The novel sigma-2 receptor ligand SW43 stabilizes pancreas cancer progression in combination with gemcitabine
<p>Abstract</p> <p>Background</p> <p>Sigma-2 receptors are over-expressed in proliferating cancer cells, making an attractive target for the targeted treatment of pancreatic cancer. In this study, we investigated the role of the novel sigma-2 receptor ligand SW43 to ind...
| Main Authors: | , , , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
BMC
2010-11-01
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| Series: | Molecular Cancer |
| Online Access: | http://www.molecular-cancer.com/content/9/1/298 |
| _version_ | 1811319848899182592 |
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| author | Goedegebuure Peter Spitzer Dirk Mitchem Jonathan B Tu Zhude Vangveravong Suwanna Xu Jinbin Hornick John R Mach Robert H Hawkins William G |
| author_facet | Goedegebuure Peter Spitzer Dirk Mitchem Jonathan B Tu Zhude Vangveravong Suwanna Xu Jinbin Hornick John R Mach Robert H Hawkins William G |
| author_sort | Goedegebuure Peter |
| collection | DOAJ |
| description | <p>Abstract</p> <p>Background</p> <p>Sigma-2 receptors are over-expressed in proliferating cancer cells, making an attractive target for the targeted treatment of pancreatic cancer. In this study, we investigated the role of the novel sigma-2 receptor ligand SW43 to induce apoptosis and augment standard chemotherapy.</p> <p>Results</p> <p>The binding affinity for sigma-2 ligands is high in pancreas cancer, and they induce apoptosis with a rank order of SV119 < SW43 < SRM <it>in vitro</it>. Combining these compounds with gemcitabine further increased apoptosis and decreased viability. Our <it>in vivo </it>model showed that sigma-2 ligand treatment decreased tumor volume to the same extent as gemcitabine. However, SW43 combination treatment with gemcitabine was superior to the other compounds and resulted in stabilization of tumor volume during treatment, with minimal toxicities.</p> <p>Conclusions</p> <p>This study shows that the sigma-2 ligand SW43 has the greatest capacity to augment gemcitabine in a pre-clinical model of pancreas cancer and has provided us with the rationale to move this compound forward with clinical investigations for patients with pancreatic cancer.</p> |
| first_indexed | 2024-04-13T12:49:35Z |
| format | Article |
| id | doaj.art-b71f817e0f2a4897a94924c9467bba7a |
| institution | Directory Open Access Journal |
| issn | 1476-4598 |
| language | English |
| last_indexed | 2024-04-13T12:49:35Z |
| publishDate | 2010-11-01 |
| publisher | BMC |
| record_format | Article |
| series | Molecular Cancer |
| spelling | doaj.art-b71f817e0f2a4897a94924c9467bba7a2022-12-22T02:46:16ZengBMCMolecular Cancer1476-45982010-11-019129810.1186/1476-4598-9-298The novel sigma-2 receptor ligand SW43 stabilizes pancreas cancer progression in combination with gemcitabineGoedegebuure PeterSpitzer DirkMitchem Jonathan BTu ZhudeVangveravong SuwannaXu JinbinHornick John RMach Robert HHawkins William G<p>Abstract</p> <p>Background</p> <p>Sigma-2 receptors are over-expressed in proliferating cancer cells, making an attractive target for the targeted treatment of pancreatic cancer. In this study, we investigated the role of the novel sigma-2 receptor ligand SW43 to induce apoptosis and augment standard chemotherapy.</p> <p>Results</p> <p>The binding affinity for sigma-2 ligands is high in pancreas cancer, and they induce apoptosis with a rank order of SV119 < SW43 < SRM <it>in vitro</it>. Combining these compounds with gemcitabine further increased apoptosis and decreased viability. Our <it>in vivo </it>model showed that sigma-2 ligand treatment decreased tumor volume to the same extent as gemcitabine. However, SW43 combination treatment with gemcitabine was superior to the other compounds and resulted in stabilization of tumor volume during treatment, with minimal toxicities.</p> <p>Conclusions</p> <p>This study shows that the sigma-2 ligand SW43 has the greatest capacity to augment gemcitabine in a pre-clinical model of pancreas cancer and has provided us with the rationale to move this compound forward with clinical investigations for patients with pancreatic cancer.</p>http://www.molecular-cancer.com/content/9/1/298 |
| spellingShingle | Goedegebuure Peter Spitzer Dirk Mitchem Jonathan B Tu Zhude Vangveravong Suwanna Xu Jinbin Hornick John R Mach Robert H Hawkins William G The novel sigma-2 receptor ligand SW43 stabilizes pancreas cancer progression in combination with gemcitabine Molecular Cancer |
| title | The novel sigma-2 receptor ligand SW43 stabilizes pancreas cancer progression in combination with gemcitabine |
| title_full | The novel sigma-2 receptor ligand SW43 stabilizes pancreas cancer progression in combination with gemcitabine |
| title_fullStr | The novel sigma-2 receptor ligand SW43 stabilizes pancreas cancer progression in combination with gemcitabine |
| title_full_unstemmed | The novel sigma-2 receptor ligand SW43 stabilizes pancreas cancer progression in combination with gemcitabine |
| title_short | The novel sigma-2 receptor ligand SW43 stabilizes pancreas cancer progression in combination with gemcitabine |
| title_sort | novel sigma 2 receptor ligand sw43 stabilizes pancreas cancer progression in combination with gemcitabine |
| url | http://www.molecular-cancer.com/content/9/1/298 |
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