Possibly, the enzymatic system was rapidly active in the presence of the three components (CL/Caspase-8 and Bid-FL), all together in the vicinity of the vesicles, such that tBid was generated and active (similar to the effect of tBid described in Figure 2d and h).
In L929 fibroblasts and Raw264.7 macrophages, IFNγ-induced Irgm1 is rapidly recruited to active plasma membrane upon phagocytosis and remains associated with phagosomes as they mature [20].
Both in physiological and pathological conditions their expression is rapidly induced when active tissue remodelling is needed.
As a reformulated prodrug, fosaprepitant avoids the problems associated with oral administration, and when infused intravenously is rapidly converted to active aprepitant by phosphatase enzymes.
Dabigatran etexilate is a prodrug that is rapidly converted to the active direct thrombin inhibitor dabigatran.
Ximelagatran (Exanta™, AstraZeneca) is a novel, oral direct thrombin inhibitor (oral DTI) that is rapidly converted to its active form, melagatran, upon administration.
IV artesunate is rapidly hydrolyzed to the active metabolite dihydroartemisinin.
Dabigatran etexilate is a prodrug that is rapidly converted into its active form, dabigatran, by esterases.
After administration, upamostat is rapidly metabolized to the active drug, WX-UK1.
Tedizolid phosphate (TR-701), previously known as torezolidphosphate, is an inactive prodrug that, after oral or intravenous administration, is rapidly converted to the active form (torezolid).
