PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 7721331-2 1994 Both CA-074 (a specific inhibitor of cathepsin B) and pepstatin A (a specific inhibitor of cathepsin D) showed an inhibitory effect on the IL-2 production from an OVA-specific, I-Ad-restricted helper T (Th) cell clone upon stimulation with OVA presented by the I-Ad-positive APC. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 5-11 cathepsin B Homo sapiens 37-48 7584919-6 1995 The PPE activity was completely inhibited by a cathepsin B specific inhibitor, CA074. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 79-84 cathepsin B Homo sapiens 47-58 35119840-1 2022 CA-074 is a selective inhibitor of cathepsin B, a lysosomal cysteine protease. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 0-6 cathepsin B Homo sapiens 35-46 8393661-5 1993 However, the processing activity was effectively blocked by cysteine proteinase inhibitors, in particular E-64 and its cathepsin-B-selective derivative CA-074. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 152-158 cathepsin B Homo sapiens 119-130 35119840-5 2022 This study demonstrated that CA-074 is most effective at inhibiting cathepsin B at an acidic pH of 4.6 with nM potency, which was more than 100-fold more potent than its inhibition at a neutral pH of 7.2. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 29-35 cathepsin B Homo sapiens 68-79 35156579-11 2022 However, Cathepsin B inhibitors, i.e., CA-074, can prevent neuronal death in AD patients. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 39-45 cathepsin B Homo sapiens 9-20 33510618-5 2020 In the glioma-derived cell line H4, the Abeta2-x levels were likewise decreased in supernatants by treatment with the more specific, but cell-impermeant CatB-inhibitor CA-074, by CA-074 Me treatment, and by CTSB gene deletion. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 168-174 cathepsin B Homo sapiens 153-157 34994563-7 2022 Based on the significant fold change (FC) >= 2 and p-value < 0.05 criteria, a total of 10, 48, and 13 proteins were deregulated after inhibiting CATB, SAPC antibodies, and the CATB inhibitor CA-074, respectively. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 193-199 cathepsin B Homo sapiens 178-182 29454581-10 2018 Examination of the CNS roles of cathepsins is limited by the shortage of highly selective inhibitors, with CA-074 being the only available specific cathepsin B inhibitor. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 107-113 cathepsin B Homo sapiens 148-159 30591146-10 2018 Inhibition of cathepsin B with the specific inhibitor CA074 significantly reduced LPA-increased invasion of 12Z. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 54-59 cathepsin B Homo sapiens 14-25 29432801-9 2018 Moreover, the levels of IL-1beta and IL-18 production decreased in CA-074 (a cathepsin B inhibitor) and NAC (an anti-oxidant) pretreated human macrophages, compared to untreated controls. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 67-73 cathepsin B Homo sapiens 77-88 25808857-6 2016 Treatment of CRC cells with the highly selective and non-permeant cathepsin B inhibitor Ca074 revealed that extracellular cathepsin B actively contributed to the invasiveness of human CRC cells while not essential for their growth in soft agar. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 88-93 cathepsin B Homo sapiens 66-77 29531800-8 2018 Also the Cathepsin B inhibitor CA074 prevents eIF2alpha from degradation and reduces cell death. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 31-36 cathepsin B Homo sapiens 9-20 29086922-5 2017 Enhanced invasion observed in 3D cultures with N1ME stefin A-low cells was reliant on cathepsin B activation, as addition of the small molecule inhibitor CA-074 rescued the DCIS-like non-invasive phenotype. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 154-160 cathepsin B Homo sapiens 86-97 25808857-6 2016 Treatment of CRC cells with the highly selective and non-permeant cathepsin B inhibitor Ca074 revealed that extracellular cathepsin B actively contributed to the invasiveness of human CRC cells while not essential for their growth in soft agar. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 88-93 cathepsin B Homo sapiens 122-133 22457711-7 2012 These activities corresponded to a cathepsin B-like enzyme since they were inhibited by CA-074, a specific cathepsin B inhibitor. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 88-94 cathepsin B Homo sapiens 35-46 26092112-10 2015 The cathepsin B inhibitor CA-074 and cathepsin B antibody prevented neuronal apoptosis. