JP2017526640A5 - - Google Patents

Info

Publication number

JP2017526640A5

JP2017526640A5 JP2017501204A JP2017501204A JP2017526640A5 JP 2017526640 A5 JP2017526640 A5 JP 2017526640A5 JP 2017501204 A JP2017501204 A JP 2017501204A JP 2017501204 A JP2017501204 A JP 2017501204A JP 2017526640 A5 JP2017526640 A5 JP 2017526640A5

Authority

JP

Japan

Prior art keywords

peptide

amino acid

antimicrobial

targeting

acid sequence

Prior art date

2015-07-07

Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)

Pending

Links

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• 108090000765 processed proteins & peptides Proteins 0.000 claims description 638
• 125000003275 alpha amino acid group Chemical group 0.000 claims description 186
• 230000008685 targeting Effects 0.000 claims description 180
• 150000001413 amino acids Chemical class 0.000 claims description 160
• 108700042778 Antimicrobial Peptides Proteins 0.000 claims description 154
• 102000044503 Antimicrobial Peptides Human genes 0.000 claims description 154
• -1 Tboc Chemical group 0.000 claims description 153
• 238000000034 method Methods 0.000 claims description 129
• 239000000203 mixture Substances 0.000 claims description 128
• 239000003910 polypeptide antibiotic agent Substances 0.000 claims description 123
• 239000012636 effector Substances 0.000 claims description 89
• 244000005700 microbiome Species 0.000 claims description 55
• 239000003504 photosensitizing agent Substances 0.000 claims description 51
• 239000003795 chemical substances by application Substances 0.000 claims description 45
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• 125000006239 protecting group Chemical group 0.000 claims description 43
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• 238000009472 formulation Methods 0.000 claims description 34
• 108020001507 fusion proteins Proteins 0.000 claims description 32
• 102000037865 fusion proteins Human genes 0.000 claims description 32
• 150000004032 porphyrins Chemical class 0.000 claims description 29
• 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 28
• 210000000214 mouth Anatomy 0.000 claims description 25
• 229920001223 polyethylene glycol Polymers 0.000 claims description 25
• 239000002202 Polyethylene glycol Substances 0.000 claims description 24
• 239000003242 anti bacterial agent Substances 0.000 claims description 23
• 239000002502 liposome Substances 0.000 claims description 22
• 230000015572 biosynthetic process Effects 0.000 claims description 20
• 150000001408 amides Chemical class 0.000 claims description 19
• 230000001580 bacterial effect Effects 0.000 claims description 19
• 229910052799 carbon Inorganic materials 0.000 claims description 18
• 241000124008 Mammalia Species 0.000 claims description 17
• 229940088710 antibiotic agent Drugs 0.000 claims description 15
• 229910052757 nitrogen Inorganic materials 0.000 claims description 15
• WTKQMHWYSBWUBE-UHFFFAOYSA-N (3-nitropyridin-2-yl) thiohypochlorite Chemical group [O-][N+](=O)C1=CC=CN=C1SCl WTKQMHWYSBWUBE-UHFFFAOYSA-N 0.000 claims description 14
• 125000004217 4-methoxybenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1OC([H])([H])[H])C([H])([H])* 0.000 claims description 14
• 241000194019 Streptococcus mutans Species 0.000 claims description 14
• 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims description 14
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• 125000002933 cyclohexyloxy group Chemical group C1(CCCCC1)O* 0.000 claims description 14
• 229910052731 fluorine Inorganic materials 0.000 claims description 14
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• 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 14
• 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 14
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• 239000003446 ligand Substances 0.000 claims description 12
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• ZCCUUQDIBDJBTK-UHFFFAOYSA-N psoralen Chemical compound C1=C2OC(=O)C=CC2=CC2=C1OC=C2 ZCCUUQDIBDJBTK-UHFFFAOYSA-N 0.000 claims description 10
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• IEQIEDJGQAUEQZ-UHFFFAOYSA-N phthalocyanine Chemical compound N1C(N=C2C3=CC=CC=C3C(N=C3C4=CC=CC=C4C(=N4)N3)=N2)=C(C=CC=C2)C2=C1N=C1C2=CC=CC=C2C4=N1 IEQIEDJGQAUEQZ-UHFFFAOYSA-N 0.000 claims description 3
• 238000007920 subcutaneous administration Methods 0.000 claims description 3
• ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims description 2
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• 210000004195 gingiva Anatomy 0.000 claims description 2
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• 125000005647 linker group Chemical group 0.000 description 74
• RUPBZQFQVRMKDG-UHFFFAOYSA-M Didecyldimethylammonium chloride Chemical compound [Cl-].CCCCCCCCCC[N+](C)(C)CCCCCCCCCC RUPBZQFQVRMKDG-UHFFFAOYSA-M 0.000 description 60
• 150000003839 salts Chemical class 0.000 description 38
• VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 30
• WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 description 28
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• LOKCTEFSRHRXRJ-UHFFFAOYSA-I dipotassium trisodium dihydrogen phosphate hydrogen phosphate dichloride Chemical compound P(=O)(O)(O)[O-].[K+].P(=O)(O)([O-])[O-].[Na+].[Na+].[Cl-].[K+].[Cl-].[Na+] LOKCTEFSRHRXRJ-UHFFFAOYSA-I 0.000 description 19
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