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These pro-drugs are converted to active intermediates by enzymatic activity either in hypoxic areas of solid tumours (Sartorelli, 1988) or by increased activity of these enzymes in tumour compared with normal tissues (Brown and Giaccia, 1998), and therefore should exhibit tumour-selective cytotoxicity.
In the host, inactive PLG is converted to active plasmin by host-expressed tissue-type PLG activator (tPA) and urokinase (uPA).
These zymogens are precursor enzymes that are converted to active enzymes by the cleavage of one or in some instances two peptide bonds.
By the process of limited proteolysis, in which several cuts in the polypeptide chains of these cofactors are formed by the enzyme thrombin, factors V and VIII are converted to active cofactors.
This also allowed the FURA-2/AM to be converted to active FURA-2 by intracellular esterases.
Furthermore, stabilized TOP3 was cleaved by the hypoxic stress-induced endogenous caspases and thus the procaspase-3 was converted to active caspase-3 specifically under hypoxic conditions.
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Most cases of latent TB infection (LTBI) convert to active TB within the first 2 years of infection [ 15].
Immunity appears to play a role, given that dormant TB often converts to active disease when immune systems falter, for instance, as a consequence of HIV/AIDS.
Patients with latent TB were recommended for prophylactic TB medication, and latent TB in patients receiving prophylactic TB medication did not convert to active TB.
In an unfortunate accident in a patient with cystic fibrosis, colistin methanosulfate was reconstituted and allowed to mostly convert to active colistin before administration, which led to fatal acute respiratory distress syndrome [14].
The zymogen PC is converted to an active serine protease activated protein C (APC) by thrombin bound to thrombomodulin on the endothelial surface [ 6].
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CEO of Professional Science Editing for Scientists @ prosciediting.com