Titel | FRO: The effect of AMA0428, a novel rock inhibitor, in a model of wet age-related macular degeneration |
Abstract Nr. | 1029 |
Doel | Rho kinase (ROCK) is associated with VEGF-driven angiogenesis and is involved in inflammation and fibrosis. Therefore, the effect of a novel ROCK inhibitor, AMA0428, was studied in wet age-related macular degeneration (AMD). |
Methodes | The effect of AMA0428 on human brain microvascular endothelial cells (HBMEC), human brain vascular pericytes (HBVP) and human tenon fibroblasts (HTF) was determined by measuring cell viability (WST-1), apoptosis (caspase 3/7) and 2 migration assays (scratch and under-agarose) The in vivo response was investigated using a laser-induced choroidal neovascularization (CNV) mouse model. Intravitreal injections were given on day 0, 4, 10 and 20 with AMA0428, murine anti-VEGFR Ab (DC101) or placebo. Outcome was assessed by analysis of inflammation (CD45), angiogenesis (FITC-dextran), vessel leakage (Texas Red-conjugated Dextran and FITC-labeled lectin) and fibrosis (Collagen I). |
Resultaten | AMA0428 dose-dependently reduced proliferation and VEGF-induced migration of HBMEC and HTF. No significant effect was seen on HBVP proliferation; however, migration and pericyte recruitment were increased. There was no apoptosis induction. AMA0428 significantly reduced CNV and vessel leakage 2 weeks after laser treatment, comparable to DC101. In addition, AMA0428 inhibited inflammation on day 5 by 20% and collagen deposition on day 30 by 39% while DC101 had no effect on inflammation nor fibrosis. |
Conclusie | Our data suggest that targeting ROCK with AMA0428 not only reduces neoangiogenesis, but also blocks inflammation and fibrosis (contrary to anti-VEGF). These results point to a potential therapeutic benefit of ROCK inhibition in wet AMD. |
Naam | HOLLANDERS |
Initialen | K |
Instituut | KUL |
Stad | Leuven |
Naam | Van Bergen |
Initialen | T |
Instituut | KUL |
Stad | Leuven |
Naam | Vandewalle |
Initialen | E |
Instituut | KUL |
Stad | Leuven |
Naam | Castermans |
Initialen | K |
Instituut | Amakem |
Stad | Diepenbeek |
Naam | Kindt |
Initialen | N |
Instituut | Amakem |
Stad | Diepenbeek |
Naam | Moons |
Initialen | L |
Instituut | KUL |
Stad | Leuven |
Naam | Stalmans |
Initialen | I |
Instituut | KUL |
Stad | Leuven |