JP2007505859A5 - - Google Patents
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- Publication number
- JP2007505859A5 JP2007505859A5 JP2006526596A JP2006526596A JP2007505859A5 JP 2007505859 A5 JP2007505859 A5 JP 2007505859A5 JP 2006526596 A JP2006526596 A JP 2006526596A JP 2006526596 A JP2006526596 A JP 2006526596A JP 2007505859 A5 JP2007505859 A5 JP 2007505859A5
- Authority
- JP
- Japan
- Prior art keywords
- pkc
- pkcθ
- gist
- evidenced
- isoforms
- 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
- 201000011243 gastrointestinal stromal tumor Diseases 0.000 description 5
- 102000001708 Protein Isoforms Human genes 0.000 description 2
- 108010029485 Protein Isoforms Proteins 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- 206010003571 Astrocytoma Diseases 0.000 description 1
- 210000000481 Breast Anatomy 0.000 description 1
- 208000000409 Breast Neoplasms Diseases 0.000 description 1
- 206010006187 Breast cancer Diseases 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- KTUFNOKKBVMGRW-UHFFFAOYSA-N Imatinib Chemical compound C1CN(C)CCN1CC1=CC=C(C(=O)NC=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)C=C1 KTUFNOKKBVMGRW-UHFFFAOYSA-N 0.000 description 1
- 239000005517 L01XE01 - Imatinib Substances 0.000 description 1
- 101700064507 MARK2 Proteins 0.000 description 1
- 102100000541 MARK2 Human genes 0.000 description 1
- 108091000081 Phosphotransferases Proteins 0.000 description 1
- 102000003923 Protein Kinase C Human genes 0.000 description 1
- 108090000315 Protein Kinase C Proteins 0.000 description 1
- 102000001253 Protein Kinases Human genes 0.000 description 1
- 210000001744 T-Lymphocytes Anatomy 0.000 description 1
- 239000000090 biomarker Substances 0.000 description 1
- 238000001574 biopsy Methods 0.000 description 1
- 230000030833 cell death Effects 0.000 description 1
- 230000024245 cell differentiation Effects 0.000 description 1
- 230000004663 cell proliferation Effects 0.000 description 1
- 210000004027 cells Anatomy 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 229960002411 imatinib Drugs 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 230000003211 malignant Effects 0.000 description 1
- 238000006366 phosphorylation reaction Methods 0.000 description 1
- 230000000865 phosphorylative Effects 0.000 description 1
- 230000019491 signal transduction Effects 0.000 description 1
- 230000011664 signaling Effects 0.000 description 1
- 239000000758 substrate Substances 0.000 description 1
- 230000004083 survival Effects 0.000 description 1
- 230000001225 therapeutic Effects 0.000 description 1
- 210000001519 tissues Anatomy 0.000 description 1
Description
タンパク質キナーゼCは、細胞シグナル伝達経路における重要な酵素の一つであり、細胞増殖および分化に中枢の役割を有する。PKCはセリン/スレオニンキナーゼのファミリーである。PKCの少なくとも12個のイソ型が同定されており、それらはそれらの構造および基質要件に基づき、一般に3群に分けられる。PKC発現は、ヒト乳房腫瘍生検サンプルで正常乳房組織と比較して上昇していることが判明しており、そして高いPKC発現は、ヒト星状細胞腫の悪性の生物学的マーカーであると見なされている。PKCイソ型の一つ、PKCθは、T細胞における生存シグナル伝達の正のレギュレーターである。興味深いことに、GISTにおけるPKCθの構成的リン酸化により明らかであり、そして、GIST細胞死をもたらすPKCθ活性の阻害により証明されるように、PKCθはGISTで活性化されている。故に、PKCθは、GISTにおける治療的介入のための標的キナーゼの可能性があると見なし得る。特に、PKC阻害剤はイマチニブ耐性GISTの処置に有利である。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US50424503P | 2003-09-19 | 2003-09-19 | |
