A squalamine derivative, NV669, as a novel PTP1B inhibitor: in vitro and in vivo effects on pancreatic and hepatic tumor growth.

A squalamine derivative, NV669, as a novel PTP1B inhibitor: in vitro and in vivo effects on pancreatic and hepatic tumor growth. Oncotarget. 2019 Nov 19;10(62):6651-6667 Authors: Carmona S, Brunel JM, Bonier R, Sbarra V, Robert S, Borentain P, Lombardo D, Mas E, Gerolami R Abstract NV669 is an aminosterol derived from squalamine found to possess strong anticancer effects. The aim of this study was to investigate NV669's beneficial effects on human pancreatic and hepatic cancer models and to decipher the cellular and molecular mechanisms involved in tumor growth decrease upon treatment with NV669. Pancreatic (BxPC3, MiaPaCa-2) and hepatic (HepG2, Huh7) cancer cells were treated with NV669, and the effects recorded on proliferation, cell cycle and death. Results showed that NV669 inhibited the viability of cancer cells, induced cell cycle arrest and subsequently promoted apoptosis. This was accompanied by a decrease in the expression of cyclin B1 and phosphorylated Cdk1 and by a cleavage of pro-apoptotic caspase-8 and PARP-1. Taken together, our studies showed that NV669 inhibits the proliferation of pancreatic and hepatic cancer cells through the regulation of G2/M phase transition via the cyclin B1-Cdk1 complex. In vitro NV669 inhibits PTP1B activity and FAK expression. NV669 impacts on the expression of adhesion molecules CDH-1, -2 and -3 in BxPC3 and Huh7 lines that form cell monolayers. Consecutively NV669 induces cell detachment. This suggests that NV...
Source: Oncotarget - Category: Cancer & Oncology Tags: Oncotarget Source Type: research

Related Links:

