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논문 기본 정보

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학술저널
저자정보
Zheng, Mei (Department of Pharmacology, College of Pharmacy, Chonnam National University) Cho, Dong-Im (Department of Pharmacology, College of Pharmacy, Chonnam National University) Le, Hang Thi (Department of Pharmacology, College of Pharmacy, Chonnam National University) Cheon, Seung Hoon (Department of Medicinal Chemistry, College of Pharmacy, Chonnam National University) Kim, Kyeong-Man (Department of Pharmacology, College of Pharmacy, Chonnam National University)
저널정보
대한약학회 Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea 제37권 제9호
발행연도
2014.1
수록면
1,177 - 1,182 (6page)

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It was reported that mast cell degranulation is inversely related to the enzymatic activity of $M_2$-type pyruvate kinase ($M_2PK$). This study shows that activation of high-affinity IgE receptor ($Fc{\varepsilon}RI$) evokes a sequential dual regulation of $M_2PK$, i.e., an immediate decrement followed by slow phase increment of enzymatic activities. Changes in the activities of $M_2PK$ and mast cell degranulation showed similar time course after antigenic stimulation of $Fc{\varepsilon}RI$. The immediate inhibition of $M_2PK$ involved tyrosine phosphorylation, and subsequently led to a cellular accumulation of glycolytic intermediates, including fructose 1,6-biphosphate (FBP), a feedforward activator of $M_2PK$. As the cellular levels of FBP were increased, both the enzymatic acitivity of $M_2PK$ and mast cell degranulation slowly returned to near basal levels. A-Raf, when exogenously introduced into RBL-2H3 cells, phosphorylated $M_2PK$ on the serine residues, elevated enzyme activities of $M_2PK$, and resulted in the inhibition of degranulation. These results suggest that dual regulation of $M_2PK$ which involves the phosphorylation of $M_2PK$ and accumulation of a feedforward activator of $M_2PK$ plays important roles in the control of mast cell degranulation.

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