JP2019501363A5 - - Google Patents
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- Publication number
- JP2019501363A5 JP2019501363A5 JP2018516113A JP2018516113A JP2019501363A5 JP 2019501363 A5 JP2019501363 A5 JP 2019501363A5 JP 2018516113 A JP2018516113 A JP 2018516113A JP 2018516113 A JP2018516113 A JP 2018516113A JP 2019501363 A5 JP2019501363 A5 JP 2019501363A5
- Authority
- JP
- Japan
- Prior art keywords
- cysteine
- protein
- reactive probe
- moiety
- reactive
- 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.)
- Granted
Links
- 238000000034 method Methods 0.000 claims 27
- 235000018102 proteins Nutrition 0.000 claims 18
- 108090000623 proteins and genes Proteins 0.000 claims 18
- 102000004169 proteins and genes Human genes 0.000 claims 18
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 claims 14
- 235000018417 cysteine Nutrition 0.000 claims 14
- 239000000523 sample Substances 0.000 claims 13
- 150000003384 small molecules Chemical group 0.000 claims 10
- 210000004027 cell Anatomy 0.000 claims 5
- 125000000151 cysteine group Chemical group N[C@@H](CS)C(=O)* 0.000 claims 4
- -1 N-hydroxysuccinimide (NHS) ester Chemical class 0.000 claims 3
- JVJFIQYAHPMBBX-UHFFFAOYSA-N 4-hydroxynonenal Chemical compound CCCCCC(O)C=CC=O JVJFIQYAHPMBBX-UHFFFAOYSA-N 0.000 claims 2
- 150000001345 alkine derivatives Chemical group 0.000 claims 2
- 238000004458 analytical method Methods 0.000 claims 2
- 230000005764 inhibitory process Effects 0.000 claims 2
- 239000003446 ligand Substances 0.000 claims 2
- 125000003396 thiol group Chemical group [H]S* 0.000 claims 2
- VHRUMKCAEVRUBK-GODQJPCRSA-N 15-deoxy-Delta(12,14)-prostaglandin J2 Chemical compound CCCCC\C=C\C=C1/[C@@H](C\C=C/CCCC(O)=O)C=CC1=O VHRUMKCAEVRUBK-GODQJPCRSA-N 0.000 claims 1
- 102000004506 Blood Proteins Human genes 0.000 claims 1
- 108010017384 Blood Proteins Proteins 0.000 claims 1
- 108010078791 Carrier Proteins Proteins 0.000 claims 1
- 108091006146 Channels Proteins 0.000 claims 1
- 102000034573 Channels Human genes 0.000 claims 1
- 108090000790 Enzymes Proteins 0.000 claims 1
- 102000004190 Enzymes Human genes 0.000 claims 1
- PEEHTFAAVSWFBL-UHFFFAOYSA-N Maleimide Chemical compound O=C1NC(=O)C=C1 PEEHTFAAVSWFBL-UHFFFAOYSA-N 0.000 claims 1
- 102000006404 Mitochondrial Proteins Human genes 0.000 claims 1
- 108010058682 Mitochondrial Proteins Proteins 0.000 claims 1
- 108010006519 Molecular Chaperones Proteins 0.000 claims 1
- 108091005764 adaptor proteins Proteins 0.000 claims 1
- 102000035181 adaptor proteins Human genes 0.000 claims 1
- HAXFWIACAGNFHA-UHFFFAOYSA-N aldrithiol Chemical compound C=1C=CC=NC=1SSC1=CC=CC=N1 HAXFWIACAGNFHA-UHFFFAOYSA-N 0.000 claims 1
- 150000001336 alkenes Chemical class 0.000 claims 1
- 125000005262 alkoxyamine group Chemical group 0.000 claims 1
- 150000001540 azides Chemical class 0.000 claims 1
- 150000001718 carbodiimides Chemical class 0.000 claims 1
- 210000004292 cytoskeleton Anatomy 0.000 claims 1
- AFOSIXZFDONLBT-UHFFFAOYSA-N divinyl sulfone Chemical compound C=CS(=O)(=O)C=C AFOSIXZFDONLBT-UHFFFAOYSA-N 0.000 claims 1
- 125000005179 haloacetyl group Chemical group 0.000 claims 1
- 238000011065 in-situ storage Methods 0.000 claims 1
