arp-100 and Ovarian-Neoplasms

arp-100 has been researched along with Ovarian-Neoplasms* in 1 studies

Other Studies

1 other study(ies) available for arp-100 and Ovarian-Neoplasms

Article	Year
Potent arylsulfonamide inhibitors of tumor necrosis factor-alpha converting enzyme able to reduce activated leukocyte cell adhesion molecule shedding in cancer cell models. Journal of medicinal chemistry, 2010, Mar-25, Volume: 53, Issue:6 Activated leukocyte cell adhesion molecule (ALCAM) plays a relevant role in tumor biology and progression. Our previous studies showed that ALCAM is expressed at the surface of epithelial ovarian cancer (EOC) cells and is released in a soluble form by ADAM-17-mediated shedding. This process is relevant to EOC cell motility and invasiveness, which is reduced by nonspecific inhibitors of ADAM-17. For this reason, ADAM-17 may represent a new useful target in anticancer therapy. Herein, we report the synthesis and biological evaluation of new ADAM-17 inhibitors containing an arylsulfonamidic scaffold. Among the new potential inhibitors, two very promising compounds 17 and 18 were discovered, with a nanomolar activity for ADAM-17 isolated enzyme. These compounds proved to be also the most potent in inhibiting soluble ALCAM release in cancer cells, showing a nanomolar activity on A2774 and SKOV3 cell lines. Topics: Activated-Leukocyte Cell Adhesion Molecule; ADAM Proteins; ADAM17 Protein; Blotting, Western; Cell Line, Tumor; Dose-Response Relationship, Drug; Enzyme Assays; Enzyme Inhibitors; Enzyme-Linked Immunosorbent Assay; Female; Humans; Hydroxamic Acids; Kinetics; Models, Chemical; Models, Molecular; Molecular Structure; Ovarian Neoplasms; Protein Binding; Structure-Activity Relationship; Sulfonamides	2010

Article

Year

Potent arylsulfonamide inhibitors of tumor necrosis factor-alpha converting enzyme able to reduce activated leukocyte cell adhesion molecule shedding in cancer cell models.

Journal of medicinal chemistry, 2010, Mar-25, Volume: 53, Issue:6

Activated leukocyte cell adhesion molecule (ALCAM) plays a relevant role in tumor biology and progression. Our previous studies showed that ALCAM is expressed at the surface of epithelial ovarian cancer (EOC) cells and is released in a soluble form by ADAM-17-mediated shedding. This process is relevant to EOC cell motility and invasiveness, which is reduced by nonspecific inhibitors of ADAM-17. For this reason, ADAM-17 may represent a new useful target in anticancer therapy. Herein, we report the synthesis and biological evaluation of new ADAM-17 inhibitors containing an arylsulfonamidic scaffold. Among the new potential inhibitors, two very promising compounds 17 and 18 were discovered, with a nanomolar activity for ADAM-17 isolated enzyme. These compounds proved to be also the most potent in inhibiting soluble ALCAM release in cancer cells, showing a nanomolar activity on A2774 and SKOV3 cell lines.

Topics: Activated-Leukocyte Cell Adhesion Molecule; ADAM Proteins; ADAM17 Protein; Blotting, Western; Cell Line, Tumor; Dose-Response Relationship, Drug; Enzyme Assays; Enzyme Inhibitors; Enzyme-Linked Immunosorbent Assay; Female; Humans; Hydroxamic Acids; Kinetics; Models, Chemical; Models, Molecular; Molecular Structure; Ovarian Neoplasms; Protein Binding; Structure-Activity Relationship; Sulfonamides

2010