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38 results

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E-64c-Hydrazide Based Cathepsin C Inhibitors: Optimizing the Interactions with the S1'-S2' Area.
Tromsdorf N, Ullrich FTH, Rethmeier M, Sommerhoff CP, Schaschke N. Tromsdorf N, et al. ChemMedChem. 2023 Sep 15;18(18):e202300218. doi: 10.1002/cmdc.202300218. Epub 2023 Jul 24. ChemMedChem. 2023. PMID: 37424408
The inhibition of this cysteine protease therefore is an interesting therapeutic approach for the treatment of inflammatory disorders with a high neutrophil burden such as COPD. Based on E-64c-hydrazide as lead structure, we have recently developed a covalently acti …
The inhibition of this cysteine protease therefore is an interesting therapeutic approach for the treatment of inflammatory disorders with a …
Intracellular versus extracellular inhibition of calpain I causes differential effects on pain in a rat model of joint inflammation.
McDougall JJ, McConnell M, Reid AR. McDougall JJ, et al. Mol Pain. 2021 Jan-Dec;17:17448069211016141. doi: 10.1177/17448069211016141. Mol Pain. 2021. PMID: 34006144 Free PMC article.
Local administration of calpain I reduced secondary allodynia in the acute inflammation model and this effect was blocked by the cell impermeable calpain inhibitor E-64c. Calpain I also blocked the algesic effect of the protease activated receptor-2 (PAR-2) cleaving …
Local administration of calpain I reduced secondary allodynia in the acute inflammation model and this effect was blocked by the cell imperm …
Role of cerium oxide nanoparticle-induced autophagy as a safeguard to exogenous H2O2-mediated DNA damage in tobacco BY-2 cells.
Sadhu A, Ghosh I, Moriyasu Y, Mukherjee A, Bandyopadhyay M. Sadhu A, et al. Mutagenesis. 2018 Apr 13;33(2):161-177. doi: 10.1093/mutage/gey004. Mutagenesis. 2018. PMID: 29506140
CeNP exposure to transgenic BY-2 cells expressing GFP-Atg8 fusion protein exhibited formation of autophagosomes at Ce10. Application of vacuolar protease inhibitor E-64c and fluorescent basic dye acridine orange, further demonstrated accumulation of particulate matt …
CeNP exposure to transgenic BY-2 cells expressing GFP-Atg8 fusion protein exhibited formation of autophagosomes at Ce10. Application of vacu …
Dissection of autophagy in tobacco BY-2 cells under sucrose starvation conditions using the vacuolar H(+)-ATPase inhibitor concanamycin A and the autophagy-related protein Atg8.
Yano K, Yanagisawa T, Mukae K, Niwa Y, Inoue Y, Moriyasu Y. Yano K, et al. Plant Signal Behav. 2015;10(11):e1082699. doi: 10.1080/15592324.2015.1082699. Plant Signal Behav. 2015. PMID: 26368310 Free PMC article.
Such accumulation did not occur in the presence of the autophagy inhibitor 3-methyladenine, and concanamycin in turn inhibited the accumulation of autolysosomes in the presence of the cysteine protease inhibitor E-64c. Electron microscopy revealed not only that the …
Such accumulation did not occur in the presence of the autophagy inhibitor 3-methyladenine, and concanamycin in turn inhibited the accumulat …
Design, synthesis, evaluation and thermodynamics of 1-substituted pyridylimidazo[1,5-a]pyridine derivatives as cysteine protease inhibitors.
Khan MS, Baig MH, Ahmad S, Siddiqui SA, Srivastava AK, Srinivasan KV, Ansari IA. Khan MS, et al. PLoS One. 2013 Aug 5;8(8):e69982. doi: 10.1371/journal.pone.0069982. Print 2013. PLoS One. 2013. PMID: 23940536 Free PMC article.
The molecular interaction between the compounds and cysteine protease (papain) was found to be very similar to the interactions observed with the respective epoxide inhibitor (E-64c) of papain. Subsequently, compounds were synthesized to validate their efficacy in w …
The molecular interaction between the compounds and cysteine protease (papain) was found to be very similar to the interactions observed wit …
E-64c-hydrazide: a lead structure for the development of irreversible cathepsin C inhibitors.
