JP2009254375A5 - - Google Patents

Info

Publication number

JP2009254375A5

JP2009254375A5 JP2009170623A JP2009170623A JP2009254375A5 JP 2009254375 A5 JP2009254375 A5 JP 2009254375A5 JP 2009170623 A JP2009170623 A JP 2009170623A JP 2009170623 A JP2009170623 A JP 2009170623A JP 2009254375 A5 JP2009254375 A5 JP 2009254375A5

Authority

JP

Japan

Prior art keywords

gpcr

compound

test compound

bone mass

seq

Prior art date

2009-07-21

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.)

Withdrawn

Links

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• 150000001875 compounds Chemical class 0.000 claims 95
• 102000003688 G-Protein-Coupled Receptors Human genes 0.000 claims 65
• 108090000045 G-Protein-Coupled Receptors Proteins 0.000 claims 65
• 210000000988 bone and bone Anatomy 0.000 claims 46
• 238000000034 method Methods 0.000 claims 37
• 210000004027 cell Anatomy 0.000 claims 34
• 241000251539 Vertebrata <Metazoa> Species 0.000 claims 30
• 102100034154 Guanine nucleotide-binding protein G(i) subunit alpha-2 Human genes 0.000 claims 28
• 125000003275 alpha amino acid group Chemical group 0.000 claims 24
• AJJISMLYIMQAKP-OAHLLOKOSA-N 5-[4-[(2r)-4-(3-fluoro-4-methylsulfonylphenoxy)butan-2-yl]piperidin-1-yl]-3-propan-2-yl-1,2,4-oxadiazole Chemical compound CC(C)C1=NOC(N2CCC(CC2)[C@H](C)CCOC=2C=C(F)C(=CC=2)S(C)(=O)=O)=N1 AJJISMLYIMQAKP-OAHLLOKOSA-N 0.000 claims 23
• 229940100607 GPR119 agonist Drugs 0.000 claims 23
• 150000001413 amino acids Chemical class 0.000 claims 21
• FWMNVWWHGCHHJJ-SKKKGAJSSA-N 4-amino-1-[(2r)-6-amino-2-[[(2r)-2-[[(2r)-2-[[(2r)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]piperidine-4-carboxylic acid Chemical compound C([C@H](C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCCCN)C(=O)N1CCC(N)(CC1)C(O)=O)NC(=O)[C@H](N)CC=1C=CC=CC=1)C1=CC=CC=C1 FWMNVWWHGCHHJJ-SKKKGAJSSA-N 0.000 claims 17
• 102000040430 polynucleotide Human genes 0.000 claims 17
• 108091033319 polynucleotide Proteins 0.000 claims 17
• 239000002157 polynucleotide Substances 0.000 claims 17
• 238000003752 polymerase chain reaction Methods 0.000 claims 14
• 102000005962 receptors Human genes 0.000 claims 14
• 108020003175 receptors Proteins 0.000 claims 14
• 210000003158 enteroendocrine cell Anatomy 0.000 claims 13
• 230000003248 secreting effect Effects 0.000 claims 12
• 238000000338 in vitro Methods 0.000 claims 9
• 230000028327 secretion Effects 0.000 claims 8
• 101710163236 Glucose-dependent insulinotropic receptor Proteins 0.000 claims 7
• 102100033839 Glucose-dependent insulinotropic receptor Human genes 0.000 claims 7
• 238000007792 addition Methods 0.000 claims 7
• 239000000556 agonist Substances 0.000 claims 7
• 230000000295 complement effect Effects 0.000 claims 7
• 238000012217 deletion Methods 0.000 claims 7
• 230000037430 deletion Effects 0.000 claims 7
• 239000003446 ligand Substances 0.000 claims 7
• 238000006467 substitution reaction Methods 0.000 claims 7
• 239000013604 expression vector Substances 0.000 claims 6
• 239000012528 membrane Substances 0.000 claims 5
• 150000003384 small molecules Chemical class 0.000 claims 5
• 101000957724 Catostomus commersonii Corticoliberin-1 Proteins 0.000 claims 4
• IVOMOUWHDPKRLL-KQYNXXCUSA-N Cyclic adenosine monophosphate Chemical group C([C@H]1O2)OP(O)(=O)O[C@H]1[C@@H](O)[C@@H]2N1C(N=CN=C2N)=C2N=C1 IVOMOUWHDPKRLL-KQYNXXCUSA-N 0.000 claims 3
• IVOMOUWHDPKRLL-UHFFFAOYSA-N UNPD107823 Natural products O1C2COP(O)(=O)OC2C(O)C1N1C(N=CN=C2N)=C2N=C1 IVOMOUWHDPKRLL-UHFFFAOYSA-N 0.000 claims 3
• 229940095074 cyclic amp Drugs 0.000 claims 3
• 210000003574 melanophore Anatomy 0.000 claims 3
• ZOOGRGPOEVQQDX-UUOKFMHZSA-N 3',5'-cyclic GMP Chemical compound C([C@H]1O2)OP(O)(=O)O[C@H]1[C@@H](O)[C@@H]2N1C(N=C(NC2=O)N)=C2N=C1 ZOOGRGPOEVQQDX-UUOKFMHZSA-N 0.000 claims 2
• 101000996752 Homo sapiens Glucose-dependent insulinotropic receptor Proteins 0.000 claims 2
• 102100033115 Mitogen-activated protein kinase kinase kinase 1 Human genes 0.000 claims 2
• 101710164423 Mitogen-activated protein kinase kinase kinase 1 Proteins 0.000 claims 2
• 240000004808 Saccharomyces cerevisiae Species 0.000 claims 2
• 238000003556 assay Methods 0.000 claims 2
• ZOOGRGPOEVQQDX-UHFFFAOYSA-N cyclic GMP Natural products O1C2COP(O)(=O)OC2C(O)C1N1C=NC2=C1NC(N)=NC2=O ZOOGRGPOEVQQDX-UHFFFAOYSA-N 0.000 claims 2
• 150000001982 diacylglycerols Chemical class 0.000 claims 2
• 230000000694 effects Effects 0.000 claims 2
• 102000056352 human GPR119 Human genes 0.000 claims 2
• 102000043136 MAP kinase family Human genes 0.000 claims 1
• 108091054455 MAP kinase family Proteins 0.000 claims 1
• MMWCIQZXVOZEGG-HOZKJCLWSA-N [(1S,2R,3S,4S,5R,6S)-2,3,5-trihydroxy-4,6-diphosphonooxycyclohexyl] dihydrogen phosphate Chemical compound O[C@H]1[C@@H](O)[C@H](OP(O)(O)=O)[C@@H](OP(O)(O)=O)[C@H](O)[C@H]1OP(O)(O)=O MMWCIQZXVOZEGG-HOZKJCLWSA-N 0.000 claims 1
• 210000000170 cell membrane Anatomy 0.000 claims 1
• 210000003890 endocrine cell Anatomy 0.000 claims 1
• 230000000968 intestinal effect Effects 0.000 claims 1
• 102000004169 proteins and genes Human genes 0.000 claims 1
• 108090000623 proteins and genes Proteins 0.000 claims 1
• XOFLBQFBSOEHOG-UUOKFMHZSA-N γS-GTP Chemical compound C1=2NC(N)=NC(=O)C=2N=CN1[C@@H]1O[C@H](COP(O)(=O)OP(O)(=O)OP(O)(O)=S)[C@@H](O)[C@H]1O XOFLBQFBSOEHOG-UUOKFMHZSA-N 0.000 claims 1