JPWO2020120984A5 - - Google Patents

Info

Publication number

JPWO2020120984A5

JPWO2020120984A5 JP2021533584A JP2021533584A JPWO2020120984A5 JP WO2020120984 A5 JPWO2020120984 A5 JP WO2020120984A5 JP 2021533584 A JP2021533584 A JP 2021533584A JP 2021533584 A JP2021533584 A JP 2021533584A JP WO2020120984 A5 JPWO2020120984 A5 JP WO2020120984A5

Authority

JP

Japan

Prior art keywords

seq

referred

lpp

loop

amino acids

Prior art date

2022-12-19

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

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• 108090000765 processed proteins & peptides Proteins 0.000 description 23
• 150000001413 amino acids Chemical class 0.000 description 20
• 239000003446 ligand Substances 0.000 description 20
• 229940024606 amino acid Drugs 0.000 description 19
• 235000001014 amino acid Nutrition 0.000 description 19
• 125000000151 cysteine group Chemical group N[C@@H](CS)C(=O)* 0.000 description 11
• 239000003814 drug Substances 0.000 description 7
• 229940079593 drug Drugs 0.000 description 6
• 239000000126 substance Substances 0.000 description 5
• FUOOLUPWFVMBKG-UHFFFAOYSA-N 2-Aminoisobutyric acid Chemical compound CC(C)(N)C(O)=O FUOOLUPWFVMBKG-UHFFFAOYSA-N 0.000 description 3
• 102000011716 Matrix Metalloproteinase 14 Human genes 0.000 description 3
• 108010076557 Matrix Metalloproteinase 14 Proteins 0.000 description 3
• 229940127089 cytotoxic agent Drugs 0.000 description 3
• 239000002254 cytotoxic agent Substances 0.000 description 3
• 231100000599 cytotoxic agent Toxicity 0.000 description 3
• 229920001184 polypeptide Polymers 0.000 description 3
• 102000004196 processed proteins & peptides Human genes 0.000 description 3
• PMMYEEVYMWASQN-DMTCNVIQSA-N Hydroxyproline Chemical compound O[C@H]1CN[C@H](C(O)=O)C1 PMMYEEVYMWASQN-DMTCNVIQSA-N 0.000 description 2
• LRQKBLKVPFOOQJ-YFKPBYRVSA-N L-norleucine Chemical compound CCCC[C@H]([NH3+])C([O-])=O LRQKBLKVPFOOQJ-YFKPBYRVSA-N 0.000 description 2
• 206010028980 Neoplasm Diseases 0.000 description 2
• IEDXPSOJFSVCKU-HOKPPMCLSA-N [4-[[(2S)-5-(carbamoylamino)-2-[[(2S)-2-[6-(2,5-dioxopyrrolidin-1-yl)hexanoylamino]-3-methylbutanoyl]amino]pentanoyl]amino]phenyl]methyl N-[(2S)-1-[[(2S)-1-[[(3R,4S,5S)-1-[(2S)-2-[(1R,2R)-3-[[(1S,2R)-1-hydroxy-1-phenylpropan-2-yl]amino]-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl]-3-methoxy-5-methyl-1-oxoheptan-4-yl]-methylamino]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-N-methylcarbamate Chemical group CC[C@H](C)[C@@H]([C@@H](CC(=O)N1CCC[C@H]1[C@H](OC)[C@@H](C)C(=O)N[C@H](C)[C@@H](O)c1ccccc1)OC)N(C)C(=O)[C@@H](NC(=O)[C@H](C(C)C)N(C)C(=O)OCc1ccc(NC(=O)[C@H](CCCNC(N)=O)NC(=O)[C@@H](NC(=O)CCCCCN2C(=O)CCC2=O)C(C)C)cc1)C(C)C IEDXPSOJFSVCKU-HOKPPMCLSA-N 0.000 description 2
• 229960003767 alanine Drugs 0.000 description 2
• 208000029618 autoimmune pulmonary alveolar proteinosis Diseases 0.000 description 2
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
• 239000002062 molecular scaffold Substances 0.000 description 2
• 239000008194 pharmaceutical composition Substances 0.000 description 2
• IYKLZBIWFXPUCS-VIFPVBQESA-N (2s)-2-(naphthalen-1-ylamino)propanoic acid Chemical compound C1=CC=C2C(N[C@@H](C)C(O)=O)=CC=CC2=C1 IYKLZBIWFXPUCS-VIFPVBQESA-N 0.000 description 1
• RWLSBXBFZHDHHX-VIFPVBQESA-N (2s)-2-(naphthalen-2-ylamino)propanoic acid Chemical compound C1=CC=CC2=CC(N[C@@H](C)C(O)=O)=CC=C21 RWLSBXBFZHDHHX-VIFPVBQESA-N 0.000 description 1
• MRTPISKDZDHEQI-YFKPBYRVSA-N (2s)-2-(tert-butylamino)propanoic acid Chemical compound OC(=O)[C@H](C)NC(C)(C)C MRTPISKDZDHEQI-YFKPBYRVSA-N 0.000 description 1
