pd-176252 has been researched along with Neoplasms* in 2 studies
1 review(s) available for pd-176252 and Neoplasms
| Article | Year |
|---|---|
Gastrin-Releasing Peptide Receptor Targeting in Cancer Treatment: Emerging Signaling Networks and Therapeutic Applications.
Growth factors of the bombesin/gastrin releasing peptide (BN/GRP) family play a critical role in proliferation and progression of malignancies. Inhibitors targeting GRP signalling have been developed and tested as anticancer compounds showing promising preclinical and early phase clinical results. In this review, we will discuss the molecular signaling, expression and the functional role of BN/GRP-GRPR in different cancer models and will focus on the available strategies to target BN/GRP-GRPR in cancer treatment as well as in tumour diagnosis and follow up. Topics: Animals; Antineoplastic Agents; Bombesin; Clinical Trials as Topic; Female; Gastrin-Releasing Peptide; Humans; Indoles; Male; Neoplasms; Peptide Fragments; Receptors, Bombesin; Signal Transduction | 2016 |
1 other study(ies) available for pd-176252 and Neoplasms
| Article | Year |
|---|---|
Design, Synthesis and Biological Evaluation of Novel 1, 3, 4-Oxadiazole PD176252 Analogues as Potential GRPR Inhibitors.
GRPR is over-expressed in cancer cells and is a potential drug target for the treatment of cancer. PD176252, as the most representative non-peptide inhibitor of GRPR, can inhibit the growth of cancer cells, but its low selectivity to cancer cells and normal cells limits its further application.. The aim of this study was to design and synthesize novel GRPR inhibitor with stronger anti-cancer activity and higher affinity with GRPR than the lead compound PD176252.. A series of 1, 3, 4-oxadiazole derivatives as PD176252 analogues (4a-4j, 6a-6q) were synthesized and their cytotoxic activity was investigated on four cancer lines with high expression of GRPR (gastric (HGC-27), colon (HCT- 116), prostate (PC-3), and lung (A549)) and one human cell line (gastric mucosal epithelial (GES-1)) by MTT assay. Flow cytometry analysis and Western Blot were used to determine whether the compound induced programmed apoptosis of cancer cells. Competitive binding experiment was used to verify the affinity between GRPR and the optimal compound.. Compound 6m exhibited significant growth inhibition on all tested cancer cell lines, especially gastric cancer cells (HGC-27 cellular IC. Our results suggested that 6m, as a novel GRPR inhibitor, had a higher affinity with GRPR and potential anti-cancer effect than PD176252, which can be used as a template for further optimization. Topics: Antineoplastic Agents; Apoptosis; Cell Line, Tumor; Cell Proliferation; Drug Screening Assays, Antitumor; Humans; Indoles; Male; Neoplasms; Oxadiazoles | 2022 |