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MTP142

Development stage: Preclinical
Modality: Small Molecules

Overview

MTP142 is a novel indole-based multitarget small molecule (MSM) designed for the treatment of glioblastoma. It was developed by combining pharmacophoric moieties from the HDAC inhibitor belinostat and the multitarget compound contilisant. MTP142 is engineered to simultaneously inhibit histone deacetylases (HDACs), monoamine oxidases (MAOs), and cholinesterases (ChEs), while also acting as a histamine H3 receptor (H3R) antagonist and a sigma-1 receptor (S1R) agonist. In preclinical studies, MTP142 demonstrated cytotoxic activity against glioma cells and impaired glioma stem cell (GSC) activity. It is predicted to cross the blood-brain barrier, making it a candidate for treating malignant primary brain tumors.

Targets

HRH3 (Histamine Receptor H3)SIGMAR1 (Sigma non-opioid intracellular receptor 1)AcetylcholinesteraseHDAC (HDAC family)MAOA (Monoamine oxidase A)

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