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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2012/11/09 15:36:08」(JST)
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- 1. ヘキソースリン酸側路およびグルタチオン代謝関連疾患 related disorders of the hexose monophosphate shunt and glutathione metabolism
- 2. 肥大型心筋症の遺伝学 genetics of hypertrophic cardiomyopathy
- 3. レフルノミドによる関節リウマチの治療 leflunomide in the treatment of rheumatoid arthritis
- 4. デュシェンヌ型およびベッカー型筋ジストロフィーの臨床的特徴および診断 clinical features and diagnosis of duchenne and becker muscular dystrophy
- 5. グルコース-6-リン酸脱水素酵素欠損症の遺伝学および病態生理 genetics and pathophysiology of glucose 6 phosphate dehydrogenase deficiency
English Journal
- Development and Binding Mode Assessment of N-[4-[2-propyn-1-yl[(6S)-4,6,7,8-tetrahydro-2-(hydroxymethyl)-4-oxo-3H-cyclopenta[g]quinazolin-6-yl]amino]benzoyl]-L-γ-glutamyl-D-glutamic acid (BGC 945), a Novel Thymidylate Synthase Inhibitor that Targets Tumor Cells.
- Tochowicz A, Dalziel S, Eidam O, O'Connell J, Griner S, Finer-Moore JS, Stroud RM.AbstractN-[4-[2-propyn-1-yl[(6S)-4,6,7,8-tetrahydro-2-(hydroxymethyl)-4-oxo-3H-cyclopenta[g]quinazolin-6-yl]amino]benzoyl]-L-γ-glutamyl-D-glutamic acid 1 (BGC 945, now known as ONX 0801), is a small molecule thymidylate synthase (TS) inhibitor discovered at the Institute of Cancer Research in London. It is licensed by Onyx Pharmaceuticals and is in Phase 1 clinical studies. It is a novel antifolate drug resembling TS inhibitors plevitrexed and raltitrexed that combines enzymatic inhibition of thymidylate synthase with α-folate receptor-mediated targeting of tumor cells. Thus, it has potential for efficacy with lower toxicity due to selective intracellular accumulation through α-folate receptor (α-FR) transport. The α-FR, a cell-surface receptor glycoprotein, which is over expressed mainly in ovarian and lung cancer tumors, has an affinity for 1 similar to that for its natural ligand, folic acid. This study describes a novel synthesis of 1, an X-ray crystal structure of its complex with Escherichia coli TS and 2'-deoxyuridine-5'-monophosphate, and a model for a similar complex with human TS.
- Journal of medicinal chemistry.J Med Chem.2013 May 27. [Epub ahead of print]
- N-[4-[2-propyn-1-yl[(6S)-4,6,7,8-tetrahydro-2-(hydroxymethyl)-4-oxo-3H-cyclopenta[g]quinazolin-6-yl]amino]benzoyl]-L-γ-glutamyl-D-glutamic acid 1 (BGC 945, now known as ONX 0801), is a small molecule thymidylate synthase (TS) inhibitor discovered at the Institute of Cancer Research in London. It is
- PMID 23710599
- Ligand-directed Acid-sensitive amidophosphate 5-trifluoromethyl-2'-deoxyuridine conjugate as a potential theranostic agent.
- Godovikova TS, Lisitskiy VA, Antonova NM, Popova TV, Zakharova OD, Chubarov AS, Koptyug IV, Sagdeev RZ, Kaptein R, Akulov AE, Kaledin VI, Nikolin VP, Baiborodin SI, Koroleva LS, Silnikov VN.SourceInstitute of Chemical Biology and Fundamental Medicine , SB RAS, 630090 Novosibirsk, Russia.
- Bioconjugate chemistry.Bioconjug Chem.2013 May 15;24(5):780-95. doi: 10.1021/bc3006072. Epub 2013 Apr 16.
- Herein, we report a novel strategy to engineer an acid-sensitive anticancer theranostic agent using a vector-drug ensemble. The ensemble was synthesized by directly conjugating the linoleic acid (LA)-modified branched polyethyleneimine with a chemotherapeutic drug trifluorothymidine. Linoleic acid r
- PMID 23521072
- Localization of putative binding sites for cyclic guanosine monophosphate and the anti-cancer drug 5-fluoro-2'-deoxyuridine-5'-monophosphate on ABCC11 in silico models.
- Honorat M, Terreux R, Falson P, Di Pietro A, Dumontet C, Payen L.SourceINSERM, UMR-S1052, Centre de Recherche en Cancérologie de Lyon, Lyon F-69008, France. lea.payen-gay@chu-lyon.fr.
- BMC structural biology.BMC Struct Biol.2013 May 6;13:7. doi: 10.1186/1472-6807-13-7.
- BACKGROUND: The Multidrug Resistance Protein ABCC11/MRP8 is expressed in physiological barriers and tumor breast tissues in which it secretes various substrates including cGMP (cyclic guanosine monophosphate) and 5FdUMP (5-fluoro-2'-deoxyuridine-5'-monophosphate), the active metabolite of the antica
- PMID 23641929
Japanese Journal
- Mechanisms for 5-Fluorouracil Resistance in Human Colon Cancer DLD-1 Cells
- Inaba Makoto,Naoe Yoshinori,Mitsuhashi Junko
- Biological & pharmaceutical bulletin 21(6), 569-573, 1998-06-15
- … As causes of resistance to DNA and RNA-directed actions of 5-FU, remarkable reduction of intracellular levels of both 5-fluorouridine 5'-triphosphate (FUTP) and 5-fluoro-2'-deoxyuridine 5'-monophosphate (FdUMP) in DLD-1/5-FU cells was confirmed. …
- NAID 110003639415
- Synthetic Nucleosides and Nucleotides. XXXV.> Synthesis and Biological Evaluations of 5-Fluoropyrimidine Nucleosides and Nucleotides of 3-Deoxy-β-D-ribofuranose and Related Compounds
- 実吉 峯郎,香坂(市川) 瑞江,八幡 昭子,木村 茂,伊豆田 俊二,山口 十四文
- Chemical & pharmaceutical bulletin 43(11), 2005-2009, 1995-11-15
- … Compounds 3a-d were saponified to give free 3'-deoxycytidine (5a), 5-fluoro-3'-deoxycytidine (5b), 3'-deoxyuridine (5c), and 5-fluoro-3'-deoxyuridine (5d), respectively. … These 3'-deoxyribonucleosides (5a-d) were then converted to corresponding 5'-monophosphate and further phosphorylated to the 5'-triphosphates by the phosphoroimidazolidate method.The nucleosides (5a-d) were examined for growth-inhibitory effects on mouse leukemic L5178Y cells, and their IC<50> …
- NAID 110003631387
- The number of 5-fluoro-2'-deoxyuridine-5'-monophosphate binding sites and reduced folate pool in human colorectal carcinoma tissues : changes after tegafur and uracil treatment
- OMURA K.
- Cancer Res 55, 3897-3901, 1995
- NAID 80008541178
Related Links
- Except where noted otherwise, data are given for materials in their standard state (at 25 °C, 100 kPa) · Infobox references. Deoxyuridine monophosphate is a deoxynucleotide. It is an intermediate in the metabolism of deoxyribonucleotides.
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★リンクテーブル★
| リンク元 | 「dUMP」「デオキシウリジン一リン酸」 |
| 関連記事 | 「monophosphate」 |
「dUMP」
「デオキシウリジン一リン酸」
「monophosphate」
- n.