Delving into the Latest Updates on TMU-7 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

EZH2 x HSP90

Action

inhibitors

Mechanism

EZH2 inhibitors(Histone-lysine N-methyltransferase EZH2 inhibitors), HSP90 inhibitors(Heat shock 90kDa proteins inhibitors)

Therapeutic Areas

NeoplasmsNervous System DiseasesOther Diseases

Active Indication

Glioblastoma

Inactive Indication-

Originator Organization

Taipei Medical University

Active Organization

Taipei Medical University

Inactive Organization-

License Organization-

Drug Highest PhaseDiscovery

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC40H48N4O6

InChIKeyHFGQPOCPRWCSRT-UHFFFAOYSA-N

CAS Registry-

Structural analysis of tazemetostat, an FDA-approved EZH2 inhibitor, led us to pinpoint a suitable site for appendage with a pharmacophoric fragment of second-generation HSP90 inhibitors. Resultantly, a magnificent dual EZH2/HSP90 inhibitor was pinpointed that exerted striking cell growth inhibitory efficacy against TMZ-resistant Glioblastoma (GBM) cell lines. Exhaustive explorations of chemical probe 7 led to several revelations such as (i) compound 7 increased apoptosis/necrosis-related gene expression, whereas decreased M phase/kinetochore/spindle-related gene expression as well as CENPs protein expression in Pt3R cells; (ii) dual inhibitor 7 induced cell cycle arrest at the M phase; (iii) compound 7 suppressed reactive oxygen species (ROS) catabolism pathway, causing the death of TMZ-resistant GBM cells; and (iv) compound 7 elicited substantial in vivo anti-GBM efficacy in experimental mice xenografted with TMZ-resistant Pt3R cells. Collectively, the study results confirm the potential of dual EZH2-HSP90 inhibitor 7 as a tractable anti-GBM agent.

01 Jul 2017·Ultrasonics SonochemistryQ1 · CHEMISTRY

Porosity and dye adsorption enhancement by ultrasonic synthesized Cd(II) based metal-organic framework

Q1 · CHEMISTRY

Article

Author: Morsali, Ali ; Masoomi, Mohammad Yaser ; Bagheri, Minoo

A Cd(II) based metal-organic framework, TMU-7, was synthesized by incorporation of V-shaped flexible dicarboxylate ligand and the N-donor pillar ligand using sonochemical method while morphology and size of particles were investigated and characterized by scanning electron microscopy and X-ray powder diffraction. Moreover, N₂ adsorption was applied to examine the effect of synthesis method on porosity. Also TMU-7 was evaluated for its Congo red adsorption.

100 Deals associated with TMU-7

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