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bocunebart   Click here for help

GtoPdb Ligand ID: 14313

Synonyms: ALD-1910 | ALD1910 | LU AG-09222 | Lu AG09222 | Lu-AG09222 | LuAG09222
Compound class: Antibody
Comment: Bocunebart (Lu AG09222 from Lundbeck; formerly ALD1910) is a humanized monoclonal antibody that targets both isoforms of PACAP (PACAP-27 and PACAP-38) [1-2]. It is designed to disrupt PACAP signaling via its receptors as a mechanism to reduce migraine episodes [2-3]. The PACAP epitope engaged by Lu AG09222 is nonlinear, with interactions at amino acids in positions 19, 22, 23, and/or 27 required for potent binding.
Bioactivity Comments
Lu AG09222 inhibits PACAP-38- and PACAP-27-induced cAMP accumulation in SH-SY5Y and PC12 cells (i.e., PAC1 receptor signaling) with picomolar IC50 values [2]. It inhibits PACAP-38- and PACAP-27-mediated signaling via human VPAC1 and VPAC2 at nanomolar concentrations. The antibody is predicted to bind mouse and rat PACAP peptides due to sequence homology with the human peptides.
Selectivity at ligand targets
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
PACAP-38 Hs None Binding 10.7 pKd - 2
⤷ pKd 10.7 (Kd 2.2x10-11 M) Ligand-binding antibody [2]
PACAP-27 Hs None Binding 10.2 pKd - 2
⤷ pKd 10.2 (Kd 5.9x10-11 M) Ligand-binding antibody [2]