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Small Molecule Modulation of NOS1AP for Molecularly Targeted Glioblastoma Therapy

Sep 2026 · Life · Vol 16, pp. 1519 · 0 citations · 32 references
Medicine

TL;DR

This study identifies an initial NOS1AP-binding compound and shows that it can alter a NOS1AP-containing protein complex in living cells, and provides a foundation for optimizing NOS1AP-directed compounds and developing delivery systems to enhance brain penetration, tumor-selective accumulation, and therapeutic exposure in future studies.

Abstract

Simple Summary Glioblastoma is an aggressive brain cancer for which new therapeutic targets and drug-delivery strategies are urgently needed. NOS1AP is a signaling protein associated with glioma-cell growth, but it has not previously been directly targeted for glioblastoma therapy. This study identifies an initial NOS1AP-binding compound and shows that it can alter a NOS1AP-containing protein complex in living cells. Experiments in two glioblastoma cell models demonstrated concentration-dependent reductions in viability, while normal human astrocytes were substantially less sensitive. The findings provide a foundation for optimizing NOS1AP-directed compounds and developing delivery systems to enhance brain penetration, tumor-selective accumulation, and therapeutic exposure in future studies.

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