Publication date: March 2020Source: Biomedicine &Pharmacotherapy, Volume 123Author(s): Ying Wang, Nayiyuan Wu, Xia Luo, Xiaoyun Zhang, Qianjin Liao, Jing WangAbstractSOX2OT is a long non-coding RNA that is highly expressed in embryonic stem cells. The SOX2OT gene is comprised of 10 exons and more than two transcription start sites. Dysregulation of SOX2OT is observed in various tumors, including lung cancer, gastric cancer, esophageal cancer, breast cancer, hepatocellular carcinoma, ovarian cancer, pancreatic ductal adenocarcinoma, laryngeal squamous cell carcinoma, cholangiocarcinoma, osteosarcoma, nasopharyngeal carc...
Source: Biomedicine and Pharmacotherapy - Category: Drugs & Pharmacology Source Type: research
Conclusion.A significant subset of patients with mPDAC can achieve long‐term survival (≥18 months) in 2018. We identified low NLR as a significant prognostic factor associated with long‐term survival in mPDAC.Implications for Practice.Metastatic pancreatic ductal adenocarcinoma (mPDAC) is one of the most lethal types of cancer. A subset of patients with mPDAC can achieve long‐term survival (≥18 months) with a modern chemotherapy regimen, such as FOLFIRINOX or gemcitabine/nab‐paclitaxel. We identified low neutrophil‐to‐lymphocyte ratio (NLR) as a significant prognostic factor associated with long‐term su...
Source: The Oncologist - Category: Cancer & Oncology Authors: Tags: Gastrointestinal Cancer Source Type: research
Abstract Pancreatic invasive ductal adenocarcinoma (PDAC) is a representative intractable malignancy under the current cancer therapies, and is considered a scirrhous carcinoma because it develops dense stroma. Both PODXL1, a member of CD34 family molecules, and C5aR, a critical cell motility inducer, have gained recent attention, as their expression was reported to correlate with poor prognosis for patients with diverse origins including PDAC; however, previous studies reported independently on their respective biological significance. Here we demonstrate that PODXL1 is essential for metastasis of PDAC cells thro...
Source: Neoplasia - Category: Cancer & Oncology Authors: Tags: Neoplasia Source Type: research
Authors: Hyde AJ, Nassabein R, AlShareef A, Armstrong D, Babak S, Berry S, Bossé D, Chen E, Colwell B, Essery C, Goel R, Goodwin R, Gray S, Hammad N, Jeyakuymar A, Jonker D, Karanicolas P, Lamond N, Letourneau R, Michael J, Patil N, Powell E, Ramjeesingh R, Saliba W, Singh R, Snow S, Stuckless T, Tadros S, Tehfé M, Thana M, Thirlwell M, Vickers M, Virik K, Welch S, Asmis T Abstract The annual Eastern Canadian Gastrointestinal Cancer Consensus Conference was held in Halifax, Nova Scotia, 20-22 September 2018. Experts in radiation oncology, medical oncology, surgical oncology, and pathology who are invo...
Source: Current Oncology - Category: Cancer & Oncology Tags: Curr Oncol Source Type: research
RAS protein activator like 2 (RASAL2) belongs to the RAS GTPase-activating protein family and plays an important role in several cancers, including ovarian cancer, nasopharyngeal carcinoma, malignant astrocytoma, renal cell carcinoma, bladder cancer, colorectal cancer, liver cancer, triple-negative breast cancer, lung adenocarcinoma, and pancreatic ductal adenocarcinoma. Traditionally, RASAL2 has been regarded as a tumor suppressor but recent studies have found that it is an oncogene in specific types of cancer, such as colorectal cancer, liver cancer, triple-negative breast cancer, triple-negative/estrogen receptor-negati...
Source: Frontiers in Oncology - Category: Cancer & Oncology Source Type: research
ConclusionThe results of our series of 13 cases indicate that intraoral soft tissue metastatic carcinomas have a male predilection with a male to female ratio of 11:2, are commonly found in the gingiva and alveolar mucosa (76.9%), present frequently as an easy-bleeding pyogenic granuloma-like lesion (92.3%). In addition, the most common primary cancer site is the liver.
Source: Journal of Dental Sciences - Category: Dentistry Source Type: research
Conclusion: Low expressing levels of miRNA-15a indicated poor OS, while miRNA-15a can be used as a prediction biomarker in different cancer types. PMID: 31061821 [PubMed - indexed for MEDLINE]
Source: Biomed Res - Category: Research Authors: Tags: Biomed Res Int Source Type: research
Abstract Myoferlin, a protein of the ferlin family, has seven C2 domains and exhibits activity in some cells, including myoblasts and endothelial cells. Recently, myoferlin was identified as a promising target and biomarker in non-small-cell lung cancer, breast cancer, pancreatic adenocarcinoma, hepatocellular carcinoma, colon cancer, melanoma, oropharyngeal squamous cell carcinoma, head and neck squamous cell carcinoma, clear cell renal cell carcinoma and endometrioid carcinoma. This evidence indicated that myoferlin was involved in the proliferation, invasion and migration of tumour cells, the mechanism of which...
Source: J Cell Mol Med - Category: Molecular Biology Authors: Tags: J Cell Mol Med Source Type: research
CONCLUSIONS: Combining an anti-PD-1 antibody, nivolumab, with a Treg-depleting anti-CCR4 antibody, mogamulizumab, provides an acceptable safety profile, antitumor activity, and a potentially effective option in cancer immunotherapy. PMID: 31455681 [PubMed - as supplied by publisher]
Source: Clinical Cancer Research - Category: Cancer & Oncology Authors: Tags: Clin Cancer Res Source Type: research
Despite histological evidence in various solid tumor entities, available experience with CXCR4-directed diagnostics and endoradiotherapy mainly focuses on hematologic diseases. With the goal of expanding the application of CXCR4 theranostics to solid tumors, we aimed to elucidate the feasibility of CXCR4-targeted imaging in a variety of such neoplasms. Methods: 19 patients with newly diagnosed, treatment-naïve solid tumors including pancreatic adenocarcinoma or neuroendocrine tumor, cholangiocarcinoma, hepatocellular carcinoma, renal cell carcinoma, ovarian cancer, and prostate cancer underwent [68Ga]Pentixafor PET/...
Source: Frontiers in Oncology - Category: Cancer & Oncology Source Type: research
More News: Adenocarcinoma | Cancer | Cancer & Oncology | Carcinoma | Hepatocellular Carcinoma | Liver Cancer | Pancreas | Pancreatic Cancer | Study