摘要:
Phosphonate-nucleotide ester compounds of the formula (I) have excellent antiviral activity and antineoplastic activity. Further, they can be orally administered. ##STR1## wherein ring A represents ##STR2## wherein R.sup.1 and R.sup.2 independently represent hydrogen, halogen, hydroxyl, mercapto, C.sub.6 -C.sub.10 arylthio or amino; R.sup.3 represents C.sub.1 -C.sub.4 alkyl or ethyl having one or more substituents selected from the group consisting of fluorine, C.sub.1 -C.sub.4 alkoxy, phenoxy, C.sub.7 -C.sub.10 phenylalkoxy and C.sub.2 -C.sub.5 acyloxy; R.sup.4 represents ethyl having one or more substituents selected from the group consisting of fluorine, C.sub.1 -C.sub.4 alkoxy, phenoxy, C.sub.7 -C.sub.10 phenylalkoxy and C.sub.2 -C.sub.5 acyloxy; X, Y and Z independently represent methyne or nitrogen atom; or a pharmaceutically acceptable salt thereof.
摘要:
A method for screening a nucleic acid library for a nucleic acid encoding a protein that interacts with a target substance, which comprises: the step of producing a library of assigning molecules each comprising a protein and a nucleic acid encoding the protein linked to each other via a linker cleavable under a condition that does not change a nucleotide sequence of the nucleic acid; the step of mixing the library of assigning molecules and the target substance; the step of separating an assigning molecule binding to the target substance; the step of cleaving a linker of the separated assigning molecule under a condition that does not change a nucleotide sequence of the nucleic acid to release the nucleic acid; and the step of collecting the released nucleic acid. By this method, screening for an assigning molecule that specifically binds to a target substance can be conducted with high efficiency.
摘要:
A compound represented by the following general formula (I) which has an antiviral activity: wherein R1 represents hydrogen atom, C1-C6 alkyl group, or C7-C10 aralkyl group; R2 represents C1-C6 alkyl group, C7-C10 aralkyl group, or phenyl group; R3 and R4 independently represent hydrogen atom, C1-C6 alkyl group, acyloxymethyl group, acylthioethyl group, or ethyl gorup substituted with at least one halogen atom; R5 represents hydrogen atom, C1-C4 alkyl gorup, C1-C4 hydroxyalkyl group, C1-C4 alkyl group substituted with at least one halogen atom; and X represents carbon atom or nitrogen atom.
摘要:
A phosphonate nucleotide compound represented by formula (I): (wherein R1 is a C1-C6 alkyl group or the like, R2 is a hydrogen atom, a C1-C4 alkyl group substituted by one or more halogen atoms or the like, R3 is a hydrogen atom, a C1-C4 alkyl group substituted by one or more halogen atoms or the like, R4 is a hydrogen atom, a C1-C4 alkyl group substituted by one or more halogen atoms and X is a carbon atom or a nitrogen atom), a salt thereof, a hydrate thereof or a solvate thereof, as well as a medicament containing the same. It is useful as an antiviral agent for human immunodeficiency virus, herpes simplex virus, hepatitis B virus or the like and as an antitumor agent.
摘要:
A phosphonate nucleotide compound having antiviral activity and is useful for an orally available and highly safe antiviral agent, which is represented by the following formula (I): ##STR1## wherein R.sup.1 represents hydrogen, a C.sub.1 -C.sub.6 alkoxy, a halogen-substituted C.sub.1 -C.sub.4 alkoxy, halogen, amino, or nitro; R.sup.2 and R.sup.3 independently represent hydrogen, a C.sub.1 -C.sub.22 alkyl, an acyloxymethy, an acylthioethyl, or a halogen-substituted ethyl; R.sup.4 represents hydrogen, a C.sub.1 -C.sub.4 alkyl, a C.sub.1 -C.sub.4 hydroxyalkyl, or a halogen-substituted C.sub.1 -C.sub.4 alkyl; and X represents carbon or nitrogen.