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 26-32 cathepsin B Homo sapiens 4-15 25209871-9 2014 A significant increase in 30% of apoptotic neurons was obtained that decreased to 5% with the specific cathepsin B inhibitor (CA-074) or with cathepsin B antibody. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 126-132 cathepsin B Homo sapiens 103-114 25260629-10 2014 This acid/CTSB-dependent activation of ENaC was ameliorated with the cell impermeable, CTSB-selective inhibitor CA074, suggesting that CTSB inhibition may have therapeutic relevance. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 112-117 cathepsin B Homo sapiens 10-14 25260629-10 2014 This acid/CTSB-dependent activation of ENaC was ameliorated with the cell impermeable, CTSB-selective inhibitor CA074, suggesting that CTSB inhibition may have therapeutic relevance. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 112-117 cathepsin B Homo sapiens 87-91 25260629-10 2014 This acid/CTSB-dependent activation of ENaC was ameliorated with the cell impermeable, CTSB-selective inhibitor CA074, suggesting that CTSB inhibition may have therapeutic relevance. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 112-117 cathepsin B Homo sapiens 87-91 22266111-6 2012 Similarly, intraperitoneal administration of the highly selective cathepsin B inhibitor CA-074 reduced metastasis in tumor-bearing animals, a reduction that was not reproduced by the broad spectrum cysteine cathepsin inhibitor JPM-OEt. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 88-94 cathepsin B Homo sapiens 66-77 22457711-7 2012 These activities corresponded to a cathepsin B-like enzyme since they were inhibited by CA-074, a specific cathepsin B inhibitor. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 88-94 cathepsin B Homo sapiens 107-118 19026616-6 2009 Interestingly, the lysosomal cathepsin B inhibitor CA074 markedly decreased BPC-induced caspase-3 and caspase-6 activation as well as cell death. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 51-56 cathepsin B Homo sapiens 29-40 22093547-12 2011 A functional role for cathepsin B was confirmed by the ability of CA074, a cell impermeable and highly selective cathepsin B inhibitor, to significantly reduce pericellular proteolysis and invasion by SUM149 cells. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 66-71 cathepsin B Homo sapiens 22-33 22093547-12 2011 A functional role for cathepsin B was confirmed by the ability of CA074, a cell impermeable and highly selective cathepsin B inhibitor, to significantly reduce pericellular proteolysis and invasion by SUM149 cells. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 66-71 cathepsin B Homo sapiens 113-124 20544024-4 2010 METHODS AND FINDINGS: We have determined, by X-ray crystallography, the first reported structure of TbCatB in complex with the cathepsin B selective inhibitor CA074. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 159-164 cathepsin B Homo sapiens 127-138 20544024-8 2010 The TbCat*CA074 structure confirms that the occluding loop, which is an essential part of the substrate-binding site, creates a larger prime side pocket in the active site cleft than is found in mammalian cathepsin B-small molecule structures. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 10-15 cathepsin B Homo sapiens 205-216 19535915-3 2009 We compared effects of CAA0225 on autophagy with those of CA-074 that was previously developed as a cathepsin B-specific inhibitor. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 58-64 cathepsin B Homo sapiens 100-111 17634228-3 2007 Whereas, CA-074 Me gave a biphasic response that differentiated between Moloney MLV Env and VSV G at low concentrations, at which the drug is highly selective for cathepsin B, but was similar for both glycoproteins at higher concentrations, at which CA-074 Me inhibits other cathepsins. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 9-15 cathepsin B Homo sapiens 163-174 18789614-8 2008 Addition of CB inhibitor, CA-074, significantly attenuated the ratio of hypodiploid and apoptotic cells, partially blocked caspase 3 activation and inhibited reduction of cell viability induced by emodin. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 26-32 cathepsin B Homo sapiens 12-14 15586230-6 2005 The protein synthesis inhibitor cycloheximide markedly increased the TRAIL sensitivity of these cell lines, whereas the CB-specific chemical inhibitor CA-074 markedly reduced the sensitivity of primary OC cells to TRAIL. