The Experts below are selected from a list of 747 Experts worldwide ranked by ideXlab platform
Sungkee Chung - One of the best experts on this subject based on the ideXlab platform.
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A guanidine-appended scyllo-Inositol Derivative AAD-66 enhances brain delivery and ameliorates Alzheimer's phenotypes
Scientific reports, 2017Co-Authors: Dohyun Lee, Kyongtai Kim, Woo-sirl Lee, Sungsu Lim, Yun Kyung Kim, Hoe-yune Jung, Sanket Das, Juhyun Lee, Wenjie Luo, Sungkee ChungAbstract:Alzheimer’s disease (AD) is a degenerative brain disease that destroys memory and other important mental functions but lacks efficient therapeutic agents. Blocking toxic amyloid β (Aβ) could be beneficial for AD and represents a promising therapeutic strategy for AD treatment. scyllo-Inositol (SI) is a potential therapeutic for AD by directly interacting with the Aβ peptide to inhibit Aβ42 fiber formation. Clinical studies of SI showed promising benefits on mild to moderate AD, however, with limitations on dosage regime. A new strategy to enhance the brain delivery of SI is needed to achieve the efficacy with minimum adverse effects. Herein, we report that a novel guanidine-appended SI Derivative AAD-66 resulted in more effective reductions of brain Aβ and plaque deposits, gliosis, and behavioral memory deficits in the disease-established 5xFAD mice. Overall, our present study reveals the potential of AAD-66 as a promising therapeutic agent for AD.
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A guanidine-appended scyllo-Inositol Derivative AAD-66 enhances brain delivery and ameliorates Alzheimer’s phenotypes
Nature Publishing Group, 2017Co-Authors: Dohyun Lee, Kyongtai Kim, Woo-sirl Lee, Sungsu Lim, Yun Kyung Kim, Hoe-yune Jung, Sanket Das, Juhyun Lee, Wenjie Luo, Sungkee ChungAbstract:Abstract Alzheimer’s disease (AD) is a degenerative brain disease that destroys memory and other important mental functions but lacks efficient therapeutic agents. Blocking toxic amyloid β (Aβ) could be beneficial for AD and represents a promising therapeutic strategy for AD treatment. scyllo-Inositol (SI) is a potential therapeutic for AD by directly interacting with the Aβ peptide to inhibit Aβ42 fiber formation. Clinical studies of SI showed promising benefits on mild to moderate AD, however, with limitations on dosage regime. A new strategy to enhance the brain delivery of SI is needed to achieve the efficacy with minimum adverse effects. Herein, we report that a novel guanidine-appended SI Derivative AAD-66 resulted in more effective reductions of brain Aβ and plaque deposits, gliosis, and behavioral memory deficits in the disease-established 5xFAD mice. Overall, our present study reveals the potential of AAD-66 as a promising therapeutic agent for AD
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syntheses of d and l myo Inositol 1 2 4 5 tetrakisphosphate and stereoselectivity of the i 1 4 5 p3 receptor binding
Bioorganic & Medicinal Chemistry Letters, 1998Co-Authors: Sungkee Chung, Boogyo Shin, Youngtae Chang, Byungchang Suh, Kyongtai KimAbstract:D- and L-myo-Inositol 1,2,4,5-tetrakisphosphate [D- & L-I(1,2,4,5)P4], which are analogues of D-myo-Inositol 1,4,5-trisphosphate [D-I(1,4,5)P3], a calcium mobilizing second messenger, were synthesized via resolution of the camphanate ester of a myo-Inositol Derivative, and the binding affinities to I(1,4,5)P3 receptor were measured.