摘要:
Provided hereinbelow is a process of extrusion-coating the central core, said core being used in a submarine coaxial cable, with an insulator of high pressure-processed polyethylene having a density of from 0.925 to 0.940 g/cm.sup.3 and a melt index of from 0.01 to 0.3 g/10 min with advantages in that said coaxial cable is allowed to be placed on a sea bottom of not less than 500 meters in depth and to effectively transmit alternating current signals with a maximum frequency of not less than 30 MHZ, while attenuation of said signals is reduced, and thus, said coaxial cable has a transmission capacity of not less than 3000 circuits or channels with a frequency band of from 3 to 6 KHz per each circuit or channels, wherein the insulator-covered-core is continuously extruded from an extruder and then is gradually cooled in cooling water troughs to room temperature so that the water content of said insulator, without formation of voids between said central core and said insulator, is reduced by as much as possible.
摘要翻译:在下文中提供了一种挤压涂覆中心芯的方法,所述芯用在海底同轴电缆中,其中具有密度为0.925-0.940g / cm 3和熔体指数为0.01的高压加工聚乙烯绝缘体 至0.3g / 10min,其特征在于允许将所述同轴电缆放置在深度不小于500米的海底上,并有效地传输最大频率不小于30MHz的交流信号,同时衰减 的所述信号被减少,因此,所述同轴电缆具有每个电路或通道具有不小于3000个电路或具有3至6KHz频带的通道的传输容量,其中绝缘体覆盖芯被连续挤出 然后在冷却水槽中逐渐冷却至室温,使得所述绝缘体的水含量在所述中心芯和所述绝缘体之间不形成空隙,由此减少 越多越好。
摘要:
An assigning molecule obtained by ligating a genotype molecule to a phenotype molecule by transpeptidation, wherein the genotype molecule is constructed by bonding (a) a spacer molecule comprising a donor region which can be bonded to a 3′-terminal end of nucleic acid, a PEG region bonded to the donor region and a peptide acceptor region which is bonded to the PEG region, to (b) a 3′ end of a nucleic acid comprising a 5′ untranslated region comprising a transcription promoter and a translation enhancer; an ORF region which comprises a polyA sequence and which is bonded to the 3′-terminal side of the 5′ untranslated region; and a 3′-terminal region that is bonded to the 3′-terminal side of the ORF region.
摘要:
A translation template comprising an ORF region coding for a protein, a 5′ untranslated region comprising a transcription promoter and a translation enhancer and locating on the 5′ side of the ORF region, and a 3′ end region comprising a poly-A sequence and locating on the 3′ side of the ORF region, is expressed in a translation system in the presence of an agent for modifying a C-terminal of a protein, which comprises an acceptor portion having a group capable of binding to a protein through a transpeptidation reaction in a protein translation system and a modifying portion comprising a nonradioactive modifying substance linked to the acceptor portion via a nucleotide linker, to cause protein synthesis and the synthesized protein is purified. Thus, the yield of modified protein in a method of modifying C-terminal of protein is improved and detection of protein interaction based on various intermolecular interaction detection methods is realized at an improved level.
摘要:
A translation template comprising an ORF region coding for a protein, a 5′ untranslated region comprising a transcription promoter and a translation enhancer and locating on the 5′ side of the ORF region, and a 3′ end region comprising a poly-A sequence and locating on the 3′ side of the ORF region, is expressed in a translation system in the presence of an agent for modifying a C-terminal of a protein, which comprises an acceptor portion having a group capable of binding to a protein through a transpeptidation reaction in a protein translation system and a modifying portion comprising a nonradioactive modifying substance linked to the acceptor portion via a nucleotide linker, to cause protein synthesis and the synthesized protein is purified. Thus, the yield of modified protein in a method of modifying C-terminal of protein is improved and detection of protein interaction based on various intermolecular interaction detection methods is realized at an improved level.