Japan Science and Technology Corporation

Japan Science and Technology Agency

Credia Japan Co., Ltd.

Ngk Insulators, Inc.

Other

Toagosei Company, Ltd.

Yamasa Shoyu Kabushiki Kaisha

Isao Saito

Hiroshi Sugiyama

Hirokazu Iida

Akimitsu Okamoto

Hisafumi Ikeda

Shinsuke Sando

Yasuko Yoshida

Toshikazu Bando

Kazuo Tanaka

Kazuhiko Nakatani

Yushin Nakamura

Takashi Saito

Hideyuki Ikehira

Kousuke Niwa

Yoko Matsuda

Kiyoshi Uchida

Takayoshi Uchida

Yoshio Saito

Fumihiko Kitagawa

Zhi-Fu Tao

Shigeo Matsuda

Kenzo Fujimoto

Zhi Fu Tao

Teruo Matsuura

Ken Hatano

A method of easily releasing a useful substance bonded to oligonucleotide without impairing a target nucleic acid; and a novel base therefore. A nucleoside of nucleotide (oligonucleotide containing thereof) represented by the formula (I) (wherein each of X and Y independently represents &#x2014;O&#x2014;, &#x2014;NH&#x2014;, &#x2014;N(alkyl)- or &#x2014;S&#x2014;; R represents a functional unit, a reporter unit or a biofunctional molecule; each of Rand Rindependently represents a hydrogen atom, a phosphate bond group, a phosphoramidite group or a nucleotide; and n is a numeral of 1 to 10). There is further provided a method of releasing the R group moiety at base portion by the use of the oligonucleotide comprising the nucleotide.

Nucleoside releasing functional unit through oxidation and process for producing oligonucleotide containing thereof

It is intended to provide a pyrrole-imidazole polyamide type functional molecule having enhanced abilities of alkylating DNA and recognizing a sequence, compared with the existing functional molecules of this type, for a specific base sequence occurring on DNA. A hairpin polyamide having an alkylation site via a vinyl linker at the end of a pyrrole-imidazole polyamide. Drugs for inhibiting the expression of a specific gene and anticancer agents containing the above hairpin polyamide.

Hairpin polyamide

A novel nucleotide derivative, in case of existing as a member of a single-stranded sequence, undergoing a change in the fluorescent signal intendity depending on the corresponding base type in the partner strand with which the single-stranded sequence is hybridized, and which is a thymin/uracil derivative (1) emitting light most intensely when a confronting base in the partner strand with which the single-stranded nucleotide sequence is hybridized is adenine; a cytosine derivative (2) emitting light most intensely when the confronting base is guanine; an adenine derivative (3) emitting light most intensely when the confronting base is cytosine; a guanine derivative (4) emitting light most intensely when the confronting base is cytosine or thymine/uracil; and an adrnine derivative (5) emitting light most intensely when the confronting base is thymine/uracil/.

Nucleotide derivative and DNA microarray

A method for screening the effect of a segment A (chemical species A) on a substance (for example, a cell) containing DNA or RNA by using artificial chemical species. Namely, a method of detecting or identifying the function of a chemical species A on a substance containing DNA or RNA by using one or more chemical species represented by the following general formula (I) which are capable of recognizing a DNA base sequence; a kit therefor; and a plate to be used therein: B-L-A (I) wherein B represents a chemical structure containing an non-natural base capable of recognizing a DNA base sequence; A represents a chemical structure having an interaction with DNA; and L represents a linker whereby the chemical structures A and B can be linked together.

Development of method for screening physiologically active pyrrole imidazole derivative

A method of forming a self-connective structure (a hairpin structure, a four-stranded structure, etc.) of a single-stranded oligonucleotide chain by forming a mimetic base pair of a mismatch base pair failing to form any normal base pair among base pairs of the single-stranded oligonucleotide chain with the use of a compounds represented by the following general formula (I): A-L-B (I) wherein A represents a chemical structural moiety capable of forming a pair with one base of a base pair failing to form any normal base pair; B represents a chemical structural moiety capable of forming a pair with the other base of the base pair failing to form any normal base pair; and L represents a linker structure by which the chemical structures A and B are linked to each other; and a method of inhibiting the activity of enzyme according to the previous method.