• NPDBDJFLKKQMCM-SCSAIBSYSA-N (2s)-2-amino-3,3-dimethylbutanoic acid Chemical compound CC(C)(C)[C@H](N)C(O)=O NPDBDJFLKKQMCM-SCSAIBSYSA-N 0.000 description 1
• SRGOJUDAJKUDAZ-LURJTMIESA-N (2s)-2-amino-3-cyclobutylpropanoic acid Chemical group OC(=O)[C@@H](N)CC1CCC1 SRGOJUDAJKUDAZ-LURJTMIESA-N 0.000 description 1
• BQQGAGGSEMLWRS-UHFFFAOYSA-N (4-aminophenyl)methyl carbamate Chemical compound NC(=O)OCC1=CC=C(N)C=C1 BQQGAGGSEMLWRS-UHFFFAOYSA-N 0.000 description 1
• UKAUYVFTDYCKQA-UHFFFAOYSA-N -2-Amino-4-hydroxybutanoic acid Natural products OC(=O)C(N)CCO UKAUYVFTDYCKQA-UHFFFAOYSA-N 0.000 description 1
• GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 description 1
• LDRFQSZFVGJGGP-GSVOUGTGSA-N 3-hydroxy-L-valine Chemical compound CC(C)(O)[C@H](N)C(O)=O LDRFQSZFVGJGGP-GSVOUGTGSA-N 0.000 description 1
• XWHHYOYVRVGJJY-QMMMGPOBSA-N 4-fluoro-L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(F)C=C1 XWHHYOYVRVGJJY-QMMMGPOBSA-N 0.000 description 1
• ODKSFYDXXFIFQN-UHFFFAOYSA-N Arginine Chemical compound OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 description 1
• OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 1
• 101001011906 Homo sapiens Matrix metalloproteinase-14 Proteins 0.000 description 1
• DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 1
• QUOGESRFPZDMMT-UHFFFAOYSA-N L-Homoarginine Natural products OC(=O)C(N)CCCCNC(N)=N QUOGESRFPZDMMT-UHFFFAOYSA-N 0.000 description 1
• QUOGESRFPZDMMT-YFKPBYRVSA-N L-homoarginine Chemical compound OC(=O)[C@@H](N)CCCCNC(N)=N QUOGESRFPZDMMT-YFKPBYRVSA-N 0.000 description 1
• UKAUYVFTDYCKQA-VKHMYHEASA-N L-homoserine Chemical group OC(=O)[C@@H](N)CCO UKAUYVFTDYCKQA-VKHMYHEASA-N 0.000 description 1
• HXEACLLIILLPRG-YFKPBYRVSA-N L-pipecolic acid Chemical compound [O-]C(=O)[C@@H]1CCCC[NH2+]1 HXEACLLIILLPRG-YFKPBYRVSA-N 0.000 description 1
• ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 1
• 239000002253 acid Substances 0.000 description 1
• 150000003863 ammonium salts Chemical class 0.000 description 1
• 230000000259 anti-tumor effect Effects 0.000 description 1
• 239000011575 calcium Substances 0.000 description 1
• 229910052791 calcium Inorganic materials 0.000 description 1
• 201000010099 disease Diseases 0.000 description 1
• 208000035475 disorder Diseases 0.000 description 1
• PMMYEEVYMWASQN-UHFFFAOYSA-N dl-hydroxyproline Natural products OC1C[NH2+]C(C([O-])=O)C1 PMMYEEVYMWASQN-UHFFFAOYSA-N 0.000 description 1
• 231100000673 dose–response relationship Toxicity 0.000 description 1
• 239000012636 effector Substances 0.000 description 1
• 125000000524 functional group Chemical group 0.000 description 1
• 102000056429 human MMP14 Human genes 0.000 description 1
• 229960002591 hydroxyproline Drugs 0.000 description 1
• HXEACLLIILLPRG-RXMQYKEDSA-N l-pipecolic acid Natural products OC(=O)[C@H]1CCCCN1 HXEACLLIILLPRG-RXMQYKEDSA-N 0.000 description 1
• 230000001404 mediated effect Effects 0.000 description 1
• 239000000546 pharmaceutical excipient Substances 0.000 description 1
• 239000011591 potassium Substances 0.000 description 1
• 229910052700 potassium Inorganic materials 0.000 description 1
• 230000002265 prevention Effects 0.000 description 1
• 150000003839 salts Chemical class 0.000 description 1
• 239000011734 sodium Substances 0.000 description 1
• 229910052708 sodium Inorganic materials 0.000 description 1
• 230000001629 suppression Effects 0.000 description 1
• 229940124597 therapeutic agent Drugs 0.000 description 1
• FGMPLJWBKKVCDB-UHFFFAOYSA-N trans-L-hydroxy-proline Natural products ON1CCCC1C(O)=O FGMPLJWBKKVCDB-UHFFFAOYSA-N 0.000 description 1
• ORQXBVXKBGUSBA-QMMMGPOBSA-N β-cyclohexyl-alanine Chemical group OC(=O)[C@@H](N)CC1CCCCC1 ORQXBVXKBGUSBA-QMMMGPOBSA-N 0.000 description 1