JP2009542229A5 - - Google Patents
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- Publication number
- JP2009542229A5 JP2009542229A5 JP2009518653A JP2009518653A JP2009542229A5 JP 2009542229 A5 JP2009542229 A5 JP 2009542229A5 JP 2009518653 A JP2009518653 A JP 2009518653A JP 2009518653 A JP2009518653 A JP 2009518653A JP 2009542229 A5 JP2009542229 A5 JP 2009542229A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- amino
- kinase
- sulfonyl
- fluorophore
- Prior art date
- 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
- -1 amino, substituted amino, aminocarbonyl Chemical group 0.000 claims description 99
- 108091000080 Phosphotransferase Proteins 0.000 claims description 88
- 102000020233 phosphotransferase Human genes 0.000 claims description 88
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims description 30
- 125000004414 alkyl thio group Chemical group 0.000 claims description 24
- 125000001072 heteroaryl group Chemical group 0.000 claims description 24
- 150000001413 amino acids Chemical class 0.000 claims description 21
- 125000000623 heterocyclic group Chemical group 0.000 claims description 20
- 125000000217 alkyl group Chemical group 0.000 claims description 16
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims description 16
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 16
- 239000002738 chelating agent Substances 0.000 claims description 14
- 108090000765 processed proteins & peptides Proteins 0.000 claims description 14
- 125000003396 thiol group Chemical class [H]S* 0.000 claims description 13
- 125000002252 acyl group Chemical group 0.000 claims description 12
- 125000004442 acylamino group Chemical group 0.000 claims description 12
- 125000004423 acyloxy group Chemical group 0.000 claims description 12
- 125000003545 alkoxy group Chemical group 0.000 claims description 12
- 125000004682 aminothiocarbonyl group Chemical group NC(=S)* 0.000 claims description 12
- 125000003118 aryl group Chemical group 0.000 claims description 12
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 12
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 12
- 125000001475 halogen functional group Chemical group 0.000 claims description 12
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 12
- 125000001820 oxy group Chemical group [*:1]O[*:2] 0.000 claims description 12
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 12
- 125000005415 substituted alkoxy group Chemical group 0.000 claims description 12
- 125000003107 substituted aryl group Chemical group 0.000 claims description 12
- 125000003441 thioacyl group Chemical group 0.000 claims description 12
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims description 8
- 230000000694 effects Effects 0.000 claims description 7
- 229910052751 metal Inorganic materials 0.000 claims description 7
- 239000002184 metal Substances 0.000 claims description 7
- GOLORTLGFDVFDW-UHFFFAOYSA-N 3-(1h-benzimidazol-2-yl)-7-(diethylamino)chromen-2-one Chemical compound C1=CC=C2NC(C3=CC4=CC=C(C=C4OC3=O)N(CC)CC)=NC2=C1 GOLORTLGFDVFDW-UHFFFAOYSA-N 0.000 claims description 6
- GJCOSYZMQJWQCA-UHFFFAOYSA-N 9H-xanthene Chemical compound C1=CC=C2CC3=CC=CC=C3OC2=C1 GJCOSYZMQJWQCA-UHFFFAOYSA-N 0.000 claims description 6
- UFWIBTONFRDIAS-UHFFFAOYSA-N Naphthalene Chemical compound C1=CC=CC2=CC=CC=C21 UFWIBTONFRDIAS-UHFFFAOYSA-N 0.000 claims description 6
- 229910052736 halogen Inorganic materials 0.000 claims description 6
- 150000002367 halogens Chemical class 0.000 claims description 6
