RGNCY-0052 (SCB4380 PTPRZ inhibitor)

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SCB4380 is the first potent inhibitor of PTPRZ (protein tyrosine phosphatase receptor type Z) that is aberrantly over-expressed in glioblastoma and is a causative factor for its malignancy.  Biochemical and mass spectrometric analyses demonstrated the binding of SCB4380 to the catalytic pocket.  The crystal structure of the catalytic domain of PTPRZ was determined and the structural basis of binding shown by molecular docking and validated by site-directed mutagenesis.  The intracellular delivery of SCB4380 by lipososome carriers inhibited PTPRZ activity in C6 glioblastoma cells.  This resulted in suppression of C6 cell migration and proliferation in vitro and tumor rat growth in a rat allograft model.  The selective inhibition of PTPRZ by SC4380 presents a promising approach for glioblastoma therapy.

Systematic Name:  sodium 3-hydroxy-4-((4-sulfonatonaphthalen-1-yl)diazenyl)naphthalene-2,7-disulfonate

SMILES:  OC1=C(N=NC2=CC=C(S(=O)(O[Na])=O)C3=CC=CC=C23)C(C=CC(S(=O)(O[Na])=O)=C4)=C4C=C1S(=O)(O[Na])=O

Formula:  C20H11N2Na3O10S3

Mol Wt: 604.46

PMID:  26857455

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