サイトカラシンA

用途イマチニブ製剤は、慢性骨髄性白血病 (CML)、フィラデルフィア染色体陽性急性リンパ性白血病 (Ph+ALL) 、KIT (CD117) 陽性消化管間質腫瘍 (GIST) に対する治療薬として用いられる。投与はメシル酸塩で行われる。

説明The cytochalasins are cell-permeable fungal metabolites which inhibit actin polymerization. This interferes with such diverse processes as cell movement, growth, phagocytosis, degranulation, and secretion. Cytochalasin A is an oxidized analog of cytochalasin B which uniquely inhibits HIV-1 protease (IC50 = 3 μM). Cytochalasins A and B differ from other cytochalasins in being able to rapidly and reversibly inhibit glucose transport by competitively binding glucose transporters (Ki = 4.0 and 0.6 μM, respectively). Cytochalasin A also induces the phosphorylation of the tyrosine phosphatase PTP3 of Dictyostelium, activating STATc.

使用Cytochalasin A is one of a family of potent mycotoxins produced by several species of fungi. All members of the class exhibit profound effects on cytoskeletal proteins, giving rise to pronounced morphogenic activity in animals and plants. Like most cytochalsins, cytochalasin A exhibits potent inhibition of actin filament function leading to cell death by apoptosis, and displays a broad range of resultant cellular actions. Despite the common mode of action, there is evidence that individual members of the class display diverse selectivity. Specifically, cytochalasin A is one of the few cytochalasins exhibiting activity against HIV-1 protease.