- 230000003993 interaction Effects 0.000 claims 1
- IQPQWNKOIGAROB-UHFFFAOYSA-N isocyanate group Chemical group [N-]=C=O IQPQWNKOIGAROB-UHFFFAOYSA-N 0.000 claims 1
- 238000002372 labelling Methods 0.000 claims 1
- 238000004949 mass spectrometry Methods 0.000 claims 1
- RDBMUARQWLPMNW-UHFFFAOYSA-N phosphanylmethanol Chemical compound OCP RDBMUARQWLPMNW-UHFFFAOYSA-N 0.000 claims 1
- 238000000575 proteomic method Methods 0.000 claims 1
- 108091006024 signal transducing proteins Proteins 0.000 claims 1
- 102000034285 signal transducing proteins Human genes 0.000 claims 1
- GWIKYPMLNBTJHR-UHFFFAOYSA-M thiosulfonate group Chemical group S(=S)(=O)[O-] GWIKYPMLNBTJHR-UHFFFAOYSA-M 0.000 claims 1
- 238000013518 transcription Methods 0.000 claims 1
- 230000035897 transcription Effects 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562244881P | 2015-10-22 | 2015-10-22 | |
| US62/244,881 | 2015-10-22 | ||
| US201662345710P | 2016-06-03 | 2016-06-03 | |
| US62/345,710 | 2016-06-03 | ||
| PCT/US2016/058308 WO2017070611A1 (en) | 2015-10-22 | 2016-10-21 | Cysteine reactive probes and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019501363A JP2019501363A (ja) | 2019-01-17 |
| JP2019501363A5 true JP2019501363A5 (https=) | 2020-01-30 |
| JP6953400B2 JP6953400B2 (ja) | 2021-10-27 |
Family
ID=58558160
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018516113A Active JP6953400B2 (ja) | 2015-10-22 | 2016-10-21 | システイン反応性プローブとその使用 |
Country Status (5)
| Country | Link |
|---|---|
| US (2) | US10670605B2 (https=) |
| EP (1) | EP3365686A4 (https=) |
| JP (1) | JP6953400B2 (https=) |
| CA (1) | CA3001847A1 (https=) |
| WO (1) | WO2017070611A1 (https=) |
Families Citing this family (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10782295B2 (en) | 2013-08-13 | 2020-09-22 | The Scripps Research Institute | Cysteine-reactive ligand discovery in proteomes |
| EP3365686A4 (en) | 2015-10-22 | 2019-03-27 | The Scripps Research Institute | REACTIVE CYSTEINSONS AND USES THEREOF |
| KR102444509B1 (ko) | 2016-05-18 | 2022-09-19 | 미라티 테라퓨틱스, 인크. | Kras g12c 억제제 |
| US20190216893A1 (en) * | 2016-06-03 | 2019-07-18 | The Scripps Research Institute | Compositions and methods of modulating immune response |
| US11535597B2 (en) | 2017-01-18 | 2022-12-27 | The Scripps Research Institute | Photoreactive ligands and uses thereof |
| WO2018144869A1 (en) * | 2017-02-03 | 2018-08-09 | The Regents Of The University Of California | Compositons and methods for modulating uba5 |
| MX2019009199A (es) * | 2017-02-03 | 2019-10-21 | Univ California | Composiciones y métodos para modular ppp2r1a. |
| MX2019009200A (es) * | 2017-02-03 | 2019-10-21 | Univ California | Composiciones y métodos para inhibir el reticulón 4. |
| US20200239530A1 (en) * | 2017-09-27 | 2020-07-30 | Vividion Therapeutics, Inc. | Compounds and methods of modulating protein degradation |
| WO2019067741A1 (en) * | 2017-09-27 | 2019-04-04 | The Scripps Research Institute | CONJUGATED PROTEINS AND USES THEREOF |
| EP3694528A4 (en) | 2017-10-13 | 2021-07-28 | The Regents of the University of California | MTORC1 MODULATORS |
| US10647715B2 (en) | 2017-11-15 | 2020-05-12 | Mirati Therapeutics, Inc. | KRas G12C inhibitors |
