GtoPdb Ligand ID: 10013

Synonyms: AbGn-168 | neihulizumab
Compound class: Antibody
Comment: AbGn-168H (neihulizumab) is a first-in-class, humanised anti-P-selectin glycoprotein 1 (PSGL-1) monoclonal antibody that is being developed by AbGenomics [2-3]. AbGn-168H targets the PSGL-1/P-selectin pathway that is involved in leukocyte recruitment to inflammatory sites. It blocks PSGL-1 expressed by activated T cells or NK cells, and inhibits their interaction with P-selectin on endothelial cells of the vasculature. AbGn-168H binds to a different epitope on P-selectin compared to the endogenous ligand PSGL-1 so it is not expected to interfere with the P-selectin-dependent recruitment of leukocytes that is essential for innate immunity. Nor does it alter aggregation of human platelets which express low levels of PSGL-1 [3].
Patent analysis identifies SEQ ID: 25 from AbGenomics' 2009 patent US7604800 [3] as the likely light chain variable region of AbGn-168H (DIQMTQSPSLSASVGDRVTITCRSSQSIVHNDGNTYFEWYQQKPGKAPKLLIYKVSNRFSGVPSRFSGSGSGTHFTLTISSLQPEDFATYYCFQGSYVPLTFGQGTKVEIK) and SEQ ID: 26 that is claimed in the same patent (EVQLVESGGGLVQPGGSLRLSCAASGFTFSTYAMSWVRQAPGKGLEWVASISTGGSTYYPDSVKGRFTISRDNAKNTLYLQMNSLRAEDTAVYYCARDYDGYFDYWGQGTLVTVSS) is the likely heavy chain. AbGn-168H was humanised from a murine anti-PSGL-1 antibody referred to as 15A7 [3].
Selectivity at ligand targets
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Target Sp. Type Action Value Parameter Concentration range (M) Reference
selectin P ligand Hs Antibody Agonist 11.5 pKd - 3
pKd 11.5 (Kd 3x10-12 M) [3]
Description: Kd calculated as the inverse of the Ka (333 nM) presented in the patent reference. Ka was calculated from a competition binding assay that measured displacement of murine anti-PSGL-1 antibody 15A7 by AbGn-168H from purified PSGL-1.