The Experts below are selected from a list of 21 Experts worldwide ranked by ideXlab platform
Tetsuro Fujita - One of the best experts on this subject based on the ideXlab platform.
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specificity of inhibitors of serine palmitoyltransferase spt a key enzyme in sphingolipid biosynthesis in intact cells a novel evaluation system using an spt defective mammalian cell mutant
Biochemical Pharmacology, 2000Co-Authors: Kentaro Hanada, Masahiro Nishijima, Tetsuro Fujita, Shū KobayashiAbstract:Abstract In the present study, we demonstrate a model cell system for evaluating the specificity of inhibitors of serine palmitoyltransferase (SPT), the enzyme that catalyzes the first step of sphingolipid biosynthesis. The LY-B strain is a Chinese hamster ovary (CHO) cell mutant defective in SPT, and the LY-B/cLCB1 strain is a genetically corrected revertant of the mutant. Although LY-B cells grew only slightly in sphingolipid-deficient medium, their growth was restored to the level of LY-B/cLCB1 cells under sphingosine-supplied conditions, indicating that, in CHO cells, the growth inhibition caused by SPT inactivation was rescued almost fully by the metabolic complementation of sphingolipids. Cultivation of LY-B/cLCB1 cells in sphingolipid-deficient medium in the presence of 10 μM sphingofungin B and ISP-1 (myriocin, Thermozymocidin), potent inhibitors of SPT activity, caused severe growth inhibition with ∼95% inhibition of de novo sphingolipid synthesis. The growth inhibition by sphingofungin B and ISP-1 was rescued substantially by exogenous sphingosine, whereas the cytotoxicity of two other types of SPT inhibitor, l- cycloserine and β-chloro- l- alanine, was hardly rescued. Similar cytotoxic patterns of these inhibitors also were observed on the growth of SPT-defective LY-B cells cultured under sphingosine-supplied conditions. The SPT inhibitors did not affect metabolic conversion of exogenous [ 3 H]sphingosine to complex sphingolipids. Thus, the cytotoxicity of sphingofungin B and ISP-1, but not l -cycloserine or β-chloro- l -alanine, is due largely to inhibition of sphingolipid synthesis by inhibiting the SPT activity.
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potent immunosuppressants 2 alkyl 2 aminopropane 1 3 diols
Journal of Medicinal Chemistry, 1996Co-Authors: Tetsuro Fujita, Ryoji Hirose, Masahiko Yoneta, Shigeo Sasaki, Kenichiro Inoue, Masatoshi Kiuchi, Susumu Hirase, Kenji Chiba, Hiroshi Sakamoto, Masafumi AritaAbstract:Several immunosuppressants, ISP-I [(2S,3R,4R)-(E)-2-amino-3,4-dihydroxy-2-(hydroxymethyl)-14-oxoeicos-6-enoic acid, myriocin = Thermozymocidin] and mycestericins A−G, were isolated from culture bro...
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design synthesis and structure activity relationships of 2 substituted 2 amino 1 3 propanediols discovery of a novel immunosuppressant fty720
Bioorganic & Medicinal Chemistry Letters, 1995Co-Authors: Kunitomo Adachi, Shigeo Sasaki, Kenji Chiba, Masafumi Arita, Toshiyuki Kohara, Noriyoshi Nakao, Tadashi Mishina, Tetsuro FujitaAbstract:FTY720 (2-amino-2-[2-(4-octylphenyl)ethyl]-1,3-propanediol hydrochloride), a novel synthetic immunosuppressant led by modification of ISP-I (myriocin, Thermozymocidin) displayed potent immunosuppressive activity both in vitro and in vivo.
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asymmetric total synthesis of isp i myriocin Thermozymocidin a potent immunosuppressive principle in the isaria sinclairii metabolite
Tetrahedron Letters, 1995Co-Authors: Shigeki Sano, Tetsuro Fujita, Yoshimaro Kobayashi, Tatsuya Kondo, Maki Takebayashi, Shigeki Maruyama, Yoshimitsu NagaoAbstract:Abstract Asymmetric total synthesis of ISP-I has been achieved by utilizing highly selective E -olefin formation based on the Schlosser-modified Wittig reaction and highly diastereoselective aldol reactions employing both chiral heterocyclic derivatives, 3-acetyl-(4 S )-isopropyl-1,3-thiazolidine-2-thione and ethyl [(5 R )-2,5-dihydro-5-isopropyl-3,6-diethoxypyrazin]-2-yl carboxylate.
