Ionotropic glutamate (iGlu) receptors play a key role in many central nervous system processes. The dysfunction of such receptors is related to many neurogenerative disorders. Hence, substrates that target these receptors are potential therapeutic agents for the treatment of those neurological diseases.
Yanli Zhao and co-workers, Nanyang Technological University, Singapore, have developed a combination treatment for metastatic melanoma cancer that uses mesoporous silica nanoparticles (MSNPs) as carriers for a neuroprotective drug, N-(4-hydroxylphenylacetyl) spermine, which is an iGlu receptor antagonist, and an anticancer drug, doxorubicin (Dox). In vitro studies on B16F10 and NIH3T3 cell lines revealed that the iGlu receptor antagonist exhibited therapeutic as well as targeting effects. In addition, the simultaneous use of the antagonist with Dox proved to be synergistic in the treatment of cancer.
The functionalized MSNPs loaded with Dox and capped with thiol cleavable groups have demonstrated selective drug release to cancer cells over normal cells. It is hoped that this method can also be used in combination with different anticancer drugs.
- An iGlu Receptor Antagonist and Its Simultaneous Use with an Anticancer Drug for Cancer Therapy,
Si Yu Tan, Chung Yen Ang, Zhong Luo, Peizhou Li, Kim Truc Nguyen, Yanli Zhao,
Chem. Europ. J. 2015.