AubipyOMe is a potent inhibitor of tartrate resistant acid phosphatase (TRAP/ACP5), a metalloenzyme expressed in activated osteoclasts and in macrophages. AubipyOMe exhibited IC50 values of 1.3 μM for TRAP5a and 1.8 μM for TRAP5b and inhibited TRAP activity in murine macrophage and human lung tissue extracts.
Molecular medicine (Cambridge, Mass.), 30(1), 89-89 (2024-06-16)
Myocardial infarction (MI) leads to enhanced activity of cardiac fibroblasts (CFs) and abnormal deposition of extracellular matrix proteins, resulting in cardiac fibrosis. Tartrate-resistant acid phosphatase 5 (ACP5) has been shown to promote cell proliferation and phenotypic transition. However, it remains
The enzyme tartrate resistant acid phosphatase (TRAP, two isoforms 5a and 5b) is highly expressed in alveolar macrophages, but its function there is unclear and potent selective inhibitors of TRAP are required to assess functional aspects of the protein. We
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