixed liposomes with egg lecithin lipids. The DNA binding capability of Pf-lipids and their liposome preparations have been demonstrated by fluorescence spectroscopic studies.
Proceedings of the National Academy of Sciences of the United States of America, Mar 3, 1998
The in vitro selection for an intramolecular AUG-cleaving hammerhead-like ribozyme is described. ... more The in vitro selection for an intramolecular AUG-cleaving hammerhead-like ribozyme is described. One of the ribozymes selected was found to cleave after this triplet, both intramolecularly and intermolecularly, with rates comparable to the rate of the native GUC-cleaving hammerhead ribozyme. Although the selection was designed for cleavage 3 of the AUG triplet, the ribozyme also cleaves 3 of the AUA triplet. AUU and AUC triplets are, however, not cleaved, and thus the selected ribozyme is purine-specific for the third position in the triplet. In addition, cleavage 3 of the AAG triplet has been observed, thus the central U is not essential. Nuclease digestion indicates that the selected ribozyme has a secondary structure similar to that of the native hammerhead ribozyme, although with an altered core and stem-loop II sequence. All nucleotides in the core, except one, are essential for activity. The nucleotides in loop II are sensitive to changes and cannot, as in the hammerhead ribozyme, be replaced by other sequences or a nonnucleotide linker. Thus there are differences between these two ribozymes even though they have similar two-dimensional structures. The new ribozyme enlarges the application of hammerhead ribozymes for the inhibition of gene expression by extending the range of cleavable triplets.
Neuropsychiatric Disease and Treatment, Apr 1, 2010
Restless legs syndrome (RLS) is a sleep-related movement disorder commonly involving an unpleasan... more Restless legs syndrome (RLS) is a sleep-related movement disorder commonly involving an unpleasant urge to move the limbs, typically the legs. Dopaminergic agents represent the first-line therapy for RLS; however, long-term use of such drugs results in worsening symptoms due to "augmentation" or other adverse events. Gabapentin, an analog of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), is an anticonvulsant/analgesic agent. Gabapentin is only mildly effective in relieving RLS symptoms, perhaps a result of its poor absorption from the gastrointestinal (GI) tract. Gabapentin enacarbil is a prodrug of gabapentin specifically designed to enhance absorption via the GI tract, and hence provide improved circulating levels of gabapentin on metabolism. Clinical trials to date have demonstrated favorable safety and (compared to traditional gabapentin) improved pharmacokinetics and efficacy in treating RLS symptoms. Thus, gabapentin enacarbil may prove to be a useful drug in treating RLS. An application of gabapentin enacarbil for treatment of RLS is currently pending with FDA for approval.
ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was e... more ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
ABSTRACT Δ-Ala peptides are formed in good yields on treatment of the corresponding serine precur... more ABSTRACT Δ-Ala peptides are formed in good yields on treatment of the corresponding serine precursors with oxalyl chloride and triethylamine in methylene chloride at 0 °C.
Abstract: Restless legs syndrome (RLS) is a sleep-related movement disorder commonly involving an... more Abstract: Restless legs syndrome (RLS) is a sleep-related movement disorder commonly involving an unpleasant urge to move the limbs, typically the legs. Dopaminergic agents rep-resent the first-line therapy for RLS; however, long-term use of such drugs results in worsen-ing symptoms due to “augmentation ” or other adverse events. Gabapentin, an analog of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), is an anticonvulsant/analgesic agent. Gabapentin is only mildly effective in relieving RLS symptoms, perhaps a result of its poor absorption from the gastrointestinal (GI) tract. Gabapentin enacarbil is a prodrug of gabapentin specifically designed to enhance absorption via the GI tract, and hence provide improved circulating levels of gabapentin on metabolism. Clinical trials to date have demon-strated favorable safety and (compared to traditional gabapentin) improved pharmacokinetics and efficacy in treating RLS symptoms. Thus, gabapentin enacarbil may prove to be a u...
