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| Content Provider | PubMed Central |
|---|---|
| Author | Moody, Terry W. Mantey, Samuel A. Moreno, Paola Nakamura, Taichi Enza, Lacivita Leopoldo, Marcello Jensen, Robert T. |
| Abstract | Bombesin receptor subtype (BRS)-3 is a G protein coupled receptor (GPCR) for the bombesin (BB)-family of peptides. BRS-3 is an orphan GPCR and little is known of its physiological role due to the lack of specific agonists and antagonists. PD168368 is a nonpeptide antagonist for the neuromedin B (NMB) receptor (R) whereas PD176252 is a nonpeptide antagonist for the gastrin releasing peptide (GRP) R and NMBR but not BRS-3. Here nonpeptide analogs of PD176252 e.g. the S-enantiomer ML-18, and the R-enantiomer, EMY-98, were investigated as BRS-3 antagonists using lung cancer cells. ML-18 and EMY-98 inhibited specific 125I-BA1 (DTyr-Gln-Trp-Ala-Val-βAla-His-Phe-Nle-NH2)BB6-14 binding to NCI-H1299 lung cancer cells stably transfected with BRS-3 with IC50 values of 4.8 and > 100 μM, respectively. In contrast, ML-18 bound with lower affinity to the GRPR and NMBR with IC50 values of 16 and >100 μM, respectively. ML-18 (16 μM), but not its enantiomer EMY-98, inhibited the ability of 10 nM BA1 to elevate cytosolic Ca2+ in a reversible manner using lung cancer cells loaded with FURA2-AM. ML-18 (16 μM), but not EMY-98, inhibited the ability of 100 nM BA1 to cause tyrosine phosphorylation of the EGFR and ERK in lung cancer cells. ML-18 but not EMY-98 inhibited the proliferation of lung cancer cells. The results indicate that ML-18 is a nonpeptide BRS-3 antagonist that should serve as a template to improve potency and selectivity. |
| Related Links | http://dx.doi.org/10.1016/j.peptides.2014.12.005 |
| Ending Page | 61 |
| Page Count | 7 |
| Starting Page | 55 |
| File Format | |
| ISSN | 18735169 |
| e-ISSN | 18735169 |
| Journal | Peptides |
| Volume Number | 64 |
| Language | English |
| Publisher Date | 2015-02-01 |
| Access Restriction | Open |
| Subject Keyword | Research in Higher Education |
| Content Type | Text |
| Resource Type | Article |
| Subject | Physiology Biochemistry Cellular and Molecular Neuroscience Endocrinology |
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