Drug intelligence / Profile preview

MMP-9 PI polyamide

Development stage
Preclinical
Lead developer
Nihon University
Modality
Small Molecules
Administration
Intravenous
01

Overview

MMP-9 PI polyamide is a synthetic pyrrole-imidazole (PI) polyamide designed as a sequence-specific gene-silencing agent targeting the promoter region of the human matrix metalloproteinase 9 (MMP-9) gene. Developed by Nihon University and Gentier Biosystems, these small molecules bind with high affinity to the minor groove of double-helical DNA, effectively blocking the binding of key transcription factors to their cognate response elements. Two primary variants have been evaluated: one targeting the activator protein-1 (AP-1) binding site (MMP-9-AP-1 PIP) and another targeting the nuclear factor-kappa B (NF-κB) binding site (MMP-9-NF-κB PIP, also known as HN.49). By preventing transcription factor engagement, the polyamides suppress MMP-9 mRNA and protein expression, thereby inhibiting extracellular matrix degradation, tumor cell invasion, and metastasis. Preclinical studies have demonstrated significant efficacy in reducing cell migration and invasion in vitro (including breast cancer, osteosarcoma, and renal cell carcinoma models) and suppressing liver metastasis in vivo.

Other names
HN.49 polyamideMMP-9-AP-1 PI polyamideMMP9-AP-1 PI polyamideMMP 9-AP-1 PI polyamideMMP-9-AP-1 PIPMMP9-AP-1 PIPMMP 9-AP-1 PIPMMP-9-NF-κB PI polyamideMMP-9-NF-κB PIPMMP-9-targeting pyrrole-imidazole polyamideMMP9-targeting pyrrole-imidazole polyamideMMP 9-targeting pyrrole-imidazole polyamidepyrrole-imidazole polyamide targeting MMP-9
02

Targets

DNA

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