- QDLAGTHXVHQKRE-UHFFFAOYSA-N lichenxanthone Natural products COC1=CC(O)=C2C(=O)C3=C(C)C=C(OC)C=C3OC2=C1 QDLAGTHXVHQKRE-UHFFFAOYSA-N 0.000 claims description 6
- 230000026731 phosphorylation Effects 0.000 claims description 6
- 238000006366 phosphorylation reaction Methods 0.000 claims description 6
- 125000006239 protecting group Chemical group 0.000 claims description 6
- BBEAQIROQSPTKN-UHFFFAOYSA-N pyrene Chemical compound C1=CC=C2C=CC3=CC=CC4=CC=C1C2=C43 BBEAQIROQSPTKN-UHFFFAOYSA-N 0.000 claims description 6
- 150000003839 salts Chemical class 0.000 claims description 6
- 239000011777 magnesium Substances 0.000 claims description 5
- 238000000034 method Methods 0.000 claims description 5
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 4
- BCHZICNRHXRCHY-UHFFFAOYSA-N 2h-oxazine Chemical compound N1OC=CC=C1 BCHZICNRHXRCHY-UHFFFAOYSA-N 0.000 claims description 3
- AYFVYJQAPQTCCC-GBXIJSLDSA-N L-threonine Chemical compound C[C@@H](O)[C@H](N)C(O)=O AYFVYJQAPQTCCC-GBXIJSLDSA-N 0.000 claims description 3
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 claims description 3
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 claims description 3
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 claims description 3
- AYFVYJQAPQTCCC-UHFFFAOYSA-N Threonine Natural products CC(O)C(N)C(O)=O AYFVYJQAPQTCCC-UHFFFAOYSA-N 0.000 claims description 3
- 239000004473 Threonine Substances 0.000 claims description 3
- 125000000539 amino acid group Chemical group 0.000 claims description 3
- 125000001295 dansyl group Chemical group [H]C1=C([H])C(N(C([H])([H])[H])C([H])([H])[H])=C2C([H])=C([H])C([H])=C(C2=C1[H])S(*)(=O)=O 0.000 claims description 3
- GVEPBJHOBDJJJI-UHFFFAOYSA-N fluoranthrene Natural products C1=CC(C2=CC=CC=C22)=C3C2=CC=CC3=C1 GVEPBJHOBDJJJI-UHFFFAOYSA-N 0.000 claims description 3
- 229910052749 magnesium Inorganic materials 0.000 claims description 3
- ANRHNWWPFJCPAZ-UHFFFAOYSA-M thionine Chemical compound [Cl-].C1=CC(N)=CC2=[S+]C3=CC(N)=CC=C3N=C21 ANRHNWWPFJCPAZ-UHFFFAOYSA-M 0.000 claims description 3
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 claims description 3
- 125000003088 (fluoren-9-ylmethoxy)carbonyl group Chemical group 0.000 claims description 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 2
- 229910019142 PO4 Inorganic materials 0.000 claims description 2
- 238000006243 chemical reaction Methods 0.000 claims description 2
- 230000001268 conjugating effect Effects 0.000 claims description 2
- 230000005284 excitation Effects 0.000 claims description 2
- 238000002875 fluorescence polarization Methods 0.000 claims description 2
- 229910052731 fluorine Inorganic materials 0.000 claims description 2
- 239000011737 fluorine Substances 0.000 claims description 2
- 230000001678 irradiating effect Effects 0.000 claims description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims description 2
- 239000010452 phosphate Substances 0.000 claims description 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 7
- 102000001253 Protein Kinase Human genes 0.000 claims 1
- 108060006633 protein kinase Proteins 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 8
- MTCFGRXMJLQNBG-REOHCLBHSA-N (2S)-2-Amino-3-hydroxypropansäure Chemical compound OC[C@H](N)C(O)=O MTCFGRXMJLQNBG-REOHCLBHSA-N 0.000 description 2
- 239000000758 substrate Substances 0.000 description 2
- 0 CC(C(*)C(O)=C1)C(C(N)=C2C=C3O*)=C1OC2=CC3=O Chemical compound CC(C(*)C(O)=C1)C(C(N)=C2C=C3O*)=C1OC2=CC3=O 0.000 description 1
- 125000003368 amide group Chemical group 0.000 description 1
- 125000003277 amino group Chemical group 0.000 description 1
