- Shape selective recognition of T·A base pairs by hairpin polyamides containing N-terminal 3-methoxy (and 3-Chloro) thiophene residues
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Hairpin polyamides selectively recognize predetermined DNA sequences with affinities comparable to naturally occurring proteins. Internal side-by-side pairs of unsymmetrical aromatic rings within the minor groove of DNA distinguish each of the four Watson-Crick base pairs. In contrast, N-terminal ring pairs exhibit less specificity, with the exception of Im/Py targeting G·C base pairs. In an effort to explore the sequence specificity of new ring pairs, a series of hairpin polyamides containing 3-substituted-thiophene-2-carboxamide residues at the N-terminus was synthesized. An N-terminal 3-methoxy (or 3-chloro) thiophene residue paired opposite Py displayed 6- (and 3-) fold selectivity for T·A relative to A·T base pair, while disfavoring G,C base pairs by >200-fold. Our data suggests shape selective recognition with projection of the 3-thiophene substituent (methoxy or chloro) to the floor of the minor groove.
- Foister, Shane,Marques, Michael A.,Doss, Raymond M.,Dervan, Peter B.
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Read Online
- Discovery of potent vascular endothelial growth factor receptor-2 inhibitors
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Substantial evidence over the last decades has implicated uncontrolled angiogenesis with various pathological states, including cancer. Vascular endothelial growth factor (VEGF) plays a critical role in its regulation. Because the tyrosine kinase VEGF rec
- Papakyriakou, Athanasios,Katsarou, Maria E.,Belimezi, Maria,Karpusas, Michael,Vourloumis, Dionisios
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experimental part
p. 118 - 129
(2010/11/02)
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- DNA-BINDING POLYMERS
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Methods and compositions are provided for forming complexes between dsDNA and novel DNA-binding polymers comprising N-terminal thiophene-containing moieties which exhibit selectivity for T-A base pairs. By appropriate choice of target sequences and DNA-binding polymers, complexes comprising polymer-DNA are obtained with high association constants. The formation of complexes can be used for identification of specific dsDNA sequences, for inhibiting gene transcription, and as a therapeutic for inhibiting proliferation of undesired cells or modulation of expression of specific genes.
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Page/Page column 15-16
(2009/07/03)
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- DNA-binding polymers
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Methods and compositions are provided for forming complexes between dsDNA and novel DNA-binding polymers comprising N-terminal thiophene-containing moieties which exhibit selectivity for T-A base pairs. By appropriate choice of target sequences and DNA-binding polymers, complexes comprising polymer-DNA are obtained with high association constants. The formation of complexes can be used for identification of specific dsDNA sequences, for inhibiting gene transcription, and as a therapeutic for inhibiting proliferation of undesired cells or modulation of expression of specific genes.
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- 2-AMINOTHIOPHENECARBOXAMIDES USEFUL AS CANCER CHEMOTHERAPEUTIC AGENTS
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This invention relates to novel 2-aminothiophenecarboxamide compounds, pharmaceutical compositions containing such compounds, and the use of those compounds or compositions as cancer chemotherapeutic agents.
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Page/Page column 34
(2010/10/20)
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- Substituted alkylamine derivatives and methods of use
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Selected heterocyclic compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
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- Substituted alkylamine derivatives and methods of use
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Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
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- Thieno pyrazine diones, their preparation and use
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Novel thieno[2,3-b]pyrazine-2,3(1H,3H)-diones or tautomeric forms thereof of the formula (I) STR1 The compounds are useful in the treatment of neurological and psychiatric diseases.
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