- SITE-SPECIFIC RADIOFLUORINATION OF PEPTIDES WITH 8-[18F]-FLUOROOCTANOIC ACID CATALYZED BY LIPOIC ACID LIGASE
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New methodologies for site-specifically radiolabeling proteins with the PET isotope [18F] are required to generate high quality radiotracers for imaging in both the preclinical and clinical settings. The enzymatic radiofluorination overcomes many of the limitations encountered to date with purely chemical approaches. The bacterial enzyme lipoic acid ligase was used to conjugate [18F]-fluorooctanoic acid to both a small peptide and a Fab antibody fragment. Labeling was site-specific and highly efficient under mild aqueous conditions using small amounts of peptide/protein (1-10 nmol). The labeled construct retained full epitope binding affinity and was stable in mouse serum. Using an optimized reaction scheme, mCi quantities of [18F]-Fab were generated, an amount sufficient for human imaging.
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Paragraph 00207
(2017/12/28)
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- DIHYDROOROTIC ACID DEHYDROGENASE INHIBITOR
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The present invention provides a novel dihydroorotic acid dehydrogenase inhibitor which is applicable to various diseases. When used as an active ingredient, a compound represented by formula (I): (wherein X represents a halogen atom, R1 represents a hydrogen atom, R2 represents an alkyl group containing 1 to 7 carbon atoms, R3 represents -CHO, and R4 represents -CH2-CH=C(CH3)-R0 (wherein R0 represents an alkyl group containing 1 to 12 carbon atoms which may have a substituent on the terminal carbon and/or on a non-terminal carbon, etc.)), an optical isomer thereof or a pharmaceutically acceptable salt thereof has a high inhibitory effect on dihydroorotic acid dehydrogenase and can be used as an immunosuppressive agent, a therapeutic agent for rheumatism, an anticancer agent, a therapeutic agent for graft rejection, an antiviral agent, an anti-H. pylori agent, a therapeutic agent for diabetes or the like.
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Paragraph 0092; 0094; 0095
(2015/04/15)
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- NOVEL DIHYDROXYBENZENE DERIVATIVES AND ANTIPROTOZOAL AGENT COMPRISING SAME AS ACTIVE INGREDIENT
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Novel compounds below are useful for preventing or treating diseases caused by protozoans. At least one of a compound represented by Formula (I) (wherein, X represents a hydrogen atom or a halogen atom; R1 represents a hydrogen atom; R2 represents a hydrogen atom or a C1-7 alkyl group; R3 represents -CHO, -C(=O)R5, -COOR5 (wherein R5 represents a C1-7 alkyl group), -CH2OH or -COOH; and R4 represents a C1-16 alkyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s), a C2-16 alkenyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s), or a C2-16 alkynyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s)), an optical isomer thereof, and a pharmaceutically acceptable salt is used.
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Paragraph 0102; 0104; 0105
(2013/09/26)
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- Reductive bromine atom-transfer reaction
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Atom-transfer radical (ATR) reactions of alkenes with R-X usually give products having new C-C and C-X bonds at the adjacent carbons. However, when the reaction was carried out under irradiation using a low-pressure Hg lamp, addition/reduction products were obtained in good yield. Hydrogen bromide, formed by H-abstraction of a bromine radical from alkenes, is likely to play a key role in the reductive ATR reaction.
- Sumino, Shuhei,Fusano, Akira,Ryu, Ilhyong
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supporting information
p. 2826 - 2829
(2013/07/19)
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- Potent oligomerization and macrocyclization activity of the thioesterase domain of vicenistatin polyketide synthase
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The thioesterase domain of the polyketide synthase involved in the biosynthesis of the 20-membered macrolactam antibiotic vicenistatin (VinTE) was found to catalyze oligomerization and macrocyclization of ω-hydroxy fatty acid ethyl esters to afford 17-28-membered macrocyclic lactones. The ring sizes of the macrocycles appear to be limited to the more moderate sizes because of the space limitation of the active site of VinTE. It was also verified that the initially formed linear dimer is first released from the active site of VinTE and then is recognized again by VinTE prior to its transformation to the cyclic dimer.
- Kudo, Fumitaka,Asou, Yusaku,Watanabe, Moe,Kitayama, Takashi,Eguchi, Tadashi
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supporting information; experimental part
p. 1843 - 1846
(2012/08/29)
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- A mild and versatile method for the tetrahydropyranylation of alcohols and their detetrahydropyranylation
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An efficient and mild method for tetrahydropyranylation of alcohols and their detetrahydropranylation using NH4Cl is described. This protocol provides a useful alternative tetrahydropyranylation of alcohols and their deprotection at different pH.
- Yadav,Srinivas, Dale,Reddy, Gondi Sudershan
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p. 1399 - 1404
(2007/10/03)
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- Tin-free reductive photochemical carboxymethylation of olefins with α- alkylthioacetates
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An efficient tin-free reductive photochemical carboxymethylation of olefins with α-alkylthioacetates is developed, which (a) is an experimentally simple technique furnishing substituted derivatives of fatty acids in moderate to good yields, (b) is compatible with polar/protic functional groups and solvents, (c) does not require a special reducing reagent, (d) is fairly insensitive to the presence of dissolved oxygen and, generally, does not require degassing prior to irradiation. The critical feature of the mechanism is the 'reluctance' of short-lived MeS' to group- transfer, resulting in hydrogen abstraction from the media.
- Deng, Lisa X.,Kutateladze, Andrei G.
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p. 7829 - 7832
(2007/10/03)
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- Reductive decyanation of α-cyano and α-alkoxycarbonyl substituted nitriles promoted by samarium(II) iodide
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Decyanation of geminal dinitriles and α-alkoxycarbonyl substituted nitriles promoted by samarium(II) iodide has been efficiently achieved. This method has advantages over the previously known radical route using tin hydride with respect to applicable substrates and the reaction temperature employed. This decyanation could broaden the synthetic applicability of the nitrile derivatives.
- Kang,Hong,Cho,Koh
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p. 7661 - 7664
(2007/10/02)
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- Synthesis of ω-fluorinated octanoic acid and its β-substituted derivatives
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Simple syntheses are described for the ω-fluorinated analogs of octanoic acid and its β-substituted derivatives in which insertion of a methyl and dimethyl group, and oxygen substitution at the C-3 position are involved, employing nucleophilic displacement with fluoride ion of the tosylate functions in the later stage of synthesis.The synthetic procedures offer easy and convenient acces to the corresponding 18F-labeled analogs using the readily available fluoride ion.
- Nagatsuki, Fumi,Sasaki, Shigeki,Maeda, Minoru
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p. 373 - 383
(2007/10/02)
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- Synthesis of (+/-)-11-Hydroxy-trans-8-dodecenoic Acid
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(+/-)-11-Hydroxy-trans-8-dodecenoic acid (2), an intermediate for the synthesis of recifeiolide, has been prepared starting from caprolactone and 1,3-butanediol.
- Bhide, K. S.,Sharma, G. V. M.
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p. 1081 - 1083
(2007/10/02)
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