ADAM proteases: Emerging role and targeting of the non-catalytic domains.

摘要: Abstract ADAM proteases are multi domain transmembrane metalloproteases that cleave a range of cell surface proteins and activate signaling pathways implicated in tumor progression, including those mediated by Notch, EFGR, the Eph receptors. Consequently, they have emerged as key therapeutic targets efforts to inhibit initiation progression. To end, two main approaches been taken develop antagonists: (i) small molecule inhibitors, (ii) monoclonal antibodies. In this mini-review we describe distinct features proteases, particularly ADAM10 ADAM17, their organization, conformational rearrangements, regulation, well emerging importance cancer. Further, highlight an anti-ADAM10 antibody recently developed, which has shown significant promise inhibiting Notch deterring growth solid tumors pre-clinical settings.