JP2014503180A5 - - Google Patents

Info

Publication number

JP2014503180A5

JP2014503180A5 JP2013532905A JP2013532905A JP2014503180A5 JP 2014503180 A5 JP2014503180 A5 JP 2014503180A5 JP 2013532905 A JP2013532905 A JP 2013532905A JP 2013532905 A JP2013532905 A JP 2013532905A JP 2014503180 A5 JP2014503180 A5 JP 2014503180A5

Authority

JP

Japan

Prior art keywords

amino acid

smo

protein

mutant

mutant smo

Prior art date

2011-10-05

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

• 235000001014 amino acid Nutrition 0.000 claims description 36
• 150000001413 amino acids Chemical class 0.000 claims description 31
• 150000001875 compounds Chemical class 0.000 claims description 25
• 238000000034 method Methods 0.000 claims description 24
• 150000007523 nucleic acids Chemical class 0.000 claims description 19
• 239000000523 sample Substances 0.000 claims description 18
• 230000035772 mutation Effects 0.000 claims description 17
• 108020004707 nucleic acids Proteins 0.000 claims description 16
• 102000039446 nucleic acids Human genes 0.000 claims description 16
• WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 claims description 13
• 235000013922 glutamic acid Nutrition 0.000 claims description 13
• 239000004220 glutamic acid Substances 0.000 claims description 13
• 101150056682 Smo gene Proteins 0.000 claims description 12
• 239000012634 fragment Substances 0.000 claims description 12
• 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 description 10
• 206010028980 Neoplasm Diseases 0.000 claims description 10
• 108020004711 Nucleic Acid Probes Proteins 0.000 claims description 7
• 239000003112 inhibitor Substances 0.000 claims description 7
• 239000002853 nucleic acid probe Substances 0.000 claims description 7
• 230000000694 effects Effects 0.000 claims description 6
• 125000000291 glutamic acid group Chemical group N[C@@H](CCC(O)=O)C(=O)* 0.000 claims description 5
• BPQMGSKTAYIVFO-UHFFFAOYSA-N vismodegib Chemical compound ClC1=CC(S(=O)(=O)C)=CC=C1C(=O)NC1=CC=C(Cl)C(C=2N=CC=CC=2)=C1 BPQMGSKTAYIVFO-UHFFFAOYSA-N 0.000 claims description 5
• 229960004449 vismodegib Drugs 0.000 claims description 5
• 210000004027 cell Anatomy 0.000 claims description 4
• 235000018102 proteins Nutrition 0.000 claims description 4
• 108090000623 proteins and genes Proteins 0.000 claims description 4
• 102000004169 proteins and genes Human genes 0.000 claims description 4
• QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 claims description 3
• KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims description 3
• 239000004472 Lysine Substances 0.000 claims description 3
• 235000004279 alanine Nutrition 0.000 claims description 3
• 201000011510 cancer Diseases 0.000 claims description 3
• 238000012216 screening Methods 0.000 claims description 3
• 239000012828 PI3K inhibitor Substances 0.000 claims description 2
• 239000000427 antigen Substances 0.000 claims description 2
• 102000036639 antigens Human genes 0.000 claims description 2
• 108091007433 antigens Proteins 0.000 claims description 2
• 210000004899 c-terminal region Anatomy 0.000 claims description 2
• 229940127089 cytotoxic agent Drugs 0.000 claims description 2
• 239000002254 cytotoxic agent Substances 0.000 claims description 2
• 231100000599 cytotoxic agent Toxicity 0.000 claims description 2
• 238000009396 hybridization Methods 0.000 claims description 2
• 229940043441 phosphoinositide 3-kinase inhibitor Drugs 0.000 claims description 2
• 125000003275 alpha amino acid group Chemical group 0.000 claims 16
• 229940079593 drug Drugs 0.000 claims 1
• 239000003814 drug Substances 0.000 claims 1
• 230000011664 signaling Effects 0.000 claims 1
• 108091028043 Nucleic acid sequence Proteins 0.000 description 3
• 230000019491 signal transduction Effects 0.000 description 2
• 230000003321 amplification Effects 0.000 description 1
• 230000000692 anti-sense effect Effects 0.000 description 1
• 230000000295 complement effect Effects 0.000 description 1
• 238000003199 nucleic acid amplification method Methods 0.000 description 1
• 239000002773 nucleotide Substances 0.000 description 1
• 125000003729 nucleotide group Chemical group 0.000 description 1
• 229920002401 polyacrylamide Polymers 0.000 description 1