Chiba-prefecture

Kyoto University

Japan Science and Technology Agency

Japan Science and Technology Corporation

Toshikazu Bando

Hiroshi Sugiyama

Hiroki Nagase

Isao Saito

Atsushi Takatori

Hirokazu Iida

The present invention provides a novel alkylating agent specifically binding to the genetic mutation site of a driver oncogene. There are provided are a complex formed by binding an alkylating agent to a pyrrole imidazole polyamide specifically binding to the genetic mutation site of a driver oncogene, a driver oncogene mutation-specific alkylating agent comprising the aforementioned complex, and a pharmaceutical composition comprising the aforementioned complex.

Alkylating agent for alkylating target with driver oncogene mutation

The present invention provides: a histone modification control agent for activating expression of a specific gene, i.e., a complex including a histone acetylation enzyme activator useful as an agent for activating a specific gene, and a polyamide for recognizing a regulatory region of a target gene; and a method for manufacturing the same. This complex specifically activates a group of genes relating to maintenance and/or differentiation of stem cells or precursor cells.

CTB-PI polyamide conjugate for activating expression of specific gene

There is provided a novel pyrrole-imidazole polyamide compound for alkylating the specific base sequence of DNA, the polyamide compound being capable of being synthesized through fewer reaction steps than known hybrid molecules and having a combination of a high reactivity in DNA alkylation and the ability to recognize a sequence. Furthermore, there is provided an alkylating agent and a molecule serving as a drug, the alkylating agent and the molecule containing the polyamide compound. An indole derivative is represented by general formula (1): wherein Rrepresents a functional group for alkylating DNA; Rrepresents a hydrogen atom, an alkyl group, or an acyl group; and X represents a divalent group having one constitutional unit or having two or more constitutional units which may be the same or different, the constitutional unit being represented by the following formula: (wherein m is an integer of 0 to 10), wherein among the constitutional units, a terminal constitutional unit adjacent to Rmay be a constitutional unit represented by the following formula: (wherein k is an integer of 0 to 10).

Indole derivative for alkylating specific base sequence of DNA and alkylating agent and drug containing the derivative

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

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.

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Kyoto, Japan

Toshikazu Bando