Zenodo (CERN European Organization for Nuclear Research), Dec 31, 1998
Fluoresc:ent quaternary salts derived from proflavin (PI) harbouring long alkyl chains, organize ... more Fluoresc:ent quaternary salts derived from proflavin (PI) harbouring long alkyl chains, organize into unilamellar bilayer vesicles of diameter ll-18 nm in water and form mixed liposomes with egg lecithin lipids. The DNA binding capability of Pf-lipids and their liposome preparations have been demonstrated by fluorescence spectroscopic studies.
Proceedings of the National Academy of Sciences of the United States of America, Mar 3, 1998
The in vitro selection for an intramolecular AUG-cleaving hammerhead-like ribozyme is described. ... more The in vitro selection for an intramolecular AUG-cleaving hammerhead-like ribozyme is described. One of the ribozymes selected was found to cleave after this triplet, both intramolecularly and intermolecularly, with rates comparable to the rate of the native GUC-cleaving hammerhead ribozyme. Although the selection was designed for cleavage 3 of the AUG triplet, the ribozyme also cleaves 3 of the AUA triplet. AUU and AUC triplets are, however, not cleaved, and thus the selected ribozyme is purine-specific for the third position in the triplet. In addition, cleavage 3 of the AAG triplet has been observed, thus the central U is not essential. Nuclease digestion indicates that the selected ribozyme has a secondary structure similar to that of the native hammerhead ribozyme, although with an altered core and stem-loop II sequence. All nucleotides in the core, except one, are essential for activity. The nucleotides in loop II are sensitive to changes and cannot, as in the hammerhead ribozyme, be replaced by other sequences or a nonnucleotide linker. Thus there are differences between these two ribozymes even though they have similar two-dimensional structures. The new ribozyme enlarges the application of hammerhead ribozymes for the inhibition of gene expression by extending the range of cleavable triplets.
Neuropsychiatric Disease and Treatment, Apr 1, 2010
Restless legs syndrome (RLS) is a sleep-related movement disorder commonly involving an unpleasan... more Restless legs syndrome (RLS) is a sleep-related movement disorder commonly involving an unpleasant urge to move the limbs, typically the legs. Dopaminergic agents represent the first-line therapy for RLS; however, long-term use of such drugs results in worsening symptoms due to "augmentation" or other adverse events. Gabapentin, an analog of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), is an anticonvulsant/analgesic agent. Gabapentin is only mildly effective in relieving RLS symptoms, perhaps a result of its poor absorption from the gastrointestinal (GI) tract. Gabapentin enacarbil is a prodrug of gabapentin specifically designed to enhance absorption via the GI tract, and hence provide improved circulating levels of gabapentin on metabolism. Clinical trials to date have demonstrated favorable safety and (compared to traditional gabapentin) improved pharmacokinetics and efficacy in treating RLS symptoms. Thus, gabapentin enacarbil may prove to be a useful drug in treating RLS. An application of gabapentin enacarbil for treatment of RLS is currently pending with FDA for approval.
ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was e... more ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
ABSTRACT Δ-Ala peptides are formed in good yields on treatment of the corresponding serine precur... more ABSTRACT Δ-Ala peptides are formed in good yields on treatment of the corresponding serine precursors with oxalyl chloride and triethylamine in methylene chloride at 0 °C.
Abstract: Restless legs syndrome (RLS) is a sleep-related movement disorder commonly involving an... more Abstract: Restless legs syndrome (RLS) is a sleep-related movement disorder commonly involving an unpleasant urge to move the limbs, typically the legs. Dopaminergic agents rep-resent the first-line therapy for RLS; however, long-term use of such drugs results in worsen-ing symptoms due to “augmentation ” or other adverse events. Gabapentin, an analog of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), is an anticonvulsant/analgesic agent. Gabapentin is only mildly effective in relieving RLS symptoms, perhaps a result of its poor absorption from the gastrointestinal (GI) tract. Gabapentin enacarbil is a prodrug of gabapentin specifically designed to enhance absorption via the GI tract, and hence provide improved circulating levels of gabapentin on metabolism. Clinical trials to date have demon-strated favorable safety and (compared to traditional gabapentin) improved pharmacokinetics and efficacy in treating RLS symptoms. Thus, gabapentin enacarbil may prove to be a u...
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