Are you sure you are not the author of this publication?
Ng, Nickols Jo, Szablowski Ae, Hargrove Bc, Li Jevgenij Raskatov Pb, Dervan
Published in
Molecular Cancer Therapeutics
Pyrrole-imidazole (Py-Im) polyamides are a class of programmable DNA minor groove binders capable of modulating the activity of DNA-binding proteins and affecting changes in gene expression. Estrogen receptor alpha (ERα) is a ligand-activated hormone receptor that binds as a homodimer to estrogen response elements (ERE) and is a driving oncogene in...
Are you sure you are not the author of this publication?
Ng, Nickols Jo, Szablowski Ae, Hargrove Bc, Li Jevgenij Raskatov Pb, Dervan
Published in
Molecular Cancer Therapeutics
Pyrrole-imidazole (Py-Im) polyamides are a class of programmable DNA minor groove binders capable of modulating the activity of DNA-binding proteins and affecting changes in gene expression. Estrogen receptor alpha (ERα) is a ligand-activated hormone receptor that binds as a homodimer to estrogen response elements (ERE) and is a driving oncogene in...
Are you sure you are not the author of this publication?
Ng, Nickols Jo, Szablowski Ae, Hargrove Bc, Li Jevgenij Raskatov Pb, Dervan
Published in
Molecular Cancer Therapeutics
Pyrrole-imidazole (Py-Im) polyamides are a class of programmable DNA minor groove binders capable of modulating the activity of DNA-binding proteins and affecting changes in gene expression. Estrogen receptor alpha (ERα) is a ligand-activated hormone receptor that binds as a homodimer to estrogen response elements (ERE) and is a driving oncogene in...
Are you sure you are not the author of this publication?
Ka, Muzikar Jl, Meier Da, Gubler Jevgenij Raskatov Pb, Dervan
Published in
Organic Letters
A furan amino acid, inspired by the recently discovered proximicin natural products, was incorporated into the scaffold of a DNA-binding hairpin polyamide. While unpaired oligomers of 2,4-disubstituted furan amino acids show poor DNA-binding activity, furan (Fn) carboxamides paired with N-methylpyrrole (Py) and N-methylimidazole (Im) rings demonstr...
Are you sure you are not the author of this publication?
Ka, Muzikar Jl, Meier Da, Gubler Jevgenij Raskatov Pb, Dervan
Published in
Organic Letters
A furan amino acid, inspired by the recently discovered proximicin natural products, was incorporated into the scaffold of a DNA-binding hairpin polyamide. While unpaired oligomers of 2,4-disubstituted furan amino acids show poor DNA-binding activity, furan (Fn) carboxamides paired with N-methylpyrrole (Py) and N-methylimidazole (Im) rings demonstr...
Are you sure you are not the author of this publication?
Ka, Muzikar Jl, Meier Da, Gubler Jevgenij Raskatov Pb, Dervan
Published in
Organic Letters
A furan amino acid, inspired by the recently discovered proximicin natural products, was incorporated into the scaffold of a DNA-binding hairpin polyamide. While unpaired oligomers of 2,4-disubstituted furan amino acids show poor DNA-binding activity, furan (Fn) carboxamides paired with N-methylpyrrole (Py) and N-methylimidazole (Im) rings demonstr...
Are you sure you are not the author of this publication?
Jevgenij Raskatov Jw, Puckett Pb, Dervan
Published in
Bioorganic & Medicinal Chemistry
In an effort to quantitate Py-Im polyamide concentrations in vivo, we synthesized the C-14 radioactively labeled compounds 1-3, and investigated their tumor localization in a subcutaneous xenograft model of prostate cancer (LNCaP). Tumor concentrations were compared with representative host tissues, and exhibited a certain degree of preferential lo...
Are you sure you are not the author of this publication?
Ae, Hargrove Jevgenij Raskatov Jl, Meier Dc, Montgomery Pb, Dervan
Published in
Journal of Medicinal Chemistry
To optimize the biological activity of pyrrole-imidazole polyamide DNA-binding molecules, we characterized the aggregation propensity of these compounds through dynamic light scattering and fractional solubility analysis. Nearly all studied polyamides were found to form measurable particles 50-500 nm in size under biologically relevant conditions, ...
Are you sure you are not the author of this publication?
Jevgenij Raskatov Jo, Szablowski Pb, Dervan
Published in
Journal of Medicinal Chemistry
Subcutaneous xenografts represent a popular approach to evaluate efficacy of prospective molecular therapeutics in vivo. In the present study, the C-14 labeled radioactive pyrrole-imidazole (Py-Im) polyamide 1, targeted to the 5 -WGWWCW-3 DNA sequence, was evaluated with regard to its uptake properties in subcutaneous xenografts, derived from the ...
Are you sure you are not the author of this publication?
Jo, Szablowski Jevgenij Raskatov Pb, Dervan
Published in
Molecular Cancer Therapeutics
Hypoxic gene expression contributes to the pathogenesis of many diseases, including organ fibrosis, age-related macular degeneration, and cancer. Hypoxia-inducible factor-1 (HIF1), a transcription factor central to the hypoxic gene expression, mediates multiple processes including neovascularization, cancer metastasis, and cell survival. Pyrrole-im...
