Topical therapeutic agent for ophthalmic diseases comprising compound capable of binding specifically to dna sequence
AssigneeNihon University
InventorsHiroki Nagase, Min Chen, Tohru Sakimoto, Takayoshi Watanabe, Noboru Fukuda
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Abstract
Disclosed is a topical therapeutic agent for ophthalmic diseases, which comprises a compound capable of binding specifically to a DNA sequence. More preferably disclosed is a topical therapeutic agent for ophthalmic diseases, which comprise a pyrrole-imidazole polyamide having a specific structure. The topical therapeutic agent for ophthalmic diseases comprises a pyrrole-imidazole polyamide which can inhibit transforming growth factor-β gene and matrix metalloproteinase 9 gene.
Claims46
A topical therapeutic agent for an ophthalmic disease containing a pyrrole-imidazole polyamide comprising an N-methylpyrrole unit (hereinafter, also referred to as Py), an N-methylimidazole unit (hereinafter, also referred to as Im), and a γ-aminobutyric acid unit, wherein the pyrrole-imidazole polyamide can be folded at the γ-aminobutyric acid unit to form a U-shaped conformation in a minor groove of a double helical region (hereinafter, also referred to as a target region) which comprises a part or a whole of a nucleotide sequence from −555 to −528 (SEQ ID NO:
- 2), a nucleotide sequence from −427 to −399 (SEQ ID NO:
- 4), or a nucleotide sequence from −384 to −355 (SEQ ID NO:
- 6) in a human transforming growth factor β (hereinafter, also referred to as TGF-β) gene promoter, and a strand complementary thereto, wherein a Py/Im pair corresponds to a C-G base pair, an Im/Py pair corresponds to a G-C base pair, and a Py/Py pair corresponds to both an A-T base pair and a T-A base pair.
A topical therapeutic agent for an ophthalmic disease containing a pyrrole-imidazole polyamide represented by the following formula.
A topical therapeutic agent for an ophthalmic disease containing a pyrrole-imidazole polyamide represented by the following formula.
A topical therapeutic agent for an ophthalmic disease containing a pyrrole-imidazole polyamide represented by the following formula.
A topical therapeutic agent for an ophthalmic disease containing a pyrrole-imidazole polyamide comprising an N-methylpyrrole unit (hereinafter, also referred to as Py), an N-methylimidazole unit (hereinafter, also referred to as Im), and a γ-aminobutyric acid unit, wherein the pyrrole-imidazole polyamide can be folded at the γ-aminobutyric acid unit to form a U-shaped conformation in a minor groove of a double helical region (hereinafter, also referred to as a target region) which comprises a part or a whole of a nucleotide sequence from −2316 to −2287 (SEQ ID NO:
- 25) or a nucleotide sequence from −2322 to −2293 (SEQ ID NO:
- 8) in a rat transforming growth factor β (hereinafter, also referred to as TGF-β) gene promoter, and a strand complementary thereto, wherein a Py/Im pair corresponds to a C-G base pair, an Im/Py pair corresponds to a G-C base pair, and a Py/Py pair corresponds to both an A-T base pair and a T-A base pair.
A topical therapeutic agent for an ophthalmic disease containing a pyrrole-imidazole polyamide represented by the following formula.
A topical therapeutic agent for an ophthalmic disease containing a pyrrole-imidazole polyamide represented by the following formula.
A topical therapeutic agent for an ophthalmic disease containing a pyrrole-imidazole polyamide comprising an N-methylpyrrole unit (hereinafter, also referred to as Py), an N-methylimidazole unit (hereinafter, also referred to as Im), and a γ-aminobutyric acid unit, wherein the pyrrole-imidazole polyamide can be folded at the γ-aminobutyric acid unit to form a U-shaped conformation in a minor groove of a double helical region (hereinafter, also referred to as a target region) which comprises a part or a whole of a nucleotide sequence from −88 to −59 (SEQ ID NO:
- 11) or a nucleotide sequence from −616 to −588 (SEQ ID NO:
- 13) in a human matrix metalloprotease 9 (hereinafter, also referred to as hMMP-9) gene promoter, and a strand complementary thereto, wherein a Py/Im pair corresponds to a C-G base pair, an Im/Py pair corresponds to a G-C base pair, and a Py/Py pair corresponds to both an A-T base pair and a T-A base pair.
A topical therapeutic agent for an ophthalmic disease containing a pyrrole-imidazole polyamide represented by the following formula.
A topical therapeutic agent for an ophthalmic disease containing a pyrrole-imidazole polyamide represented by the following formula.
A topical therapeutic agent for an ophthalmic disease containing a pyrrole-imidazole polyamide comprising an N-methylpyrrole unit (hereinafter, also referred to as Py), an N-methylimidazole unit (hereinafter, also referred to as Im), and a γ-aminobutyric acid unit, wherein the pyrrole-imidazole polyamide can be folded at the γ-aminobutyric acid unit to form a U-shaped conformation in a minor groove of a double helical region (hereinafter, also referred to as a target region) which comprises a part or a whole of a nucleotide sequence from −105 to −76 (SEQ ID NO:
- 15) or a nucleotide sequence from −602 to −575 (SEQ ID NO:
- 17) in a rat matrix metalloprotease 9 (hereinafter, also referred to as rMMP-9) gene promoter, and a strand complementary thereto, wherein a Py/Im pair corresponds to a C-G base pair, an Im/Py pair corresponds to a G-C base pair, and a Py/Py pair corresponds to both an A-T base pair and a T-A base pair.
A topical therapeutic agent for an ophthalmic disease containing a pyrrole-imidazole polyamide represented by the following formula.
A topical therapeutic agent for an ophthalmic disease containing a pyrrole-imidazole polyamide represented by the following formula.
Dependencies are inferred from the claim text.