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synthesis of l chiro Inositol 1 2 3 trisphosphate and 1 2 3 5 tetrakisphosphate by ferrier reaction of methyl α d mannopyranoside
Bioorganic & Medicinal Chemistry Letters, 1996Co-Authors: Sungkee ChungAbstract:Abstract The Ferrier rearrangement of a methyl α- d -mannopyranoside Derivative (8a), followed by a stereoselective reduction gave a l -chiro- Inositol Derivative (2), which was converted to l -chiro- Inositol 1,2,3-trisphosphate (3) and l -chiro- Inositol 1,2,3,5-tetrakisphosphate (4). Compounds 3 and 4 may be considered to be the C3-position stereoisomers of d -myo- Inositol 1,2,6-trisphosphate (α-trInositol) and d -myo- Inositol 1,3,4,5-tetrakisphosphate, respectively, and should be useful for the binding studies with their macromolecular counterparts.
Kyongtai Kim - One of the best experts on this subject based on the ideXlab platform.
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A guanidine-appended scyllo-Inositol Derivative AAD-66 enhances brain delivery and ameliorates Alzheimer's phenotypes
Scientific reports, 2017Co-Authors: Dohyun Lee, Kyongtai Kim, Woo-sirl Lee, Sungsu Lim, Yun Kyung Kim, Hoe-yune Jung, Sanket Das, Juhyun Lee, Wenjie Luo, Sungkee ChungAbstract:Alzheimer’s disease (AD) is a degenerative brain disease that destroys memory and other important mental functions but lacks efficient therapeutic agents. Blocking toxic amyloid β (Aβ) could be beneficial for AD and represents a promising therapeutic strategy for AD treatment. scyllo-Inositol (SI) is a potential therapeutic for AD by directly interacting with the Aβ peptide to inhibit Aβ42 fiber formation. Clinical studies of SI showed promising benefits on mild to moderate AD, however, with limitations on dosage regime. A new strategy to enhance the brain delivery of SI is needed to achieve the efficacy with minimum adverse effects. Herein, we report that a novel guanidine-appended SI Derivative AAD-66 resulted in more effective reductions of brain Aβ and plaque deposits, gliosis, and behavioral memory deficits in the disease-established 5xFAD mice. Overall, our present study reveals the potential of AAD-66 as a promising therapeutic agent for AD.
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A guanidine-appended scyllo-Inositol Derivative AAD-66 enhances brain delivery and ameliorates Alzheimer’s phenotypes
Nature Publishing Group, 2017Co-Authors: Dohyun Lee, Kyongtai Kim, Woo-sirl Lee, Sungsu Lim, Yun Kyung Kim, Hoe-yune Jung, Sanket Das, Juhyun Lee, Wenjie Luo, Sungkee ChungAbstract:Abstract Alzheimer’s disease (AD) is a degenerative brain disease that destroys memory and other important mental functions but lacks efficient therapeutic agents. Blocking toxic amyloid β (Aβ) could be beneficial for AD and represents a promising therapeutic strategy for AD treatment. scyllo-Inositol (SI) is a potential therapeutic for AD by directly interacting with the Aβ peptide to inhibit Aβ42 fiber formation. Clinical studies of SI showed promising benefits on mild to moderate AD, however, with limitations on dosage regime. A new strategy to enhance the brain delivery of SI is needed to achieve the efficacy with minimum adverse effects. Herein, we report that a novel guanidine-appended SI Derivative AAD-66 resulted in more effective reductions of brain Aβ and plaque deposits, gliosis, and behavioral memory deficits in the disease-established 5xFAD mice. Overall, our present study reveals the potential of AAD-66 as a promising therapeutic agent for AD
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syntheses of d and l myo Inositol 1 2 4 5 tetrakisphosphate and stereoselectivity of the i 1 4 5 p3 receptor binding
Bioorganic & Medicinal Chemistry Letters, 1998Co-Authors: Sungkee Chung, Boogyo Shin, Youngtae Chang, Byungchang Suh, Kyongtai KimAbstract:D- and L-myo-Inositol 1,2,4,5-tetrakisphosphate [D- & L-I(1,2,4,5)P4], which are analogues of D-myo-Inositol 1,4,5-trisphosphate [D-I(1,4,5)P3], a calcium mobilizing second messenger, were synthesized via resolution of the camphanate ester of a myo-Inositol Derivative, and the binding affinities to I(1,4,5)P3 receptor were measured.
