Abstract
In spite of the recent advancement in the molecular characterization of malignant gliomas and medulloblastomas, the treatment of primary brain tumors remains suboptimal. The use of small molecule inhibitors of intracellular signaling pathways, inhibitors of angiogenesis, and immunotherapic agents is limited by systemic adverse effects, limited brain penetration, and, in some cases, lack of efficacy. Thus, adjuvant chemo-therapy and radiotherapy still remain the gold standard in the treatment of grade-IV astrocytoma (glioblastoma multiforme) and medulloblastoma. We review evidence that supports the development of mGlu3 receptor antagonists as add-on drugs in the treatment of malignant gliomas. These drugs appear to display pleiotropic effect on tumor cells, affecting proliferation, differentiation, and response to chemotherapy. mGlu1 and mGlu4 receptors could also be targeted by potential anticancer agents in the treatment of malignant gliomas and medulloblastoma, but extensive research is required for target validation.
| Original language | English |
|---|---|
| Pages (from-to) | 59-64 |
| Number of pages | 6 |
| Journal | Current Opinion in Pharmacology |
| Volume | 38 |
| DOIs | |
| Publication status | Published - Feb 1 2018 |
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ASJC Scopus subject areas
- Pharmacology
- Drug Discovery
Cite this
Targeting metabotropic glutamate receptors in the treatment of primary brain tumors. / Iacovelli, Luisa; Orlando, Rosamaria; Rossi, Alessandro; Spinsanti, Paola; Melchiorri, Daniela; Nicoletti, Ferdinando.
In: Current Opinion in Pharmacology, Vol. 38, 01.02.2018, p. 59-64.Research output: Contribution to journal › Review article
}
TY - JOUR
T1 - Targeting metabotropic glutamate receptors in the treatment of primary brain tumors
AU - Iacovelli, Luisa
AU - Orlando, Rosamaria
AU - Rossi, Alessandro
AU - Spinsanti, Paola
AU - Melchiorri, Daniela
AU - Nicoletti, Ferdinando
PY - 2018/2/1
Y1 - 2018/2/1
N2 - In spite of the recent advancement in the molecular characterization of malignant gliomas and medulloblastomas, the treatment of primary brain tumors remains suboptimal. The use of small molecule inhibitors of intracellular signaling pathways, inhibitors of angiogenesis, and immunotherapic agents is limited by systemic adverse effects, limited brain penetration, and, in some cases, lack of efficacy. Thus, adjuvant chemo-therapy and radiotherapy still remain the gold standard in the treatment of grade-IV astrocytoma (glioblastoma multiforme) and medulloblastoma. We review evidence that supports the development of mGlu3 receptor antagonists as add-on drugs in the treatment of malignant gliomas. These drugs appear to display pleiotropic effect on tumor cells, affecting proliferation, differentiation, and response to chemotherapy. mGlu1 and mGlu4 receptors could also be targeted by potential anticancer agents in the treatment of malignant gliomas and medulloblastoma, but extensive research is required for target validation.
AB - In spite of the recent advancement in the molecular characterization of malignant gliomas and medulloblastomas, the treatment of primary brain tumors remains suboptimal. The use of small molecule inhibitors of intracellular signaling pathways, inhibitors of angiogenesis, and immunotherapic agents is limited by systemic adverse effects, limited brain penetration, and, in some cases, lack of efficacy. Thus, adjuvant chemo-therapy and radiotherapy still remain the gold standard in the treatment of grade-IV astrocytoma (glioblastoma multiforme) and medulloblastoma. We review evidence that supports the development of mGlu3 receptor antagonists as add-on drugs in the treatment of malignant gliomas. These drugs appear to display pleiotropic effect on tumor cells, affecting proliferation, differentiation, and response to chemotherapy. mGlu1 and mGlu4 receptors could also be targeted by potential anticancer agents in the treatment of malignant gliomas and medulloblastoma, but extensive research is required for target validation.
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UR - http://www.scopus.com/inward/citedby.url?scp=85043243893&partnerID=8YFLogxK
U2 - 10.1016/j.coph.2018.02.005
DO - 10.1016/j.coph.2018.02.005
M3 - Review article
VL - 38
SP - 59
EP - 64
JO - Current Opinion in Pharmacology
JF - Current Opinion in Pharmacology
SN - 1471-4892
ER -