Molecules capable of binding to telomere and the like and method with the use of the same

A process for amino acid derivatives shown by the below general formula (I): (wherein Rmeans a hydrogen atom or a straight chain or branched chain alkyl group with 1-5 carbon atoms.) having an object to provide a process of the amino acid derivatives of the formula (I) and their synthetic intermediate, t-butoxycarbonylamino-ethylamine, whereby it requires no tedious procedure and is also good in yield, and its application to a mass production is easy, and to provide novel amino acid derivatives of the formula (IV), their synthetic intermediates, and a process thereof, characterized in that it comprises a step to obtain the amino acid derivatives shown by the general formula (I) by hydrolysis of compounds shown by the below formula (II): (wherein Rhas the same meaning as described above, and Rmeans a straight chain or branched chain alkyl group with 1-4 carbon atoms.) as well as amino acid derivatives shown by the general formula (IV): (wherein Rmeans a hydrogen atom or a straight chain or branched chain alkyl group with 1-5 carbon atoms, and n means any one of integers 1-11.), and a process for the amino acid derivative, characterized in that it comprises a reduction step of benzyloxycarbonyl-&#x3c9;-amino acid derivatives.

T-butoxycarbonylaminoethylamine for the synthesis of PNA monomer units, amino acid derivatives, intermediates therof, and processes for productions of them

A novel nucleotide derivative, in case of existing as a member of a single-stranded sequence, undergoing a change in the fluorescent signal intensity depending on the corresponding base type in the partner strand with which the single-stranded sequence is hybridized, and which is (1) a thymine/uracil derivative emitting light most intensely when a confronting base in the partner strand with which the single-stranded nucleotide sequence is hybridized is adenine; (2) a cytosine derivative emitting light most intensely when the confronting base is guanine; (3) an adenine derivative emitting light most intensely when the confronting base is cytosine; and, (4) a guanine derivative emitting light most intensely when the confronting base is cytosine or thymine/uracil.

A compound represented by the general formula (I) below: In the formula, A is as defined in the specification and B denotes where n is an integer of 1 to 4, and a process for producing the above compound includes a reaction between an activated ester and a t-butoxycarbonylaminoethylamine or an &#x3c9;-amino acid derivative.

Functional peptide nucleic acid monomer and process for producing the same

A nucleic acid base for hole transportation in DNAs which does not cause oxidative decomposition; and an artificial DNA molecule which can realize effective hole transportation in DNAs while maintaining the double spiral structure of the DNAs. Provided are: a nucleic acid which contains a benzodeazaadenine derivative base represented by the general formula (I): (wherein R, R, R, R, R, and Reach independently represents hydrogen, amino, mono (lower alkyl) amino, di (lower alkyl) amino, hydroxy, lower alkoxy, halogeno, cyano, mercapto, lower alkylthio, or aryl; and Rand Reach independently represents hydrogen or a group bonded to phosphoric acid);

Benzodeazaadenine derivative base and electronic material containing the same

It is intended to provide a method of producing a pyrrole-imidazole polyamide whereby a longer pyrrole-imidazole polyamide can be conveniently synthesized and a peptide (protein) can be easily transferred. According to this method, a pyrrole-imidazole polyamide having a carboxylate group which can be excised from a solid phase carrier at its end, makes it possible to directly transfer various functional groups and can exactly distinguish DNA sequences can be efficiently produced. A method of synthesizing a pyrrole-imidazole polyamide characterized by performing automatic synthesis by the solid phase Fmoc method with the used of a peptide synthesizer; a pyrrole-imidazole polyamide having a carboxyl group at its end obtained by this method; a pyrrole-imidazole polyamide having a DNA alkylation agent transferred into the carboxyl group at the end of the above-described pyrrole-imidazole polyamide; and a sequence-specific DNA alkylation method characterized by using the above compound.

