366 results match your criteria xenograft a2780

Repositioning Trimebutine Maleate as a Cancer Treatment Targeting Ovarian Cancer Stem Cells.

Cells 2021 Apr 16;10(4). Epub 2021 Apr 16.

New Drug Development Center, DGMIF, 80 Chumbok-ro, Dong-gu, Daegu 41061, Korea.

The overall five-year survival rate for late-stage patients of ovarian cancer is below 29% due to disease recurrence and drug resistance. Cancer stem cells (CSCs) are known as a major contributor to drug resistance and recurrence. Accordingly, therapies targeting ovarian CSCs are needed to overcome the limitations of present treatments. Read More

View Article and Full-Text PDF

Targeting ACLY Attenuates Tumor Growth and Acquired Cisplatin Resistance in Ovarian Cancer by Inhibiting the PI3K-AKT Pathway and Activating the AMPK-ROS Pathway.

Front Oncol 2021 17;11:642229. Epub 2021 Mar 17.

Department of Obstetrics and Gynecology, Qilu Hospital of Shandong University, Jinan, China.

Ovarian cancer is the most lethal female genital malignancy. Although cisplatin is the first-line chemotherapy to treat ovarian cancer patients along with debulking surgeries, its efficacy is limited due to the high incidence of cisplatin resistance. ATP citrate lyase (ACLY) has been shown to be a key metabolic enzyme and is associated with poor prognosis in various cancers, including ovarian cancer. Read More

View Article and Full-Text PDF

Overexpression of NPTX2 Promotes Malignant Phenotype of Epithelial Ovarian Carcinoma IL6-JAK2/STAT3 Signaling Pathway Under Hypoxia.

Front Oncol 2021 9;11:643986. Epub 2021 Mar 9.

Department of Gynecologic Oncology, Fudan University Shanghai Cancer Center, Shanghai, China.

Background: Epithelial ovarian cancer (EOC) is the main subtype of ovarian cancer and shows an aggressive phenotype and poor prognosis. Neuronal pentraxin II (NPTX2) is a member of the neuronal pentraxin family and plays a contradictory role in different tumors. However, there has been no report about the possible role and effect of NPTX2 in EOC. Read More

View Article and Full-Text PDF

Redox-sensitive carrier-free nanoparticles self-assembled by disulfide-linked paclitaxel-tetramethylpyrazine conjugate for combination cancer chemotherapy.

Theranostics 2021 20;11(9):4171-4186. Epub 2021 Feb 20.

College of Materials Science and Engineering, Nanjing Tech Universit`y, Nanjing 211816, People's Republic of China.

Combinations of two or more therapeutic agents targeting different signaling pathways involved in tumor progression can have synergistic anticancer effects. However, combination chemotherapies are greatly limited by the different pharmacokinetics, tumor targeting, and cellular uptake capacities of the combined drugs. We have previously demonstrated the potential synergistic efficacy of paclitaxel (PTX) and the natural anti-angiogenic agent tetramethylpyrazine (TMP) for suppressing ovarian carcinoma growth. Read More

View Article and Full-Text PDF
February 2021

Long non-coding RNA SNHG1 stimulates ovarian cancer progression by modulating expression of miR-454 and ZEB1.

Mol Oncol 2021 May 19;15(5):1584-1596. Epub 2021 Mar 19.

Department of Radiotherapy, Oncology Department, First Affiliated Hospital of Xi'an Jiaotong University, China.

Ovarian cancer (OC) is highly prevalent and is associated with high mortality rates due to metastasis and relapse. In this study, we assessed the role of long non-coding RNA (lncRNA) small nucleolar RNA host gene 1 (SNHG1) in OC to gain further insight into mechanisms that contribute to its aggressiveness. We analyzed the correlation between SNHG1, miR-454 and zinc finger E-box-binding homeobox 1 (ZEB1) using a dual-luciferase reporter assay. Read More

View Article and Full-Text PDF

Near-infrared fluorescence-guided resection of micrometastases derived from esophageal squamous cell carcinoma using a c-Met-targeted probe in a preclinical xenograft model.