Reinhard Hensel - One of the best experts on this subject based on the ideXlab platform.
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di myo Inositol 1 1 phosphate a new Inositol phosphate isolated from pyrococcus woesei
FEBS Letters, 1992Co-Authors: Stefan Scholz, Johann Sonnenbichler, Wolfram Schäfer, Reinhard HenselAbstract:Abstract A new Inositol Derivative could be isolated from the Archaeum Pyrococcus woesei and identified as di-myo-Inositol-1,1′-phosphate by 1H, 31P NMR spectroscopy, mass spectrometry and thin layer chromatograpy. In P. woesel, this Inositol phosphate represents the dominant counterion of K+ which ranges from 500 to 600 mM. The role of the potassium salt of di-myo-Inositol-1,1′-phosphate as thermostabilizer is discussed.
Yutaka Watanabe - One of the best experts on this subject based on the ideXlab platform.
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diastereomixture and racemate of myo Inositol Derivatives stronger organogelators than the corresponding homochiral isomers
Organic Letters, 2004Co-Authors: Yutaka Watanabe, Tomomi Miyasou, Minoru HayashiAbstract:Contrary to the usually accepted phenomena, an optically heterogeneous 1:1 diastereomixture of DS and LS and a racemate of LS and DR obtained, respectively, from a racemic myo-Inositol Derivative and (S)- and racemic O-acetylmandelic acid formed stronger organogels, especially with aromatic fluids, than those formed from homochiral isomers, DS and LS. One of the plausible reasons for the formation of the stronger diastereomeric gel is shown to be the complementary interaction of two diastereomers.
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regioselective phosphorylation of vicinal 3 4 hydroxy myo Inositol Derivative promoted practical synthesis of d ptdins 4 5 p2 and d ins 1 4 5 p3
ChemInform, 2003Co-Authors: Fushe Han, Minoru Hayashi, Yutaka WatanabeAbstract:Abstract The reactivity of 3 and 4-OH in 3,4-diol myo -Inositol Derivatives were observed through the phosphorylation, acylation and silylation. The results indicated that 3-OH is much more reactive than 4-OH, giving regiospecifically 3-mono-functionalized products. This investigation provided a concise methodology for the synthesis of natural d -form of PtdIns(4,5)P2 and d -Ins(1,4,5)P3 from l -1,2- O -cyclohexylidene-3,4- O -(tetraisopropyl disiloxane-1,3-diyl)- myo -Inositol.
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a short synthesis of dipalmitoylphosphatidylInositol 4 5 bisphosphate via 3 o selective phosphorylation of a 3 4 free Inositol Derivative
ChemInform, 2003Co-Authors: Fushe Han, Minoru Hayashi, Yutaka WatanabeAbstract:DipalmitoylphosphatidylInositol 4,5-bisphosphate was conveniently synthesized via the regioselective phosphorylation of L-1,2-O-cyclohexylidene-5,6-di-O-(o-xylylene phosphoryl)-myo-Inositol derived from 1,2-O-cyclohexylidene-3,4-O-(tetraisopropyldisiloxane-1,3-diyl)-myo-Inositol.
Stefan Scholz - One of the best experts on this subject based on the ideXlab platform.
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di myo Inositol 1 1 phosphate a new Inositol phosphate isolated from pyrococcus woesei
FEBS Letters, 1992Co-Authors: Stefan Scholz, Johann Sonnenbichler, Wolfram Schäfer, Reinhard HenselAbstract:Abstract A new Inositol Derivative could be isolated from the Archaeum Pyrococcus woesei and identified as di-myo-Inositol-1,1′-phosphate by 1H, 31P NMR spectroscopy, mass spectrometry and thin layer chromatograpy. In P. woesel, this Inositol phosphate represents the dominant counterion of K+ which ranges from 500 to 600 mM. The role of the potassium salt of di-myo-Inositol-1,1′-phosphate as thermostabilizer is discussed.