| Assay Method Information | |
| | Cathepsin B Inhibitor Series SAR Study |
| Description: | Human liver cathepsin B (EC 3.4.22.1) is a lysosomal cysteine protease. There has been a recent resurgence of interest in cathepsin B due to research showing that proteolysis by this enzyme is required for the entry and replication of the Ebola and SARS viruses in human cells. Thus cathepsin B inhibitors have potential as novel anti-viral agents. Cathepsin B is also implicated in cancer progression. Upregulation and secretion of this enzyme occurs in many types of tumors and correlates positively with their invasive and metastatic capabilities. Cathepsin B facilitates tumor invasion by dissolving extracellular barriers. Inhibitors of cathepsin B thus have been studied as potential anti-cancer agents. Two high-throughput screens against cathepsin B reported previously under AID 453 and AID 488 each independently revealed the same series of aminopyrazole inhibitors. Six compounds active in the original HTS were resynthesized, and 21 new compounds were made to explore SAR. As in the o |
| Affinity data for this assay | |
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