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asymmetric total synthesis of isp i myriocin Thermozymocidin a potent immunosuppressive principle in the isaria sinclairii metabolite
Tetrahedron Letters, 1995Co-Authors: Shigeki Sano, Tetsuro Fujita, Yoshimaro Kobayashi, Tatsuya Kondo, Maki Takebayashi, Shigeki Maruyama, Yoshimitsu NagaoAbstract:Abstract Asymmetric total synthesis of ISP-I has been achieved by utilizing highly selective E -olefin formation based on the Schlosser-modified Wittig reaction and highly diastereoselective aldol reactions employing both chiral heterocyclic derivatives, 3-acetyl-(4 S )-isopropyl-1,3-thiazolidine-2-thione and ethyl [(5 R )-2,5-dihydro-5-isopropyl-3,6-diethoxypyrazin]-2-yl carboxylate.
Yoshimitsu Nagao - One of the best experts on this subject based on the ideXlab platform.
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asymmetric total synthesis of isp i myriocin Thermozymocidin a potent immunosuppressive principle in the isaria sinclairii metabolite
Tetrahedron Letters, 1995Co-Authors: Shigeki Sano, Tetsuro Fujita, Yoshimaro Kobayashi, Tatsuya Kondo, Maki Takebayashi, Shigeki Maruyama, Yoshimitsu NagaoAbstract:Abstract Asymmetric total synthesis of ISP-I has been achieved by utilizing highly selective E -olefin formation based on the Schlosser-modified Wittig reaction and highly diastereoselective aldol reactions employing both chiral heterocyclic derivatives, 3-acetyl-(4 S )-isopropyl-1,3-thiazolidine-2-thione and ethyl [(5 R )-2,5-dihydro-5-isopropyl-3,6-diethoxypyrazin]-2-yl carboxylate.
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asymmetric total synthesis of isp i myriocin Thermozymocidin a potent immunosuppressive principle in the isaria sinclairii metabolite
Tetrahedron Letters, 1995Co-Authors: Shigeki Sano, Tetsuro Fujita, Yoshimaro Kobayashi, Tatsuya Kondo, Maki Takebayashi, Shigeki Maruyama, Yoshimitsu NagaoAbstract:Abstract Asymmetric total synthesis of ISP-I has been achieved by utilizing highly selective E -olefin formation based on the Schlosser-modified Wittig reaction and highly diastereoselective aldol reactions employing both chiral heterocyclic derivatives, 3-acetyl-(4 S )-isopropyl-1,3-thiazolidine-2-thione and ethyl [(5 R )-2,5-dihydro-5-isopropyl-3,6-diethoxypyrazin]-2-yl carboxylate.
Shigeki Sano - One of the best experts on this subject based on the ideXlab platform.
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asymmetric total synthesis of isp i myriocin Thermozymocidin a potent immunosuppressive principle in the isaria sinclairii metabolite
Tetrahedron Letters, 1995Co-Authors: Shigeki Sano, Tetsuro Fujita, Yoshimaro Kobayashi, Tatsuya Kondo, Maki Takebayashi, Shigeki Maruyama, Yoshimitsu NagaoAbstract:Abstract Asymmetric total synthesis of ISP-I has been achieved by utilizing highly selective E -olefin formation based on the Schlosser-modified Wittig reaction and highly diastereoselective aldol reactions employing both chiral heterocyclic derivatives, 3-acetyl-(4 S )-isopropyl-1,3-thiazolidine-2-thione and ethyl [(5 R )-2,5-dihydro-5-isopropyl-3,6-diethoxypyrazin]-2-yl carboxylate.
