DX-2507   Click here for help

GtoPdb Ligand ID: 9959

Immunopharmacology Ligand
Compound class: Antibody
Comment: DX-2507 is a fully human anti-FcRn monoclonal antibody [2] that was originally developed by Dyax Corporation, and is being progressed by Shire following their acquisition of Dyax.
A X-ray crystal structure of DX-2507-Fab in complex with FcRn has been published [1]. The Protein Data Bank identifier for the 2.15Å structure of unbound DX-2507-Fab is 5WHJ.
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Bioactivity Comments
DX-2507 binds IgG throughout the endocytic/exocytosis cycle both in the endosome at acidic pH and at the cell surface at neutral pH [2]. It depletes IgG in monkeys by >60% following two subcutaneous injections [2]. DX-2507 does not disrupt serum albumin binding to FcRn. It does not induce hypogammaglobulinemia and has no effect on other classes of antibodies. Nor does DX-2507 disrupt the primary response to novel antigen. All indications are that DX-2507-mediated FcRn antagonism has little implication with regards to general immune system disruption or infection risk.
Selectivity at other protein targets
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
Fc fragment of IgG receptor and transporter Primary target of this compound Hs Antibody Antagonist 8.7 pKd - 2
pKd 8.7 (Kd 1.8x10-9 M) [2]
Description: Binding affinity at acidic pH (6.0).