2004 Fiscal Year Final Research Report Summary
Design of drugs for Vitamin D receptor mutant related to hereditary vitamin D-resistant rickets
| Project/Area Number |
15590107
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Drug development chemistry
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| Research Institution | National Institute of Health Sciences |
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Principal Investigator |
KURIHARA Masaaki National Institute of Health Sciences, 有機科学部 (20205206)
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| Project Period (FY) |
2003 – 2004
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| Keywords | vitamin D_3 analogues / hereditary vitamin D-resistant rickets / vitamin D receptor / コンピュータモデリング |
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| Research Abstract |
Hereditary vitamin D-resistant rickets(HVDRR) is a genetic disorder caused by mutations in the vitamin D receptor, which lead to resistance to 1a,25-dihydroxyvitamin D_3[1a,25(OH)_2D_3]. We found that the A ring-modified analogues, 2a-(3-hydroxypropyl)- and 2a-(3-hydroxypropoxy)- 1a,25(OH)_2D_3, (O1C3 and O2C3) can bind better than the natural hormone to the mutant VDR (R274A), which similar to the HVDRR mutant, R274L, had lost the hydrogen bond to the 1a-hydroxyl group of 1a,25(OH)_2D_3,.
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Research Products
(18 results)
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[Journal Article] Design and Efficient Synthesis of 2α-(w-Hydroxyalkoxy)-1α, 25-dihydroxyvitamin D_3 An alogues, Including 2-epi-ED-71 and Their 20-Epimers with HL-60 Cell Differentiation Activity2004
Author(s)
N.Saito, Y.Suhara, M.Kurihara, T.Fujishima, S.Honzawa, H.Takayanagi, T.Kozono, M.Matsumoto, M.Ohmori, N.Miyata, H.Takayama, A.Kittaka
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Journal Title
J.Org.Chem. 69
Pages: 7463-7471
Description
「研究成果報告書概要(和文)」より
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[Journal Article] 2,2-Functionlized Analogues of 1α, 25-Dihydroxyvitamin D_3, The Potent Inducers of Cell Differentiation2004
Author(s)
T.Fujishima, A.Kittaka, M.Kurihara, N.Saito, S.Honzawa, S.Kishimoto, T.Sugiura, K.Waku, H.Takayama
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Journal Title
J.Steroid Biochem.Mol.Biol. 89-90
Pages: 89-92
Description
「研究成果報告書概要(和文)」より
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[Journal Article] Design and Efficient Synthesis of 2α-(w-Hydroxyalkoxy)-1α,25-dihydroxyvitamin D_3 Analogues, Including 2-epi-ED-71 and Their 20-Epimers with HL-60 Cell Differentiation Activity2004
Author(s)
N.Saito, Y.Suhara, M.Kurihara, T.Fujishima, S.Honzawa, H.Takayanagi, T.Kozono, M.Matsumoto, M.Ohmori, N.Miyata, H.Takayama, A.Kittaka
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Journal Title
J.Org.Chem. 69
Pages: 7463-7471
Description
「研究成果報告書概要(欧文)」より
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-
[Journal Article] 2,2-Functionlized Analogues of 1α,25-Dihydroxyvitamin D_3, The Potent Inducers of Cell Differentiation2004
Author(s)
T.Fujishima, A.Kittaka, M.Kurihara, N.Saito, S.Honzawa, S.Kishimoto, T.Sugiura, K.Waku, H.Takayama
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Journal Title
J.Steroid Biochem.Mol.Biol. 89-90
Pages: 89-92
Description
「研究成果報告書概要(欧文)」より
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[Journal Article] Concise Synthesis and Biological Activities of 2α-Alkyl- and 2α-(ω-Hydroxyalkyl)-20-epi-1α,25-dihydroxyvitamin D_32003
Author(s)
S.Honzawa, Y.Suhara, K.Nihei, N.Saito, S.Kishimoto, T.Fujishima, M.Kurihara, T.Sugiura, K.Waku, H.Takayama, A.Kittaka
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Journal Title
Bioorg.Med.Chem.Lett. 13
Pages: 3503-3506
Description
「研究成果報告書概要(欧文)」より
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