Are you sure you are not the author of this publication?
Jevgenij Raskatov Ae, Hargrove Ay, So Pb, Dervan
Published in
Journal of the American Chemical Society
The pharmacokinetic properties of three pyrrole-imidazole (Py-Im) polyamides of similar size and Py-Im content but different shape were studied in the mouse. Remarkably, hairpin and cyclic oligomers programmed for the same DNA sequence 5 -WGGWWW-3 displayed distinct pharmacokinetic properties. Furthermore, the hairpin 1 and cycle 2 exhibited vastl...
Are you sure you are not the author of this publication?
Jevgenij Raskatov Ng, Nickols Ae, Hargrove Gk, Marinov B, Wold Pb, Dervan
Published in
Proceedings of the National Academy of Sciences
Gene regulation by DNA binding small molecules could have important therapeutic applications. This study reports the investigation of a DNA-binding pyrrole-imidazole polyamide targeted to bind the DNA sequence 5 -WGGWWW-3 with reference to its potency in a subcutaneous xenograft tumor model. The molecule is capable of trafficking to the tumor site...
Are you sure you are not the author of this publication?
E, Kinski P, Marzenell W, Hofer H, Hagen Jevgenij Raskatov Kx, Knaup Em, Zolnhofer K, Meyer A, Mokhir
Published in
Journal of Inorganic Biochemistry
Aminoferrocene-based prodrugs are activated in the presence of cancer-specific amounts of reactive oxygen species, e.g. H2O2, with the formation of products of two types: Fe-containing complexes, which catalyze generation of HO and O2(-), and quinone methides, which alkylate glutathione and inhibit the antioxidative system of the cell. Both process...
Are you sure you are not the author of this publication?
Cj, Warner S, Dutta Ar, Foley Jevgenij Raskatov
Published in
Chemistry - A European Journal
Are you sure you are not the author of this publication?
Ar, Green S, Barbour T, Horn J, Carlos Jevgenij Raskatov Tr, Holman
Published in
Biochemistry
Lipoxins are an important class of lipid mediators that induce the resolution of inflammation and arise from transcellular exchange of arachidonic acid (AA)-derived lipoxygenase products. Human epithelial 15-lipoxygenase-2 (h15-LOX-2), the major lipoxygenase in macrophages, has exhibited strict regiospecificity, catalyzing only the hydroperoxidatio...
Are you sure you are not the author of this publication?
Jo, Szablowski Jevgenij Raskatov Pb, Dervan
Published in
Molecular Cancer Therapeutics
Hypoxic gene expression contributes to the pathogenesis of many diseases, including organ fibrosis, age-related macular degeneration, and cancer. Hypoxia-inducible factor-1 (HIF1), a transcription factor central to the hypoxic gene expression, mediates multiple processes including neovascularization, cancer metastasis, and cell survival. Pyrrole-im...
Are you sure you are not the author of this publication?
Jo, Szablowski Jevgenij Raskatov Pb, Dervan
Published in
Molecular Cancer Therapeutics
Hypoxic gene expression contributes to the pathogenesis of many diseases, including organ fibrosis, age-related macular degeneration, and cancer. Hypoxia-inducible factor-1 (HIF1), a transcription factor central to the hypoxic gene expression, mediates multiple processes including neovascularization, cancer metastasis, and cell survival. Pyrrole-im...
Are you sure you are not the author of this publication?
Jevgenij Raskatov Ng, Nickols Ae, Hargrove Gk, Marinov B, Wold Pb, Dervan
Published in
Proceedings of the National Academy of Sciences
Gene regulation by DNA binding small molecules could have important therapeutic applications. This study reports the investigation of a DNA-binding pyrrole-imidazole polyamide targeted to bind the DNA sequence 5 -WGGWWW-3 with reference to its potency in a subcutaneous xenograft tumor model. The molecule is capable of trafficking to the tumor site...
Are you sure you are not the author of this publication?
E, Kinski P, Marzenell W, Hofer H, Hagen Jevgenij Raskatov Kx, Knaup Em, Zolnhofer K, Meyer A, Mokhir
Published in
Journal of Inorganic Biochemistry
Aminoferrocene-based prodrugs are activated in the presence of cancer-specific amounts of reactive oxygen species, e.g. H2O2, with the formation of products of two types: Fe-containing complexes, which catalyze generation of HO and O2(-), and quinone methides, which alkylate glutathione and inhibit the antioxidative system of the cell. Both process...
Are you sure you are not the author of this publication?
Cj, Schulze Ms, Donia Jl, Siqueira-Neto D, Ray Jevgenij Raskatov Re, Green Jh, Mckerrow Ma, Fischbach Rg, Linington
Published in
ACS Chemical Biology
Marine natural products are an important source of lead compounds against many pathogenic targets. Herein, we report the discovery of lobosamides A-C from a marine actinobacterium, Micromonospora sp., representing three new members of a small but growing family of bacterially produced polyene macrolactams. The lobosamides display growth inhibitory ...