- 125000006598 aminocarbonylamino group Chemical group 0.000 description 1
- 125000000565 sulfonamide group Chemical group 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US81943206P | 2006-07-07 | 2006-07-07 | |
| US11/624,686 US20070196860A1 (en) | 2006-01-18 | 2007-01-18 | Methods for Measuring Real Time Kinase Activity |
| PCT/US2007/073000 WO2008016762A1 (en) | 2006-07-07 | 2007-07-06 | Fluorogenic protein kinase substrates |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2009542229A JP2009542229A (ja) | 2009-12-03 |
| JP2009542229A5 true JP2009542229A5 (https=) | 2010-08-19 |
Family
ID=38919529
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009518653A Pending JP2009542229A (ja) | 2006-07-07 | 2007-07-06 | 蛍光タンパク質キナーゼ基質 |
Country Status (4)
| Country | Link |
|---|---|
| US (2) | US20070196860A1 (https=) |
| EP (1) | EP2063915A4 (https=) |
| JP (1) | JP2009542229A (https=) |
| WO (1) | WO2008016762A1 (https=) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7619059B2 (en) | 2003-07-29 | 2009-11-17 | Life Technologies Corporation | Bimolecular optical probes |
| CA2445420A1 (en) | 2003-07-29 | 2005-01-29 | Invitrogen Corporation | Kinase and phosphatase assays |
| US7727752B2 (en) | 2003-07-29 | 2010-06-01 | Life Technologies Corporation | Kinase and phosphatase assays |
| EP1670816B1 (en) * | 2003-10-08 | 2017-09-06 | Massachusetts Institute Of Technology | Fluorescence assay for kinase activity |
| US20070196860A1 (en) * | 2006-01-18 | 2007-08-23 | Invitrogen Corporation | Methods for Measuring Real Time Kinase Activity |
| US7964729B2 (en) * | 2006-08-28 | 2011-06-21 | Massachusetts Institute Of Technology | Sox-based kinase sensor |
| US20100248975A1 (en) * | 2006-12-29 | 2010-09-30 | Gunjan Tiwari | Fluorogenic peptide substrate arrays for highly multiplexed, real-time monitoring of kinase activities |
| US8440835B2 (en) * | 2007-02-26 | 2013-05-14 | Massachusetts Institute Of Technology | Environmentally sensitive fluorophores |
| WO2010027877A2 (en) * | 2008-08-26 | 2010-03-11 | Gyrasol Technologies, Inc. | Small molecule fluorescent sensors for detection of post-translational modifications and protein-protein interactions in bioassays |
| US20110046919A1 (en) * | 2009-03-02 | 2011-02-24 | Juliesta Elaine Sylvester | Method for accurate measurement of enzyme activities |
| WO2011025546A1 (en) * | 2009-08-31 | 2011-03-03 | Massachusetts Institute Of Technology | 1, 2, 3-triazole containing protein kinase sensors |
| EP2956138B1 (en) | 2013-02-15 | 2022-06-22 | Kala Pharmaceuticals, Inc. | Therapeutic compounds and uses thereof |
| US9688688B2 (en) | 2013-02-20 | 2017-06-27 | Kala Pharmaceuticals, Inc. | Crystalline forms of 4-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxyquinazolin-7-yl)oxy)-1-(2-oxa-7-azaspiro[3.5]nonan-7-yl)butan-1-one and uses thereof |
| MX368903B (es) | 2013-02-20 | 2019-10-21 | Kala Pharmaceuticals Inc | Compuestos terapéuticos y sus usos en el tratamiento de enfermedades proliferativas. |
| US9890173B2 (en) | 2013-11-01 | 2018-02-13 | Kala Pharmaceuticals, Inc. | Crystalline forms of therapeutic compounds and uses thereof |
| US9458169B2 (en) | 2013-11-01 | 2016-10-04 | Kala Pharmaceuticals, Inc. | Crystalline forms of therapeutic compounds and uses thereof |
| US20200063182A1 (en) * | 2016-05-04 | 2020-02-27 | Assayquant Technologies, Inc. | Fluorophore-based kinase sensors |
| EP3509423A4 (en) | 2016-09-08 | 2020-05-13 | Kala Pharmaceuticals, Inc. | CRYSTALLINE FORMS OF THERAPEUTIC COMPOUNDS AND USES THEREOF |
