Rethinking Glioblastoma Therapy: MDA-9/Syntenin Targeted Small Molecule

Swadesh K Das; Devanand Sarkar; Webster K Cavenee; Luni Emdad; Paul B Fisher

doi:10.1021/acschemneuro.9b00016

Rethinking Glioblastoma Therapy: MDA-9/Syntenin Targeted Small Molecule

ACS Chem Neurosci. 2019 Mar 20;10(3):1121-1123. doi: 10.1021/acschemneuro.9b00016. Epub 2019 Jan 25.

Authors

Swadesh K Das^{1

2

3}, Devanand Sarkar^{1

2

3}, Webster K Cavenee⁴, Luni Emdad^{1

2

3}, Paul B Fisher^{1

2

3}

Affiliations

¹ Department of Human and Molecular Genetics , Virginia Commonwealth University, School of Medicine , Richmond , Virginia 23298 , United States.
² VCU Institute of Molecular Medicine , Virginia Commonwealth University, School of Medicine , Richmond , Virginia , 23298 , United States.
³ VCU Massey Cancer Center , Virginia Commonwealth University, School of Medicine , Richmond , Virginia , 23298 , United States.
⁴ Ludwig Institute for Cancer Research , University of California , San Diego , California 92093 , United States.

PMID: 30681320
DOI: 10.1021/acschemneuro.9b00016

Abstract

Effective therapies for glioblastoma multiforme (GBM) are not currently available. A small molecule has been identified using fragment-based drug-discovery guided by NMR that targets important protein-protein interactions controlling GBM invasion and pathogenicity. This first generation drug displays excellent pharmacokinetic properties, passes through the blood-brain barrier and is effective in preclinical animal models of GBM, particularly when combined with radiation therapy.

Keywords: Glioblastoma multiforme; MDA-9/Syntenin; invasion; pathogenicity.

Publication types

Research Support, N.I.H., Extramural
Research Support, Non-U.S. Gov't
Review

MeSH terms

Animals
Antineoplastic Agents / administration & dosage*
Antineoplastic Agents / metabolism*
Brain Neoplasms / drug therapy
Brain Neoplasms / metabolism*
Drug Delivery Systems / methods
Drug Delivery Systems / trends*
Glioblastoma / drug therapy
Glioblastoma / metabolism*
Humans
Syntenins / antagonists & inhibitors
Syntenins / metabolism*

Substances

Antineoplastic Agents
SDCBP protein, human
Syntenins