urb-597 and Neoplasms

urb-597 has been researched along with Neoplasms* in 2 studies

Other Studies

2 other study(ies) available for urb-597 and Neoplasms

ArticleYear
The fatty-acid amide hydrolase inhibitor URB597 inhibits MICA/B shedding.
    Scientific reports, 2020, 09-23, Volume: 10, Issue:1

    MICA/B proteins are expressed on the surface of various types of stressed cells, including cancer cells. Cytotoxic lymphocytes expressing natural killer group 2D (NKG2D) receptor recognize MICA/B and eliminate the cells. However, cancer cells evade such immune recognition by inducing proteolytic shedding of MICA/B proteins. Therefore, preventing the shedding of MICA/B proteins could enhance antitumor immunity. Here, by screening a protease inhibitor library, we found that the fatty-acid amide hydrolase (FAAH) inhibitor, URB597, suppresses the shedding of MICA/B. URB597 significantly reduced the soluble MICA level in culture medium and increased the MICA level on the surface of cancer cells. The effect was indirect, being mediated by increased expression of tissue inhibitor of metalloproteinases 3 (TIMP3). Knockdown of TIMP3 expression reversed the effect of URB597, confirming that TIMP3 is required for the MICA shedding inhibition by URB597. In contrast, FAAH overexpression reduced TIMP3 expression and the cell-surface MICA level and increased the soluble MICA level. These results suggest that inhibition of FAAH could prevent human cancer cell evasion of immune-mediated clearance.

    Topics: Amidohydrolases; Benzamides; Carbamates; Cell Line, Tumor; Culture Media; Gene Expression Regulation, Neoplastic; Histocompatibility Antigens Class I; Humans; Neoplasms; NK Cell Lectin-Like Receptor Subfamily K; T-Lymphocytes, Cytotoxic; Tissue Inhibitor of Metalloproteinase-3

2020
New Approaches to Cancer Therapy: Combining Fatty Acid Amide Hydrolase (FAAH) Inhibition with Peroxisome Proliferator-Activated Receptors (PPARs) Activation.
    Journal of medicinal chemistry, 2019, 12-26, Volume: 62, Issue:24

    Over the course of the past decade, peroxisome proliferator-activated receptors (PPARs) have been identified as part of the cannabinoid signaling system: both phytocannabinoids and endocannabinoids are capable of binding and activating these nuclear receptors. Fatty acid amide hydrolase (FAAH) hydrolyzes the endocannabinoid anandamide and other

    Topics: Amidohydrolases; Animals; Antineoplastic Agents; Humans; Neoplasms; Peroxisome Proliferator-Activated Receptors

2019