| LT3710439T (lt) | 2017-11-15 | 2023-05-10 | Mirati Therapeutics, Inc. | Kras g12c inhibitoriai |
| CN111698986B (zh) * | 2017-12-11 | 2023-02-03 | 广州君赫生物科技有限公司 | 双硫仑的新应用 |
| WO2019217307A1 (en) | 2018-05-07 | 2019-11-14 | Mirati Therapeutics, Inc. | Kras g12c inhibitors |
| EP3849537B1 (en) | 2018-09-10 | 2024-10-23 | Mirati Therapeutics, Inc. | Combination therapies |
| EA202190749A1 (ru) | 2018-09-10 | 2021-07-09 | Мирати Терапьютикс, Инк. | Способы комбинированной терапии |
| JP2022500385A (ja) | 2018-09-10 | 2022-01-04 | ミラティ セラピューティクス， インコーポレイテッド | 組み合わせ療法 |
| EP3849535A4 (en) | 2018-09-10 | 2022-06-29 | Mirati Therapeutics, Inc. | Combination therapies |
| MX2021002804A (es) | 2018-12-05 | 2021-07-15 | Mirati Therapeutics Inc | Terapias de combinacion. |
| EP3908283A4 (en) | 2019-01-10 | 2022-10-12 | Mirati Therapeutics, Inc. | KRAS G12C INHIBITORS |
| US12366579B2 (en) | 2019-03-21 | 2025-07-22 | University Of Virginia Patent Foundation | Sulfur-heterocycle exchange chemistry and uses thereof |
| CA3148610A1 (en) * | 2019-08-05 | 2021-02-11 | Bridgene Biosciences, Inc. | Method for proteome-wide discovery of covalent ligands and compositions thereof |
| MX2022002465A (es) | 2019-08-29 | 2022-05-19 | Mirati Therapeutics Inc | Inhibidores de kras g12d. |
| WO2021061749A1 (en) | 2019-09-24 | 2021-04-01 | Mirati Therapeutics, Inc. | Combination therapies |
| US20230236170A1 (en) * | 2019-10-15 | 2023-07-27 | Jnana Therapeutics Inc. | Reactive affinity probe-interaction discovery platform |
| EP4045043A4 (en) * | 2019-10-16 | 2023-11-08 | Vividion Therapeutics, Inc. | COMPOUNDS AND METHODS FOR MODULATING IMMUNE PROTEINS |
| WO2021076755A1 (en) * | 2019-10-16 | 2021-04-22 | The Scripps Research Institute | An activity-guide map of electrophile-cysteine interactions in primary human immune cells |
| CN111063389B (zh) * | 2019-12-04 | 2021-10-29 | 浙江工业大学 | 一种基于深度卷积神经网络的配体绑定残基预测方法 |
| PH12022551513A1 (en) | 2019-12-20 | 2023-04-24 | Mirati Therapeutics Inc | Sos1 inhibitors |
| EP4210833A4 (en) | 2020-09-11 | 2024-09-11 | Mirati Therapeutics, Inc. | CRYSTALLINE FORMS OF A KRAS G12C INHIBITOR |
| CN112255396A (zh) * | 2020-10-15 | 2021-01-22 | 南开大学 | 一种测量小分子药物抑制蛋白核酸互作的单分子力学方法 |
| JP2023553492A (ja) | 2020-12-15 | 2023-12-21 | ミラティ セラピューティクス， インコーポレイテッド | アザキナゾリン汎ＫＲａｓ阻害剤 |
| EP4262803A4 (en) | 2020-12-16 | 2025-03-12 | Mirati Therapeutics, Inc. | Tetrahydropyridopyrimidine pan-kras inhibitors |
| WO2022240966A1 (en) * | 2021-05-11 | 2022-11-17 | Opna Immuno-Oncology Sa | Compounds and methods for yap/tead modulation and indications therefor |
| WO2023092133A1 (en) * | 2021-11-22 | 2023-05-25 | The Scripps Research Institute | Stereoselective covalent ligands for oncogenic and immunological proteins |
| US20260079154A1 (en) * | 2022-09-12 | 2026-03-19 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Composition, device, system, and methods for detecting environmental toxicants |
| US20260103438A1 (en) * | 2022-09-28 | 2026-04-16 | The General Hospital Corporation | Probes and methods to identify ligandable fatty acylation sites for therapeutic target identification |
| CN116790698B (zh) * | 2023-06-21 | 2024-06-18 | 南京大学 | 基于氧化脱羧酶的硫醛合成方法及其应用 |
