[HTML][HTML] Targeting autocrine HB-EGF signaling with specific ADAM12 inhibition using recombinant ADAM12 prodomain

MA Miller, ML Moss, G Powell, R Petrovich… - Scientific reports, 2015 - nature.com
MA Miller, ML Moss, G Powell, R Petrovich, L Edwards, AS Meyer, LG Griffith
Scientific reports, 2015nature.com
Dysregulation of ErbB-family signaling underlies numerous pathologies and has been
therapeutically targeted through inhibiting ErbB-receptors themselves or their cognate
ligands. For the latter,“decoy” antibodies have been developed to sequester ligands
including heparin-binding epidermal growth factor (HB-EGF); however, demonstrating
sufficient efficacy has been difficult. Here, we hypothesized that this strategy depends on
properties such as ligand-receptor binding affinity, which varies widely across the known …
Abstract
Dysregulation of ErbB-family signaling underlies numerous pathologies and has been therapeutically targeted through inhibiting ErbB-receptors themselves or their cognate ligands. For the latter, “decoy” antibodies have been developed to sequester ligands including heparin-binding epidermal growth factor (HB-EGF); however, demonstrating sufficient efficacy has been difficult. Here, we hypothesized that this strategy depends on properties such as ligand-receptor binding affinity, which varies widely across the known ErbB-family ligands. Guided by computational modeling, we found that high-affinity ligands such as HB-EGF are more difficult to target with decoy antibodies compared to low-affinity ligands such as amphiregulin (AREG). To address this issue, we developed an alternative method for inhibiting HB-EGF activity by targeting its cleavage from the cell surface. In a model of the invasive disease endometriosis, we identified A Disintegrin and Metalloproteinase 12 (ADAM12) as a protease implicated in HB-EGF shedding. We designed a specific inhibitor of ADAM12 based on its recombinant prodomain (PA12), which selectively inhibits ADAM12 but not ADAM10 or ADAM17. In endometriotic cells, PA12 significantly reduced HB-EGF shedding and resultant cellular migration. Overall, specific inhibition of ligand shedding represents a possible alternative to decoy antibodies, especially for ligands such as HB-EGF that exhibit high binding affinity and localized signaling.
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