PCT/EP2004/010467 WO2005027971A1 (en) | 2003-09-19 | 2004-09-17 | Treatment of gastrointestinal stromal tumors with imatinib and midostaurin |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2007505859A JP2007505859A (ja) | 2007-03-15 |
JP2007505859A5 true JP2007505859A5 (ja) | 2007-11-01 |
Family
ID=34375467
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2006526596A Pending JP2007505859A (ja) | 2003-09-19 | 2004-09-17 | イマチニブおよびミドスタウリンでの消化管間質腫瘍の処置 |
Country Status (11)
Country | Link |
---|---|
US (1) | US20080096864A1 (ja) |
EP (1) | EP1667719B1 (ja) |
JP (1) | JP2007505859A (ja) |
CN (1) | CN100467064C (ja) |
AT (1) | ATE489109T1 (ja) |
AU (1) | AU2004273605B2 (ja) |
BR (1) | BRPI0414527A (ja) |
CA (1) | CA2538523A1 (ja) |
DE (1) | DE602004030265D1 (ja) |
MX (1) | MXPA06003056A (ja) |
WO (1) | WO2005027971A1 (ja) |
Families Citing this family (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR101153647B1 (ko) * | 2003-11-18 | 2012-06-18 | 노파르티스 아게 | Kit 돌연변이형에 대한 저해제 |
AU2005279344B2 (en) * | 2004-08-31 | 2009-11-12 | Novartis Ag | Use of midostaurin for treating gastrointestinal stromal tumors |
RU2445960C2 (ru) * | 2005-05-02 | 2012-03-27 | Новартис Аг | Применение производных пиримидиламинобензамида для лечения системного мастоцитоза |
AU2006271652B2 (en) * | 2005-07-20 | 2010-04-29 | Peter Valent | Compositions for treatment of systemic mastocytosis |
CA2629478C (en) | 2005-11-14 | 2013-10-15 | Universitat Zurich | Staurosporine derivatives for use in alveolar rhabdomyosarcoma |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CO4940418A1 (es) * | 1997-07-18 | 2000-07-24 | Novartis Ag | Modificacion de cristal de un derivado de n-fenil-2- pirimidinamina, procesos para su fabricacion y su uso |
ITMI992711A1 (it) * | 1999-12-27 | 2001-06-27 | Novartis Ag | Composti organici |
KR100885129B1 (ko) * | 2000-10-27 | 2009-02-23 | 노파르티스 아게 | 위장관의 기질 종양의 치료 |
KR20040093058A (ko) * | 2002-02-28 | 2004-11-04 | 노파르티스 아게 | N-(5-(4-(4-메틸-피페라지노-메틸)-벤조일아미도-2-메틸페닐)-4-(3-피리딜)-2-피리미딘-아민 코팅된 스텐트 |
ATE386528T1 (de) * | 2002-04-10 | 2008-03-15 | Univ Virginia Commonwealth | Kombination von glivec (sti571) mit einem cyclinabhängigen kinaseinhibitoren, ins besonders flavopiridol, zur behandlung von krebs |
-
2004
- 2004-09-17 CN CNB2004800270630A patent/CN100467064C/zh not_active Expired - Fee Related
- 2004-09-17 JP JP2006526596A patent/JP2007505859A/ja active Pending
- 2004-09-17 DE DE602004030265T patent/DE602004030265D1/de not_active Expired - Lifetime
- 2004-09-17 MX MXPA06003056A patent/MXPA06003056A/es not_active Application Discontinuation
- 2004-09-17 WO PCT/EP2004/010467 patent/WO2005027971A1/en active Application Filing
- 2004-09-17 CA CA002538523A patent/CA2538523A1/en not_active Abandoned
- 2004-09-17 AT AT04765359T patent/ATE489109T1/de not_active IP Right Cessation
- 2004-09-17 BR BRPI0414527-5A patent/BRPI0414527A/pt not_active IP Right Cessation
- 2004-09-17 EP EP04765359A patent/EP1667719B1/en not_active Expired - Lifetime
- 2004-09-17 US US10/572,259 patent/US20080096864A1/en not_active Abandoned
- 2004-09-17 AU AU2004273605A patent/AU2004273605B2/en not_active Ceased
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