| WO2025182683A1 (ja) * | 2024-02-29 | 2025-09-04 | 国立大学法人 東京大学 | タンパク質の活性／反応性部位の、活性／反応性の評価方法 |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6344330B1 (en) | 1998-03-27 | 2002-02-05 | The Regents Of The University Of California | Pharmacophore recombination for the identification of small molecule drug lead compounds |
| WO2000077184A1 (en) * | 1999-06-10 | 2000-12-21 | Pharmacia & Upjohn Company | Caspase-8 crystals, models and methods |
| CA2430234C (en) * | 2000-11-21 | 2008-02-12 | Sunesis Pharmaceuticals, Inc. | An extended tethering approach for rapid identification of ligands |
| WO2005118833A2 (en) | 2004-06-01 | 2005-12-15 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with sterile-alpha motif and leucine zipper containing kinase (zak) |
| US7935479B2 (en) | 2004-07-19 | 2011-05-03 | Cell Biosciences, Inc. | Methods and devices for analyte detection |
| US8314215B2 (en) * | 2006-08-04 | 2012-11-20 | The Board Of Trustees Of The Leland Stanford Junior University | Mild chemically cleavable linker system |
| EP2060563A4 (en) * | 2006-09-08 | 2010-12-22 | Dainippon Sumitomo Pharma Co | CYCLIC AMINO ALKYL CY CARBOXYL AMIDE DERIVATIVE |
| JP2010505868A (ja) | 2006-10-02 | 2010-02-25 | ザ スクリプス リサーチ インスティチュート | エーテル脂質シグナル伝達経路を制御する酵素 |
| CN101219219B (zh) * | 2007-01-10 | 2013-02-13 | 北京普罗吉生物科技发展有限公司 | 包含血管抑素或其片段的复合物、其制备方法及应用 |
| EP1947193A1 (en) | 2007-01-17 | 2008-07-23 | Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. | Screening method for anti-diabetic compounds |
| CA2679643A1 (en) * | 2007-03-09 | 2008-09-18 | The University Of British Columbia | Procaspase 8-mediated disease targeting |
| EP2254574A1 (en) * | 2008-02-26 | 2010-12-01 | Ludwig-Maximilians-Universität München | Beta-lactones as antibacterial agents |
| US9907828B2 (en) * | 2012-06-22 | 2018-03-06 | The University Of Vermont And State Agricultural College | Treatments of oxidative stress conditions |
| US20140357512A1 (en) | 2013-06-03 | 2014-12-04 | Acetylon Pharmaceuticals, Inc. | Histone deacetylase (hdac) biomarkers in multiple myeloma |
| US10782295B2 (en) | 2013-08-13 | 2020-09-22 | The Scripps Research Institute | Cysteine-reactive ligand discovery in proteomes |
| EP3182971A4 (en) | 2014-08-21 | 2018-04-25 | SRX Cardio, LLC | Composition and methods of use of small molecules as binding ligands for the modulation of proprotein convertase subtilisin/kexin type 9(pcsk9) protein activity |
| EP3365686A4 (en) * | 2015-10-22 | 2019-03-27 | The Scripps Research Institute | REACTIVE CYSTEINSONS AND USES THEREOF |
| US11535597B2 (en) | 2017-01-18 | 2022-12-27 | The Scripps Research Institute | Photoreactive ligands and uses thereof |
-
2016
- 2016-10-21 EP EP16858391.2A patent/EP3365686A4/en not_active Withdrawn
- 2016-10-21 JP JP2018516113A patent/JP6953400B2/ja active Active
- 2016-10-21 US US15/331,745 patent/US10670605B2/en active Active
- 2016-10-21 WO PCT/US2016/058308 patent/WO2017070611A1/en not_active Ceased
- 2016-10-21 CA CA3001847A patent/CA3001847A1/en active Pending
-
2020
- 2020-06-02 US US16/890,966 patent/US20200292555A1/en not_active Abandoned
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