| US10336767B2 (en) | 2016-09-08 | 2019-07-02 | Kala Pharmaceuticals, Inc. | Crystalline forms of therapeutic compounds and uses thereof |
| AU2017324713B2 (en) | 2016-09-08 | 2020-08-13 | KALA BIO, Inc. | Crystalline forms of therapeutic compounds and uses thereof |
Family Cites Families (49)
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| US4603209A (en) * | 1984-09-07 | 1986-07-29 | The Regents Of The University Of California | Fluorescent indicator dyes for calcium ions |
| US4812409A (en) * | 1986-01-31 | 1989-03-14 | Eastman Kodak Company | Hydrolyzable fluorescent substrates and analytical determinations using same |
| US5569587A (en) | 1986-04-18 | 1996-10-29 | Carnegie Mellon University | Method for labeling and detecting materials employing luminescent arysulfonate cyanine dyes |
| US5268486A (en) * | 1986-04-18 | 1993-12-07 | Carnegie-Mellon Unversity | Method for labeling and detecting materials employing arylsulfonate cyanine dyes |
| US5627027A (en) | 1986-04-18 | 1997-05-06 | Carnegie Mellon University | Cyanine dyes as labeling reagents for detection of biological and other materials by luminescence methods |
| US6048982A (en) * | 1986-04-18 | 2000-04-11 | Carnegie Mellon University | Cyanine dyes as labeling reagents for detection of biological and other materials by luminescence methods |
| US4810636A (en) * | 1986-12-09 | 1989-03-07 | Miles Inc. | Chromogenic acridinone enzyme substrates |
| US4774339A (en) * | 1987-08-10 | 1988-09-27 | Molecular Probes, Inc. | Chemically reactive dipyrrometheneboron difluoride dyes |
| US4945171A (en) * | 1987-08-10 | 1990-07-31 | Molecular Probes, Inc. | Xanthene dyes having a fused (C) benzo ring |
| US4849362A (en) * | 1988-05-19 | 1989-07-18 | Smithkline Beckman Corporation | Fluorescent intracellular calcium indicators |
| US5132432A (en) * | 1989-09-22 | 1992-07-21 | Molecular Probes, Inc. | Chemically reactive pyrenyloxy sulfonic acid dyes |
| US5274113A (en) * | 1991-11-01 | 1993-12-28 | Molecular Probes, Inc. | Long wavelength chemically reactive dipyrrometheneboron difluoride dyes and conjugates |
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| US20030113711A1 (en) * | 2001-05-30 | 2003-06-19 | Blackburn Robert Kevin | Protein kinase peptide substrate determination using peptide libraries |
| US6906104B2 (en) * | 2001-06-13 | 2005-06-14 | Pharmacia & Upjohn Company | Aminediols for the treatment of Alzheimer's disease |
| US20040171034A1 (en) | 2002-05-03 | 2004-09-02 | Brian Agnew | Compositions and methods for detection and isolation of phosphorylated molecules |
| US7759459B2 (en) | 2003-01-10 | 2010-07-20 | Albert Einstein College Of Medicine Of Yeshiva University | Fluorescent assays for protein kinases |
| EP1670816B1 (en) | 2003-10-08 | 2017-09-06 | Massachusetts Institute Of Technology | Fluorescence assay for kinase activity |
| US6906194B2 (en) * | 2003-10-08 | 2005-06-14 | Massachusetts Instititue Of Technology | Fluorescence assay for kinase activity |
| US20070196860A1 (en) | 2006-01-18 | 2007-08-23 | Invitrogen Corporation | Methods for Measuring Real Time Kinase Activity |
| JP2009523452A (ja) | 2006-01-18 | 2009-06-25 | ライフ テクノロジーズ コーポレーション | キナーゼ活性を測定するための方法 |
-
2007
- 2007-01-18 US US11/624,686 patent/US20070196860A1/en not_active Abandoned
- 2007-07-06 JP JP2009518653A patent/JP2009542229A/ja active Pending
- 2007-07-06 US US11/774,554 patent/US8124368B2/en active Active
- 2007-07-06 WO PCT/US2007/073000 patent/WO2008016762A1/en not_active Ceased
- 2007-07-06 EP EP07812697A patent/EP2063915A4/en not_active Withdrawn
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