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 151-157 cathepsin B Homo sapiens 120-122 16620747-3 2006 By this technique, activity of purified human liver cathepsin B was detected at a concentration as low as 50 ng and was blocked only in the presence of the cysteine protease inhibitor E-64 and the specific cathepsin B inhibitor CA-074 but not by aspartate, serine, or matrix metalloprotease inhibitors. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 228-234 cathepsin B Homo sapiens 52-63 16620747-3 2006 By this technique, activity of purified human liver cathepsin B was detected at a concentration as low as 50 ng and was blocked only in the presence of the cysteine protease inhibitor E-64 and the specific cathepsin B inhibitor CA-074 but not by aspartate, serine, or matrix metalloprotease inhibitors. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 228-234 cathepsin B Homo sapiens 206-217 16051222-3 2005 In vitro proteolysis of IGF-I using an endosomal lysate required an acidic pH and was sensitive to CA074, an inhibitor of the cathepsin B enzyme. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 99-104 cathepsin B Homo sapiens 126-137 17399759-7 2007 The VSMC death was also inhibited by a neutralizing anti-TNF receptor 1 antibody, the caspase inhibitor z-VAD, and the cathepsin B inhibitor CA074, a finding indicative of the role of both caspases and cathepsin B in this process. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 141-146 cathepsin B Homo sapiens 119-130 16831419-5 2006 Caspase-3, and -6 activity induced by BPC in K562 cells was prevented by the cathepsin-B inhibitor [N-(L-3-trans-propylcarbamoyl-oxirane-2-carbonyl)-L-isoleucyl-L-proline] (CA074). N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 173-178 cathepsin B Homo sapiens 77-88 16164418-6 2005 The selective cathepsin B inhibitor, CA074, blocked the conversion of endogenous APP to A beta in isolated regulated secretory vesicles. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 37-42 cathepsin B Homo sapiens 14-25 12581740-4 2003 CA-074, a membrane-impermeable cathepsin B-selective inhibitor and its membrane-permeable analogue CA-074Me showed similar inhibition of invasion at 10 microM, i.e., 24.9 and 27.0%, respectively. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 0-6 cathepsin B Homo sapiens 31-42 11309313-6 2001 The anionic cathepsin B inhibitor (L-3-trans-propylcarbamoyloxirane-2-carbony)-L-isoleucyl-L-proline (CA-074), at a concentration of 1 microM, caused a nearly quantitative inhibition of extracellular cathepsin B but had no effect on Matrigel invasion. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 102-108 cathepsin B Homo sapiens 12-23 11815600-4 2002 Pro-uPA activation was preceded by dramatic changes in lysosome trafficking and the extracellular appearance of cathepsin B and beta-hexosaminidase but not cathepsins D or L. Co-treatment of cultures with the cathepsin B inhibitors CA-074 or Z-FA-FMK suppressed the cytostatic effects of TPA and activation of pro-uPA. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 232-238 cathepsin B Homo sapiens 112-123 11815600-4 2002 Pro-uPA activation was preceded by dramatic changes in lysosome trafficking and the extracellular appearance of cathepsin B and beta-hexosaminidase but not cathepsins D or L. Co-treatment of cultures with the cathepsin B inhibitors CA-074 or Z-FA-FMK suppressed the cytostatic effects of TPA and activation of pro-uPA. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 232-238 cathepsin B Homo sapiens 209-220 11327703-5 2001 Cathepsin B in RA fluid could degrade collagen, and this degradation was suppressed by the addition of CA-074, a specific inhibitor of cathepsin B. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 103-109 cathepsin B Homo sapiens 0-11 11327703-5 2001 Cathepsin B in RA fluid could degrade collagen, and this degradation was suppressed by the addition of CA-074, a specific inhibitor of cathepsin B. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 103-109 cathepsin B Homo sapiens 135-146 11517939-7 2001 By comparison, CA074 was found to inactivate cathepsin B at least 34000-fold more efficiently than cathepsin X. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 15-20 cathepsin B Homo sapiens 45-56 11309313-8 2001 Surprisingly, at a concentration of 10 microM, CA-074 slowly permeated the cells, causing an 80-95% inhibition of intracellular cathepsin B after 12 h, the duration of the invasion assay. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 47-53 cathepsin B Homo sapiens 128-139 11258881-13 2001 In particular, CA074 was found to inactivate cathepsin B at least 34000-fold more efficiently than cathepsin X. