JP2016513073A5 - - Google Patents

Info

Publication number

JP2016513073A5

JP2016513073A5 JP2015550762A JP2015550762A JP2016513073A5 JP 2016513073 A5 JP2016513073 A5 JP 2016513073A5 JP 2015550762 A JP2015550762 A JP 2015550762A JP 2015550762 A JP2015550762 A JP 2015550762A JP 2016513073 A5 JP2016513073 A5 JP 2016513073A5

Authority

JP

Japan

Prior art keywords

sequence

amino acid

terminal region

fgf19

peptide

Prior art date

2013-12-26

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.)

Granted

Links

• Espacenet
• Global Dossier
• Discuss

• 108090000765 processed proteins & peptides Proteins 0.000 claims 65
• 102100031734 Fibroblast growth factor 19 Human genes 0.000 claims 55
• 101000846394 Homo sapiens Fibroblast growth factor 19 Proteins 0.000 claims 55
• 210000004897 n-terminal region Anatomy 0.000 claims 47
• 125000003275 alpha amino acid group Chemical group 0.000 claims 40
• 150000001413 amino acids Chemical class 0.000 claims 27
• 210000004899 c-terminal region Anatomy 0.000 claims 24
• 102000003973 Fibroblast growth factor 21 Human genes 0.000 claims 21
• 108090000376 Fibroblast growth factor 21 Proteins 0.000 claims 21
• 125000000539 amino acid group Chemical group 0.000 claims 21
• 206010073071 hepatocellular carcinoma Diseases 0.000 claims 16
• 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 16
• HSINOMROUCMIEA-FGVHQWLLSA-N (2s,4r)-4-[(3r,5s,6r,7r,8s,9s,10s,13r,14s,17r)-6-ethyl-3,7-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-17-yl]-2-methylpentanoic acid Chemical compound C([C@@]12C)C[C@@H](O)C[C@H]1[C@@H](CC)[C@@H](O)[C@@H]1[C@@H]2CC[C@]2(C)[C@@H]([C@H](C)C[C@H](C)C(O)=O)CC[C@H]21 HSINOMROUCMIEA-FGVHQWLLSA-N 0.000 claims 15
• 239000003613 bile acid Substances 0.000 claims 15
• 230000000694 effects Effects 0.000 claims 12
• 238000012217 deletion Methods 0.000 claims 11
• 230000037430 deletion Effects 0.000 claims 11
• 102100027844 Fibroblast growth factor receptor 4 Human genes 0.000 claims 10
• 101710182387 Fibroblast growth factor receptor 4 Proteins 0.000 claims 10
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 8
• 238000006467 substitution reaction Methods 0.000 claims 8
• 208000035475 disorder Diseases 0.000 claims 7
• 230000013632 homeostatic process Effects 0.000 claims 7
• 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 7
• 108091006116 chimeric peptides Proteins 0.000 claims 6
• 239000012634 fragment Substances 0.000 claims 6
• 241001465754 Metazoa Species 0.000 claims 5
• 230000014509 gene expression Effects 0.000 claims 5
• 241000699670 Mus sp. Species 0.000 claims 4
• -1 amino acid amino acids Chemical class 0.000 claims 4
• HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims 4
• 239000003814 drug Substances 0.000 claims 4
• 238000003780 insertion Methods 0.000 claims 4
• 230000037431 insertion Effects 0.000 claims 4
• 150000002632 lipids Chemical class 0.000 claims 4
• 239000003550 marker Substances 0.000 claims 4
• 102000004196 processed proteins & peptides Human genes 0.000 claims 4
• 206010008635 Cholestasis Diseases 0.000 claims 3
• 230000015572 biosynthetic process Effects 0.000 claims 3
• 230000001965 increasing effect Effects 0.000 claims 3
• 238000004519 manufacturing process Methods 0.000 claims 3
• 238000000034 method Methods 0.000 claims 3
• 108010084469 Aldo-Keto Reductases Proteins 0.000 claims 2
• 102000005602 Aldo-Keto Reductases Human genes 0.000 claims 2
• 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims 2
• 208000033222 Biliary cirrhosis primary Diseases 0.000 claims 2
• 206010012735 Diarrhoea Diseases 0.000 claims 2
• 206010028980 Neoplasm Diseases 0.000 claims 2
• 208000012654 Primary biliary cholangitis Diseases 0.000 claims 2
• 101150041420 Slc1a2 gene Proteins 0.000 claims 2
• 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