Radzey H, Rethmeier M, Klimpel D, Grundhuber M, Sommerhoff CP, Schaschke N. Radzey H, et al. ChemMedChem. 2013 Aug;8(8):1314-21. doi: 10.1002/cmdc.201300093. Epub 2013 Jun 18. ChemMedChem. 2013. PMID: 23780739
Here, the hydrazide of (2S,3S)-trans-epoxysuccinyl-L-leucylamido-3-methylbutane (E-64c) (k2/Ki =1405 M(-1) s(-1)) is demonstrated to be a lead structure for the development of irreversible cathepsin C inhibitors. ...
Here, the hydrazide of (2S,3S)-trans-epoxysuccinyl-L-leucylamido-3-methylbutane (E-64c) (k2/Ki =1405 M(-1) s(-1)) is demonstra …
Autophagy in tobacco BY-2 cells cultured under sucrose starvation conditions: isolation of the autolysosome and its characterization.
Takatsuka C, Inoue Y, Higuchi T, Hillmer S, Robinson DG, Moriyasu Y. Takatsuka C, et al. Plant Cell Physiol. 2011 Dec;52(12):2074-87. doi: 10.1093/pcp/pcr137. Epub 2011 Oct 27. Plant Cell Physiol. 2011. PMID: 22039105
The digestion process in autolysosomes can be retarded by addition of the cysteine protease inhibitor E-64c to the culture medium, resulting in the accumulation of autolysosomes. ...
The digestion process in autolysosomes can be retarded by addition of the cysteine protease inhibitor E-64c to the culture med …
Use of protease inhibitors for detecting autophagy in plants.
Moriyasu Y, Inoue Y. Moriyasu Y, et al. Methods Enzymol. 2008;451:557-80. doi: 10.1016/S0076-6879(08)03232-1. Methods Enzymol. 2008. PMID: 19185740
In cultured tobacco (BY-2) cells, autophagy seems to be induced under nutrient-starvation conditions, whereas in root cells from Arabidopsis and barley, it occurs constitutively though is activated under nutrient starvation conditions. In both cases, protease inhibitors such as E …
In cultured tobacco (BY-2) cells, autophagy seems to be induced under nutrient-starvation conditions, whereas in root cells from Arabidopsis …
A novel type of autophagy occurs together with vacuole genesis in miniprotoplasts prepared from tobacco culture cells.
Yano K, Hattori M, Moriyasu Y. Yano K, et al. Autophagy. 2007 May-Jun;3(3):215-21. doi: 10.4161/auto.3739. Epub 2007 May 26. Autophagy. 2007. PMID: 17224627
The miniprotoplasts had few vacuoles immediately after preparation, but had large vacuoles after 1 to 2 d. When the cysteine protease inhibitor E-64c or E-64d was added to culture media, almost all vacuoles formed contained materials of cytoplasmic origin. ...
The miniprotoplasts had few vacuoles immediately after preparation, but had large vacuoles after 1 to 2 d. When the cysteine protease inhibi …
A homologue of cathepsin L identified in conditioned medium from Sf9 insect cells.
Lindskog E, Svensson I, Häggström L. Lindskog E, et al. Appl Microbiol Biotechnol. 2006 Jul;71(4):444-9. doi: 10.1007/s00253-005-0181-9. Epub 2005 Nov 10. Appl Microbiol Biotechnol. 2006. PMID: 16283300
This peptidase showed the same inhibitor profile, substrate range and optimum pH (5.0) as the 39-kDa form, indicating that Sf9 cathepsin L has two active forms, at 39 and 22 kDa. Addition of the cysteine peptidase inhibitor E-64c to an Sf9 culture inhibited all prot …
This peptidase showed the same inhibitor profile, substrate range and optimum pH (5.0) as the 39-kDa form, indicating that Sf9 cathepsin L h …
38 results