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6 | 53

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"It was strongly inhibited by HgCl2, ZnSO4, iodoacetate, iodoacetamide, and N-ethylmaleimide which indicated that it is a thiol protease, and by leupeptin, a strong inhibitor of cathepsin B from other sources."

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"For example, leupeptin inhibits trypsin, plasmin, thrombokinase, cathepsin B, and papain; chymostatin inhibits chymotrypsin; and elastatinal inhibits elastase."

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"Leupeptin, a strong inhibitor of liver cathepsin B (Umezawa and Aoyagi, 1977), strongly inhibited the retinal cathepsin B activity (90 inhibition at 10-6 M), but pepstatin, an inhibitor of pepsin and [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"Because cathepsins are the principal lysosomal proteases, we used cathepsin specific inhibitors, such as leupeptin, E-64 and pepstatin, to determine the relative importance of different cathepsins in degrading MT. The study reveals that cathepsin B and/or L is (are) probably the most important enzyme (s) in degrading hepatic MT, because leupeptin, which blocks cathepsin B and L activity, inhibited the degradation of apo-MT by about 80%."

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"Our finding that cathepsin B reduces the frequency of 6-TG resistant mutants while leupeptin does not, could be because leupeptin inhibits the activities of not only cathepsin B, but also cathepsin A,[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"However, inhibition of cathepsin B, L, and S in B cells treated with leupeptin results in the accumulation of intermediate sized fragments of 21 kD and 10 kD, derived from partial degradation of Ii [2[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"Leupeptin inhibits the cysteine protei nase activity of cathepsin B and papain with f Jn ID50 if I 1iM whereas the 1050 for inhibition of thrombin, a serine proteinase, is 20 mM (46)."

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"SARS-CoV infection was blocked by specific inhibitors of the pH-sensitive endosomal protease cathepsin L. S-mediated entry into Vero E6 and 293T/hACE2 cells was blocked by leupeptin, Z-lll-FMK (an inhibitor of both CTSB and CTSL), and E64c (an inhibitor of cysteine proteases) [21]."

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"Leupeptin (LeuP; Thermo Fisher Scientific, 78435) was given to the cells to inhibit cysteine-cathepsins (e.g., CTSB and CTSL) and was used at 5 µM for 72 h. Generation of CTSD-deficient H4 cells."

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"The neutral proteinase and cathepsin B like activity were inhibited by leupeptin and not by pepstatin while the converse obtained for cathepsin D activity."

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"Leupeptin is a potent inhibitor of cathepsin B in vitro and is presumed to act in a similar manner in vivo."

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"Cathepsin B1 is inhibited completely by 1pM leupeptin."

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"There are several major groups of proteinases : the serine proteinases (plasmin family, inhibited by aprotinin, al-proteinase inhibitor and leupeptin); the aspartic proteinases (cathepsin D family, in[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"Injection of leupeptin or E-64 into rats actually inhibits the activities of cathepsin B and cathepsin L in the lysosomal fraction of liver and results in inhibition of turnover rate of liver aldolase[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"Leupeptin is an inhibitor of cathepsin B and some other serine proteases."

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"Leupeptin is a reversible inhibitor of cathepsin B (IC 50% 1 mumol)."

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"Livers of non starved rats were perfused cyclically for 2 h in the presence of either 4 x the normal concentration of amino acids (known to suppress proteolysis to basal level), or the same medium together with leupeptin (an inhibitor of cathepsin B, H and L)."

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"Since homogenates of leupeptin treated muscles had decreased cathepsin B activity, this lysosomal protease may play a role in protein turnover in normal and diseased muscles."

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"Both the cathepsin B activities were completely inhibited by iodoacetamide and leupeptin, but phenylmethanesulfonyl fluoride and o-phenanthroline were ineffective."

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"The extent of inactivation of cathepsin B by leupeptin and E-64 significantly decreased in the presence of SA."

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"However, interpretation of the results obtained on whole tissue has been complicated by the fact that antipain and leupeptin are potent inhibitors of lyso- somal cathepsin B, as well as the sarcoplasm[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"Although 0.1 mM leupeptin inhibited 100% of BANA hydrolyzing activity of cathepsin B, it inhibited only about 95% of the BANA hydrolyzing activity and only about 80% of the Leu-NA-hydrolyzing activity[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"110, No. 1, 1983 January 14, 1983 BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS Pages 332-338 PARADOXICAL EFFECT OF LEUPEPTIN IN VIVO ON CATHEPSIN B ACTIVITY J.H.R. Sutherland and L.M. Greenbaum[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"The thiol proteinases, cathepsin B, H and L, which are known to be inhibited by leupeptin, are apparently involved in initiating digestion of rat 125I-asialoorosomucoid within liver lysosomes."

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"Thus, to narrow down the potential mechanism through which CQ treatment affects receptor processing and/or trafficking we studied if treatment with a protease inhibitor, leupeptin (N-acetyl-L-leucyl-L-leucyl-L-argininal; inhibitor of serine and cysteine proteases including cathepsin B), could mimic the effects of CQ on VEGFR2 abundance."

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"Dose dependent effects on the embryo were demonstrated using the acid bisazo dye Trypan Blue, which inhibits endocytosis, and an enzyme inhibitor of bacterial origin known as leupeptin which inhibits cathepsin B, H and L. Homogenates of rat kidney and placenta also produced congenital defects; the concommitant electron microscopical changes in the yolk sac suggest that these effects too are due to alterations in the availability or quality of histiotroph."