Method of the solid phase synthesis of pyrrole-imidazole polyamide

Compounds represented by the general formula (I): which two DNA strands can be interstrand-crossliked:A-L-B-X-B-L-A&#x2003;&#x2003;(I)wherein B represents a chemical structure capable of recognizing the nucleotide sequence of DNA; A represents a chemical structure capable of binding to one of the bases of DNA; L represents a linker by which the chemical structures of A and B can be linked to each other; X represents a spacer by which the A-L-B components can be linked to each other. A method of interstrand-crosslinking DNA by using these compounds; and medicinal compositions containing interstarand-crosslinking agents of DNA.

Interstrand crosslinking agents for DNA and compounds therefor

A process for amino acid derivatives shown by the below general formula (I):(wherein Rmeans a hydrogen atom or a straight chain or branched chain alkyl group with 1-5 carbon atoms.) having an object to provide a process of the amino acid derivatives of the formula (I) and their synthetic intermediate, t-butoxycarbonylamino-ethylamine, whereby it requires no tedious procedure and is also good in yield, and its application to a mass production is easy, and to provide novel amino acid derivatives of the formula (IV), their synthetic intermediates, and a process thereof, characterized in that it comprises a step to obtain the amino acid derivatives shown by the general formula (I) by hydrolysis of compounds shown by the below formula (II):(wherein Rhas the same meaning as described above, and Rmeans a straight chain or branched chain alkyl group with 1-4 carbon atoms.) as well as amino acid derivatives shown by the general formula (IV):(wherein Rmeans a hydrogen atom or a straight chain or branched chain alkyl group with 1-5 carbon atoms, and n means any one of integers 1-11.), and a process for the amino acid derivative, characterized in that it comprises a reduction step of benzyloxycarbonyl-&#x3c9;-amino acid derivatives.

T-butoxycarbonylaminoethylamine for the synthesis of PNA monomer units, amino acid derivatives, intermediates thereof, and processes for productions of them

Novel chemical species capable of simultaneously alkylating double-stranded DNA and cleaving the same; methods for alkylating and cleaving DNA by using these species; and anticancer agents with the use of these compounds. Compounds represented by the following general formula (I) which are capable of simultaneously alkylating double-stranded DNA and cleaving the same; a method for alkylating DNA and a method for cleaving double stranded DNA by using these compounds; and medicinal compositions with the use of these compounds: B&mdash;L&mdash;A(I) wherein B represents a chemical structure capable of recognizing the base sequence of DNA, for example, optionally substituted pyrrole-imidazole polyamide; A represents a chemical structure capable of binding to one base of DNA, for example, the alkylation moiety of duocarmycin A; and L represents a linker capable of binding the chemical structures A and B, for example, vinyl.

Compounds capable of cleaving double-stranded DNA and method of utilization of the same

A method whereby a mismatched base pair in a nucleic acid such as DNA or RNA can be conveniently and highly sensitively detected; and detection reagents therefor. A method comprising, in a base pair failing to form a normal base pair, forming a mimetic base pair with the use of a mismatch-recognizing molecule represented by the following general formula (I): A&mdash;L&mdash;B (I) wherein A represents a chemical structure moiety capable of forming a pair with one of the bases of the base pair failing to form a normal base pair; B represents a chemical structure moiety capable of forming a pair with the other of the bases of the base pair failing to form a normal base pair; and L represents a linker structure whereby the chemical structure moieties A and B are linked to each other; and measuring the formation of the above-described mimetic base pair to thereby detect and identify the base pair failing to form a normal base pair; kits therefor; reagents for detecting a mismatch; and a method of detecting an abnormality in the base sequence of a gene.

Growing community of inventors

Kyoto, Japan

Isao Saito