• 230000007870 cholestasis Effects 0.000 claims 2
• 231100000359 cholestasis Toxicity 0.000 claims 2
• 235000012000 cholesterol Nutrition 0.000 claims 2
• 230000006698 induction Effects 0.000 claims 2
• 208000001024 intrahepatic cholestasis Diseases 0.000 claims 2
• 230000007872 intrahepatic cholestasis Effects 0.000 claims 2
• 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 2
• 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 2
• 229920001184 polypeptide Polymers 0.000 claims 2
• UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 claims 2
• TVZRAEYQIKYCPH-UHFFFAOYSA-N 3-(trimethylsilyl)propane-1-sulfonic acid Chemical group C[Si](C)(C)CCCS(O)(=O)=O TVZRAEYQIKYCPH-UHFFFAOYSA-N 0.000 claims 1
• 206010069703 Bile acid malabsorption Diseases 0.000 claims 1
• 206010056375 Bile duct obstruction Diseases 0.000 claims 1
• 206010009900 Colitis ulcerative Diseases 0.000 claims 1
• 206010009944 Colon cancer Diseases 0.000 claims 1
• 208000011231 Crohn disease Diseases 0.000 claims 1
• 150000008574 D-amino acids Chemical class 0.000 claims 1
• 206010016654 Fibrosis Diseases 0.000 claims 1
• 208000022072 Gallbladder Neoplasms Diseases 0.000 claims 1
• WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 1
• 206010020772 Hypertension Diseases 0.000 claims 1
• 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
• 150000008575 L-amino acids Chemical class 0.000 claims 1
• 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
• 241000699666 Mus <mouse, genus> Species 0.000 claims 1
• 206010056528 Neonatal cholestasis Diseases 0.000 claims 1
• 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
• 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
• 230000002159 abnormal effect Effects 0.000 claims 1
• 238000010521 absorption reaction Methods 0.000 claims 1
• 239000008186 active pharmaceutical agent Substances 0.000 claims 1
• WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims 1
• 210000000013 bile duct Anatomy 0.000 claims 1
• 201000011510 cancer Diseases 0.000 claims 1
• 201000001883 cholelithiasis Diseases 0.000 claims 1
• 230000007882 cirrhosis Effects 0.000 claims 1
• 208000019425 cirrhosis of liver Diseases 0.000 claims 1
• 208000029742 colonic neoplasm Diseases 0.000 claims 1
• 230000006835 compression Effects 0.000 claims 1
• 238000007906 compression Methods 0.000 claims 1
• 230000006735 deficit Effects 0.000 claims 1
• 201000010099 disease Diseases 0.000 claims 1
• 230000003828 downregulation Effects 0.000 claims 1
• 229940079593 drug Drugs 0.000 claims 1
• 208000009866 extrahepatic cholestasis Diseases 0.000 claims 1
• 208000019298 familial intrahepatic cholestasis Diseases 0.000 claims 1
• 201000010175 gallbladder cancer Diseases 0.000 claims 1
• 208000001130 gallstones Diseases 0.000 claims 1
• 239000008103 glucose Substances 0.000 claims 1
• 230000010030 glucose lowering effect Effects 0.000 claims 1
• 201000007270 liver cancer Diseases 0.000 claims 1
• 208000014018 liver neoplasm Diseases 0.000 claims 1
• 210000005228 liver tissue Anatomy 0.000 claims 1
• 230000001404 mediated effect Effects 0.000 claims 1
• 230000004060 metabolic process Effects 0.000 claims 1
• 239000008194 pharmaceutical composition Substances 0.000 claims 1
• 210000003240 portal vein Anatomy 0.000 claims 1
• 230000035935 pregnancy Effects 0.000 claims 1
• 230000000750 progressive effect Effects 0.000 claims 1
• 230000001603 reducing effect Effects 0.000 claims 1
• 238000002271 resection Methods 0.000 claims 1
• 208000010157 sclerosing cholangitis Diseases 0.000 claims 1
• 210000000813 small intestine Anatomy 0.000 claims 1
• 125000006850 spacer group Chemical group 0.000 claims 1
• 208000024891 symptom Diseases 0.000 claims 1
• 238000003786 synthesis reaction Methods 0.000 claims 1
• 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
• 230000003827 upregulation Effects 0.000 claims 1