Cysteine Protease inhibitor - CAS 921625-62-9
Catalog number: 921625-62-9
Category: Inhibitor
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Molecular Weight:
Cysteine Protease inhibitor is a inhibitor of cysteine protease.
2-Pyrimidinecarbonitrile, 4-[[4'-(aminomethyl)[1,1'-biphenyl]-3-yl]oxy]-
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1.The Kunitz-Type Protein ShPI-1 Inhibits Serine Proteases and Voltage-Gated Potassium Channels.
García-Fernández R1, Peigneur S2, Pons T3, Alvarez C4, González L5, Chávez MA6, Tytgat J7. Toxins (Basel). 2016 Apr 13;8(4). pii: E110. doi: 10.3390/toxins8040110.
The bovine pancreatic trypsin inhibitor (BPTI)-Kunitz-type protein ShPI-1 (UniProt: P31713) is the major protease inhibitor from the sea anemone Stichodactyla helianthus. This molecule is used in biotechnology and has biomedical potential related to its anti-parasitic effect. A pseudo wild-type variant, rShPI-1A, with additional residues at the N- and C-terminal, has a similar three-dimensional structure and comparable trypsin inhibition strength. Further insights into the structure-function relationship of rShPI-1A are required in order to obtain a better understanding of the mechanism of action of this sea anemone peptide. Using enzyme kinetics, we now investigated its activity against other serine proteases. Considering previous reports of bifunctional Kunitz-type proteins from anemones, we also studied the effect of rShPI-1A on voltage-gated potassium (Kv) channels. rShPI-1A binds Kv1.1, Kv1.2, and Kv1.6 channels with IC50 values in the nM range.
2.Cathepsin L in tumor angiogenesis and its therapeutic intervention by the small molecule inhibitor KGP94.
Sudhan DR1,2, Rabaglino MB3, Wood CE4, Siemann DW5,6. Clin Exp Metastasis. 2016 Apr 7. [Epub ahead of print]
A significant proportion of breast cancer patients harbor clinically undetectable micrometastases at the time of diagnosis. If left untreated, these micro-metastases may lead to disease relapse and possibly death. Hence, there is significant interest in the development of novel anti-metastatic agents that could also curb the growth of pre-established micrometastases. Like primary tumor, the growth of metastases also is driven by angiogenesis. Although the role of cysteine protease Cathepsin L (CTSL) in metastasis associated tumor cell functions such as migration and invasion is well recognized, its role in tumor angiogenesis remains less explored. The present study examines the contribution of CTSL to breast cancer angiogenesis and evaluates the anti-angiogenic efficacy of CTSL inhibitor KGP94. CTSL semi-quantitative RT-PCR analysis on breast tissue panels revealed significant upregulation of CTSL in breast cancer patients which strongly correlated with increased relapse and metastatic incidence and poor overall survival.
3.A Brucella spp. Protease Inhibitor Limits Antigen Lysosomal Proteolysis, Increases Cross-Presentation, and Enhances CD8+ T Cell Responses.
Coria LM1, Ibañez AE1, Tkach M2, Sabbione F3, Bruno L1, Carabajal MV1, Berguer PM4, Barrionuevo P3, Schillaci R2, Trevani AS3, Giambartolomei GH5, Pasquevich KA1, Cassataro J6. J Immunol. 2016 Apr 15. pii: 1501188. [Epub ahead of print]
In this study, we demonstrate that the unlipidated (U) outer membrane protein (Omp) 19 fromBrucellaspp. is a competitive inhibitor of human cathepsin L. U-Omp19 inhibits lysosome cathepsins and APC-derived microsome activity in vitro and partially inhibits lysosomal cathepsin L activity within live APCs. Codelivery of U-Omp19 with the Ag can reduce intracellular Ag digestion and increases Ag half-life in dendritic cells (DCs). U-Omp19 retains the Ag in Lamp-2+compartments after its internalization and promotes a sustained expression of MHC class I/peptide complexes in the cell surface of DCs. Consequently, U-Omp19 enhances Ag cross-presentation by DCs to CD8+T cells. U-Omp19 s.c. delivery induces the recruitment of CD11c+CD8α+DCs and monocytes to lymph nodes whereas it partially limits in vivo Ag proteolysis inside DCs. Accordingly, this protein is able to induce CD8+T cell responses in vivo against codelivered Ag. Antitumor responses were elicited after U-Omp19 coadministration, increasing survival of mice in a murine melanoma challenge model.
4.Microbial inhibitors of cysteine proteases.
Kędzior M1, Seredyński R2, Gutowicz J2. Med Microbiol Immunol. 2016 Apr 5. [Epub ahead of print]
Cysteine proteases are one of the major classes of proteolytic enzymes involved in a number of physiological and pathological processes in plants, animals and microorganisms. When their synthesis, activity and localization in mammalian cells are altered, they may contribute to the development of many diseases, including rheumatoid arthritis, osteoporosis and cancer. Therefore, cysteine proteases have become promising drug targets for the medical treatment of these disorders. Inhibitors of cysteine proteases are also produced by almost every group of living organisms, being responsible for the control of intracellular proteolytic activity. Microorganisms synthesize cysteine protease inhibitors not only to regulate the activity of endogenous, often virulent enzymes, but also to hinder the host's proteolytic defense system and evade its immune responses against infections. Present work describes known to date microbial inhibitors of cysteine proteases in terms of their structure, enzyme binding mechanism, specificity and pathophysiological roles.
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