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"Literature reports that leupeptin is a competitive inhibitor of the enzyme cathepsin B therefore we expect that the compounds should also inhibit the enzyme in a competitive manner."

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"Leupeptin is a selective inhibitor of serine endopeptidases such as trypsin and cathepsin B [16]."

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"It is believed that CYLA uses these transporter systems to cross the BBB.CYLA is not 100% specific for calpain; it most likely inhibits other cysteine proteases such as cathepsin B, just as Leupeptin [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"Leupeptin and E-64 dose dependently inhibited both cathepsin B and cathepsin L activities, and pepstatin A strongly inhibited cathepsin D activity in rat kidney lysosomes."

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"Barrett [35] has shown that leupeptin inhibits human cathepsin B1."

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"Leupeptin and p-chloromercuribenzoate inhibited both cathepsin B and collagenolytic cathepsin in the ciliary body lysosomes."

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"During the time that cathepsin B plus L activities in autophagic vacuoles are inhibited by the injection of leupeptin, cytosolic enzymes are being accumulated in autophagic vacuoles suggesting that leupeptin blocks intralysosomal proteolysis, and that cytosolic enzymes are sequestered continuously into autophagosomes."

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"Leupeptin and antipain inhibit some other proteases, and thus probably also cathepsin B1, in a competitive way; under our incubation conditions their inhibition was, however, practically complete."

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"Leupeptin is an inhibitor of cathepsin B and other thiol proteases and would be expected to inhibit degradation of albumin intralysosomally."

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"Libby and Goldberg (1978) showed that leupeptin, which inhibits trypsin, plasmin, papain and cathepsin B, is a more efficient muscle proteinase inhibitor in normal and diseased muscle than pepstatin, [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"Previously [1] we found that administration of leupeptin or E-64 to rats inhibited the lysosomal cathepsin B and cathepsin L activity in their liver."

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"The ability of protease inhibitors, antipain (inhibitor for trypsin, u-PA, papain and cathepsin A/B), E-64 (inhibitor for thiol proteases), pepstatin A (inhibitor for pepsin, cathepsin D/E and renin),[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"Indeed, addition of leupeptin to homogenates of control fibroblasts caused an inhibition of cathepsin B at a concentration of 0.05 ' UM and upwards, as reported by many authors (24), whereas the activ[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"Leupeptin (inhibitor of cathepsin B) being a peptide can be more complementary to the enzyme active site due to its flexibility and presence of similar type of backbone structure as that of enzyme sho[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"Leupeptin has been reported to inhibit cathepsin B with a high degree of selectivity (17)."

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"Both the proteinase and cytotoxic activities of the purified amoebal cathepsin B were inhibited by leupeptin and serum and activated by free sulfhydryl groups, supporting the hypothesis that both activities are characteristics of amoebal cathepsin B. Virulent strains of E. histolytica (HM-1 and Rahman) had significantly more cathepsin B activity per milligram protein than less virulent strains (HK-9, Laredo, and Huff)."

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"DISCUSSIOn The present study confirms the earlier findings on a paradoxical stimulatory effect of leupeptin - a known inhibitor of cathepsin B - towards the activity of this enzyme when measured on ho[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"Therefore, the aspartyl protease inhibitor pepstatin A (Pep A), which inhibits lysosomal cathepsin D, and leupeptin (Leu), which inhibits lysosomal cathepsin B, were pre-incubated with Au-Ag@PDA NPs, [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"Leupeptin has broad protease specificity and may also inhibit cathepsin B; thus we tested the effect that Sm-p80 might have in CD23 cleavage."

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"Cathepsin B like activity in 15091 A tumor cells and in their membrane vesicles is also inhibited by leupeptin, antipain and IAA (50)."

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"Injection of leupeptin into rats [1] actually inhibits the activities of cathepsin B and cathepsin L in the lysosomal fraction of the liver cells."

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"The ability of protease inhibitors, E-64 (inhibitor for thiol proteases), pepstatin A (inhibitor for pepsin, cathepsin D/E, and renin), leupeptin (inhibitor for trypsin, plasmin, papain, and cathepsin[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"When cathepsin D was inhibited by pepstatin, the proteolysis of 125I labeled low density lipoproteins was inhibited by more than 90%, whereas when cathepsin B was inhibited by leupeptin, the rate of proteolysis decreased by approx."

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"In fact, this is consistent with a previous report, which stated that Leupeptin inhibits plasmin, trypsin, papain, calpain, and cathepsin B; but does not inhibit pepsin, cathepsins A and D, thrombin, [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"As reported in literature, Leupeptin being a potent peptide inhibitor of cathepsin B, inhibited the goat brain cathepsin B competitively with Ki value of 12.5 × l0−9 M [66] whereas Ki value for human liver cathepsin B [78] was reported to be 7.0 × 10−9 M."

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"Administration of leupeptin abolished the increased activity of two intracellular proteases calpain and cathepsin B induced by controlled mechanical ventilation."

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"In these experiments we assessed leupeptin, a serine and cysteine protease inhibitor, pepstatin A, an inhibitor of aspartic proteases, E-64-d, which inhibits cysteine proteases including cathepsin B, [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"