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抗靶標

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在藥物學中,一個抗靶標可以是一個受體,或者其它生物靶標,當其和藥物作用時會引起不希望的不良反應副反應)。對於藥物研發公司來說,在藥物設計和開發過程中確保新藥不和大量的被意外發現的抗靶標產生顯著活性是至關重要的。[1][2]


最知名和最顯著的抗靶標分別是hERG通道和5-HT2B 受體,會在小範圍但不可預知比例的用藥人身上分別引發心臟功能的長期問題——QT間期延長綜合症心肌纖維化。這些靶標的發現是由於某些上市藥物高頻率的特有不良反應;一些具有顯著hERG活性的老藥依然被警示使用中,大部分被發現是強烈的 5-HT2B激動劑的藥物不得不從市場退市。因此,任何先導化合物如果在初期的藥物篩選中顯示出和這些靶標有較高的親和力,幾乎都會被終止開發。 [3][4][5][6][7][8]

參考文獻

[編輯]
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