JPWO2020148530A5 - - Google Patents

Info

Publication number

JPWO2020148530A5

JPWO2020148530A5 JP2021541187A JP2021541187A JPWO2020148530A5 JP WO2020148530 A5 JPWO2020148530 A5 JP WO2020148530A5 JP 2021541187 A JP2021541187 A JP 2021541187A JP 2021541187 A JP2021541187 A JP 2021541187A JP WO2020148530 A5 JPWO2020148530 A5 JP WO2020148530A5

Authority

JP

Japan

Prior art keywords

seq

referred

peptide ligand

amino acid

sar

Prior art date

2023-01-25

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

• Espacenet
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• 108090000765 processed proteins & peptides Proteins 0.000 description 37
• 239000003446 ligand Substances 0.000 description 34
• 125000003275 alpha amino acid group Chemical group 0.000 description 21
• YBJHBAHKTGYVGT-ZKWXMUAHSA-N (+)-Biotin Chemical compound N1C(=O)N[C@@H]2[C@H](CCCCC(=O)O)SC[C@@H]21 YBJHBAHKTGYVGT-ZKWXMUAHSA-N 0.000 description 20
• 125000000151 cysteine group Chemical group N[C@@H](CS)C(=O)* 0.000 description 17
• 150000003839 salts Chemical class 0.000 description 12
• 229960002685 biotin Drugs 0.000 description 10
• 235000020958 biotin Nutrition 0.000 description 10
• 239000011616 biotin Substances 0.000 description 10
• 235000001014 amino acid Nutrition 0.000 description 9
• 150000001413 amino acids Chemical class 0.000 description 9
• QNAYBMKLOCPYGJ-UHFFFAOYSA-N D-alpha-Ala Natural products CC([NH3+])C([O-])=O QNAYBMKLOCPYGJ-UHFFFAOYSA-N 0.000 description 8
• 229940079593 drug Drugs 0.000 description 6
• 239000003814 drug Substances 0.000 description 6
• UCMIRNVEIXFBKS-UHFFFAOYSA-N beta-alanine Chemical compound NCCC(O)=O UCMIRNVEIXFBKS-UHFFFAOYSA-N 0.000 description 5
• 239000000126 substance Substances 0.000 description 5
• 101000777636 Homo sapiens ADP-ribosyl cyclase/cyclic ADP-ribose hydrolase 1 Proteins 0.000 description 4
• 125000000539 amino acid group Chemical group 0.000 description 4
• 102100031585 ADP-ribosyl cyclase/cyclic ADP-ribose hydrolase 1 Human genes 0.000 description 3
• 206010028980 Neoplasm Diseases 0.000 description 3
• WDLRUFUQRNWCPK-UHFFFAOYSA-N Tetraxetan Chemical compound OC(=O)CN1CCN(CC(O)=O)CCN(CC(O)=O)CCN(CC(O)=O)CC1 WDLRUFUQRNWCPK-UHFFFAOYSA-N 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
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
• 239000002062 molecular scaffold Substances 0.000 description 2
• GHITVUOBZBZMND-UHFFFAOYSA-N 1,3,5-tris(bromomethyl)benzene Chemical compound BrCC1=CC(CBr)=CC(CBr)=C1 GHITVUOBZBZMND-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
• OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 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
• 229930126263 Maytansine Natural products 0.000 description 1
• 241001465754 Metazoa Species 0.000 description 1
• 241000699670 Mus sp. Species 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
• 125000003118 aryl group Chemical group 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
• 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
• 102000052645 human CD38 Human genes 0.000 description 1
• WKPWGQKGSOKKOO-RSFHAFMBSA-N maytansine Chemical group CO[C@@H]([C@@]1(O)C[C@](OC(=O)N1)([C@H]([C@@H]1O[C@@]1(C)[C@@H](OC(=O)[C@H](C)N(C)C(C)=O)CC(=O)N1C)C)[H])\C=C\C=C(C)\CC2=CC(OC)=C(Cl)C1=C2 WKPWGQKGSOKKOO-RSFHAFMBSA-N 0.000 description 1
• 230000001404 mediated effect Effects 0.000 description 1
• 239000008194 pharmaceutical composition Substances 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
• 239000011734 sodium Substances 0.000 description 1
• 229910052708 sodium Inorganic materials 0.000 description 1
• 230000001629 suppression Effects 0.000 description 1
• 230000004580 weight loss Effects 0.000 description 1