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asymmetric total synthesis of isp i myriocin Thermozymocidin a potent immunosuppressive principle in the isaria sinclairii metabolite
Tetrahedron Letters, 1995Co-Authors: Shigeki Sano, Tetsuro Fujita, Yoshimaro Kobayashi, Tatsuya Kondo, Maki Takebayashi, Shigeki Maruyama, Yoshimitsu NagaoAbstract:Abstract Asymmetric total synthesis of ISP-I has been achieved by utilizing highly selective E -olefin formation based on the Schlosser-modified Wittig reaction and highly diastereoselective aldol reactions employing both chiral heterocyclic derivatives, 3-acetyl-(4 S )-isopropyl-1,3-thiazolidine-2-thione and ethyl [(5 R )-2,5-dihydro-5-isopropyl-3,6-diethoxypyrazin]-2-yl carboxylate.
Shigeki Maruyama - One of the best experts on this subject based on the ideXlab platform.
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asymmetric total synthesis of isp i myriocin Thermozymocidin a potent immunosuppressive principle in the isaria sinclairii metabolite
Tetrahedron Letters, 1995Co-Authors: Shigeki Sano, Tetsuro Fujita, Yoshimaro Kobayashi, Tatsuya Kondo, Maki Takebayashi, Shigeki Maruyama, Yoshimitsu NagaoAbstract:Abstract Asymmetric total synthesis of ISP-I has been achieved by utilizing highly selective E -olefin formation based on the Schlosser-modified Wittig reaction and highly diastereoselective aldol reactions employing both chiral heterocyclic derivatives, 3-acetyl-(4 S )-isopropyl-1,3-thiazolidine-2-thione and ethyl [(5 R )-2,5-dihydro-5-isopropyl-3,6-diethoxypyrazin]-2-yl carboxylate.
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asymmetric total synthesis of isp i myriocin Thermozymocidin a potent immunosuppressive principle in the isaria sinclairii metabolite
Tetrahedron Letters, 1995Co-Authors: Shigeki Sano, Tetsuro Fujita, Yoshimaro Kobayashi, Tatsuya Kondo, Maki Takebayashi, Shigeki Maruyama, Yoshimitsu NagaoAbstract:Abstract Asymmetric total synthesis of ISP-I has been achieved by utilizing highly selective E -olefin formation based on the Schlosser-modified Wittig reaction and highly diastereoselective aldol reactions employing both chiral heterocyclic derivatives, 3-acetyl-(4 S )-isopropyl-1,3-thiazolidine-2-thione and ethyl [(5 R )-2,5-dihydro-5-isopropyl-3,6-diethoxypyrazin]-2-yl carboxylate.
Maki Takebayashi - One of the best experts on this subject based on the ideXlab platform.
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asymmetric total synthesis of isp i myriocin Thermozymocidin a potent immunosuppressive principle in the isaria sinclairii metabolite
Tetrahedron Letters, 1995Co-Authors: Shigeki Sano, Tetsuro Fujita, Yoshimaro Kobayashi, Tatsuya Kondo, Maki Takebayashi, Shigeki Maruyama, Yoshimitsu NagaoAbstract:Abstract Asymmetric total synthesis of ISP-I has been achieved by utilizing highly selective E -olefin formation based on the Schlosser-modified Wittig reaction and highly diastereoselective aldol reactions employing both chiral heterocyclic derivatives, 3-acetyl-(4 S )-isopropyl-1,3-thiazolidine-2-thione and ethyl [(5 R )-2,5-dihydro-5-isopropyl-3,6-diethoxypyrazin]-2-yl carboxylate.
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asymmetric total synthesis of isp i myriocin Thermozymocidin a potent immunosuppressive principle in the isaria sinclairii metabolite
Tetrahedron Letters, 1995Co-Authors: Shigeki Sano, Tetsuro Fujita, Yoshimaro Kobayashi, Tatsuya Kondo, Maki Takebayashi, Shigeki Maruyama, Yoshimitsu NagaoAbstract:Abstract Asymmetric total synthesis of ISP-I has been achieved by utilizing highly selective E -olefin formation based on the Schlosser-modified Wittig reaction and highly diastereoselective aldol reactions employing both chiral heterocyclic derivatives, 3-acetyl-(4 S )-isopropyl-1,3-thiazolidine-2-thione and ethyl [(5 R )-2,5-dihydro-5-isopropyl-3,6-diethoxypyrazin]-2-yl carboxylate.