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 15-20 cathepsin B Homo sapiens 45-56 10662686-9 2000 Esterifying CA-074 resulted in a cell-permeable inhibitor with dramatically reduced activity and specificity for cathepsin B. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 12-18 cathepsin B Homo sapiens 113-124 10951198-3 2000 The enzyme was also inhibited by two specific synthetic cathepsin B inhibitors, CA-074 and GFG-semicarbazone. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 80-86 cathepsin B Homo sapiens 56-67 10936287-0 2000 Inhibitory effect of cathepsin B inhibitor CA 074 on mouse anti-rat mixed lymphocyte reaction: novel immunosuppressive strategy for indirect xenoantigen recognition. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 43-49 cathepsin B Homo sapiens 21-32 10447678-9 1999 Pretreatment of cells with the membrane-permeant proinhibitor CA-074Me completely abolished pericellular and total cathepsin B activity whereas pretreatment with the active drug CA-074 had no effect. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 62-68 cathepsin B Homo sapiens 115-126 10543449-2 1999 For the detection of enzymatic activities we used the synthetic substrate Z-Phe-Arg-AMC, and for discrimination between cathepsin L, S and cathepsin B the specific inhibitor CA-074 for blocking interfering cathepsin B activities was applied. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 174-180 cathepsin B Homo sapiens 139-150 10543449-2 1999 For the detection of enzymatic activities we used the synthetic substrate Z-Phe-Arg-AMC, and for discrimination between cathepsin L, S and cathepsin B the specific inhibitor CA-074 for blocking interfering cathepsin B activities was applied. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 174-180 cathepsin B Homo sapiens 206-217 10447678-6 1999 To validate the assay, we determined that human liver cathepsin B was stable and active under the conditions of the assay and its activity could be inhibited by the selective epoxide derivative CA-074. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 194-200 cathepsin B Homo sapiens 54-65 9546050-1 1998 The Ile-Pro sequence of CA074, potent covalent-type inhibitor, is necessary to exhibit the specificity for cathepsin B, but not for papain. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 24-29 cathepsin B Homo sapiens 107-118 10380357-5 1999 E-64-c and CA074 are representative derivatives developed from E-64 as a clinical usable and a cathepsin B-specific inhibitors, respectively. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 11-16 cathepsin B Homo sapiens 95-106 10380357-6 1999 In contrast with similar binding/inhibitory modes of E-64-c and E-64 for cysteine proteases, the inhibitory mechanism of cathepsin B-specific CA074 results from the binding to the Sn" subsite. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 142-147 cathepsin B Homo sapiens 121-132 9751144-0 1998 Inhibition of ischaemic hippocampal neuronal death in primates with cathepsin B inhibitor CA-074: a novel strategy for neuroprotection based on "calpain-cathepsin hypothesis". N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 90-96 cathepsin B Homo sapiens 68-79 9751144-5 1998 When a specific inhibitor of cathepsin B, the epoxysuccinyl peptide CA-074 (C18H29N3O6) was intravenously administered immediately after the ischaemic insult, approximately 67% of CA1 neurons were saved from delayed neuronal death on day 5 in eight monkeys undergoing 20 min brain ischaemia: the extent of inhibition was excellent in three of eight and good in five of eight monkeys. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 68-74 cathepsin B Homo sapiens 29-40 9762356-2 1998 Administration of cathepsin B inhibitors, E-64, CA-074 and vitamin B6, caused the strong suppression of the Th-2 type immune responses. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 48-54 cathepsin B Homo sapiens 18-29 8814458-5 1996 More than 95% of Z-Arg-Arg-MCA hydrolytic activity in each GCF sample was inhibited by CA-074, specific inhibitor of cathepsin B. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 87-93 cathepsin B Homo sapiens 117-128 8645703-2 1996 Cathepsin B activity was measured using a fluorescent synthetic substrate, 7-N-benzyloxycarbonyl-L-arginyl-L-arginylamide-4-methylcoumarin, and its specificity was checked with E-64, a specific inhibitor of cysteine proteinases and CA074, a specific inhibitor of the enzyme. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 232-237 cathepsin B Homo sapiens 0-11 9099961-2 1997 Specificity was verified with the cath B blocking inhibitors E-64 and CA-074. N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline 70-76 cathepsin B Homo sapiens 34-40