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학술연구/단체지원/교육 등 연구자 활동을 지속하도록 DBpia가 지원하고 있어요.
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논문 기본 정보
- 자료유형
- 학술저널
- 저자정보
- 발행연도
- 2019.1
- 수록면
- 311 - 317 (7page)
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초록· 키워드
오류제보하기
Mast cells are the most prominent effector cells of Type 1 hypersensitivity immune responses. CYC116 [4-(2-amino-4-methyl-1,3-thiazol-5-yl)-N-[4-(morpholin-4-yl)phenyl] pyrimidin-2-amine] is under development to be used as an anti-cancer drug, but the inhibitory effects of CYC116 on the activation of mast cells and related allergy diseases have not reported as of yet. In this study, we demonstrated, for the first time, that CYC116 inhibited the degranulation of mast cells by antigen stimulation ($IC_{50}$, ${\sim}1.42{\mu}M$). CYC116 also inhibited the secretion of pro-inflammatory cytokines including TNF-${\alpha}$ ($IC_{50}$, ${\sim}1.10{\mu}M$), and IL-6 ($IC_{50}$, ${\sim}1.24{\mu}M$). CYC116 inhibited the mast cell-mediated allergic responses, passive cutaneous anaphylaxis (ED50, ~22.5 mg/kg), and passive systemic anaphylaxis in a dose-dependent manner in laboratory experiments performed on mice. Specifically, CYC116 inhibited the activity of Fyn in mast cells and inhibited the activation of Syk and Syk-dependent signaling proteins including LAT, $PLC{\gamma}$, Akt, and MAP kinases. Our results suggest that CYC116 could be used as an alternative therapeutic medication for mast cell-mediated allergic disorders, such as atopic dermatitis and allergic rhinitis.
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등록된 정보가 없습니다.
참고문헌 (35)
참고문헌 신청
Baba Y / 2006 / Coupling of STIM1 to store-operated Ca2+ entry through its constitutive and inducible movement in the endoplasmic reticulum / Proc Natl Acad Sci USA 103:16704~16709
Beuchet P / 1999 / New 2-sulfonamidothiazoles substituted at C-4 : synthesis of polyoxy-genated aryl derivatives and in vitro evaluation of antifungal activity / Eur. J. Med. Chem 34:773~779
Bradding P / 1994 / Interleukin-4, -5, and-6 and tumor necrosis factor-alpha in normal and asthmatic airways : evidence for the human mast cell as a source of these cytokines / Am J Respir Cell Mol Biol 10:471~480
Carmena M / 2003 / The cellular geography of aurora kinases / Nat Rev Mol Cell Biol 4:842~854
Das J / 2006 / Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors / Bioorg Med Chem Lett 16:3706~3712
Beuchet P / 1999 / New 2-sulfonamidothiazoles substituted at C-4 : synthesis of polyoxy-genated aryl derivatives and in vitro evaluation of antifungal activity / Eur. J. Med. Chem 34:773~779
Bradding P / 1994 / Interleukin-4, -5, and-6 and tumor necrosis factor-alpha in normal and asthmatic airways : evidence for the human mast cell as a source of these cytokines / Am J Respir Cell Mol Biol 10:471~480
Carmena M / 2003 / The cellular geography of aurora kinases / Nat Rev Mol Cell Biol 4:842~854
Das J / 2006 / Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors / Bioorg Med Chem Lett 16:3706~3712
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