J Control Release 2021 Apr 24;332:171-183. Epub 2021 Feb 24.

Center for Interventional Medicine, The Fifth Affiliated Hospital, Sun Yat-sen University, Zhuhai, Guangdong Province 519000, China; Guangdong Provincial Key Laboratory of Biomedical Imaging and Guangdong Provincial Engineering Research Center of Molecular Imaging, The Fifth Affiliated Hospital, Sun Yat-sen University, Zhuhai, Guangdong Province 519000, China. Electronic address:

The postoperative survival of esophageal squamous cell carcinoma (eSCC) is notably hindered by cancer recurrence due to difficulty in identifying occult metastases. Cellular mesenchymal-epithelial transition factor (c-Met), which is highly expressed in different cancers, including eSCC, has become a target for the development of imaging probes and therapeutic antibodies. In this study, we synthesized an optical probe (SHRmAb-IR800) containing a near-infrared fluorescence (NIRF) dye and c-Met antibody, which may help in NIRF-guided resection of micrometastases derived from eSCC. Read More

View Article and Full-Text PDF

YYB-101, a Humanized Antihepatocyte Growth Factor Monoclonal Antibody, Inhibits Ovarian Cancer Cell Motility and Proliferation.

Anticancer Res 2021 Feb;41(2):671-678

Biopharmaceutical Chemistry Major, School of Applied Chemistry, Kookmin University, Seoul, Republic of Korea

Background/aim: Hepatocyte growth factor (HGF) acts as a key regulator in promoting ovarian cancer metastasis. Previously, we observed that YYB-101, a humanized anti-HGF antibody, effectively inhibits ovarian cancer cell migration, invasion, and progression. Here, we evaluated the signaling mechanisms affected by YYB-101 that are important in ovarian cancer cell progression. Read More

View Article and Full-Text PDF
February 2021

Daphnetin triggers ROS-induced cell death and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway in ovarian cancer.

Phytomedicine 2021 Feb 11;82:153465. Epub 2021 Jan 11.

Department of Obstetrics and Gynecology, The First Hospital of Jilin University, Changchun, China. Electronic address:

Background: Ovarian cancer is one of the most common gynecological malignancies in the world. Daphnetin (Daph) was previously reported to possess antitumor potential, but its potential and molecular mechanisms in ovarian cancer remain poorly understood.

Purpose: In the current study, we aimed to explore the antitumor effect and detailed mechanisms of Daph in ovarian cancer cells. Read More

View Article and Full-Text PDF
February 2021

Discovery of indole-3-butyric acid derivatives as potent histone deacetylase inhibitors.

J Enzyme Inhib Med Chem 2021 Dec;36(1):425-436

Department of Medicinal Chemistry, School of Pharmacy, Weifang Medical University, Weifang, Shandong, China.

In discovery of HDAC inhibitors (HDACIs) with improved anticancer potency, structural modification was performed on the previous derived indole-3-butyric acid derivative. Among all the synthesised compounds, molecule exhibited high HDAC inhibitory and antiproliferative potencies in the investigations. The IC values of against HDAC1, HDAC3, and HDAC6 were 13. Read More

View Article and Full-Text PDF
December 2021

Oncogenic Role of NUPR1 in Ovarian Cancer.

Onco Targets Ther 2020 30;13:12289-12300. Epub 2020 Nov 30.

Department of Obstetrics and Gynecology, Qilu Hospital, Cheeloo College of Medicine, Shandong University, Jinan 250012, People's Republic of China.

Background: Nuclear protein 1 (NUPR1) plays a critical role in the development and progression of various types of human cancers. However, the role and mechanism of NUPR1 in ovarian cancer have not been elucidated. The purpose of this study was to investigate the effect of NUPR1 on ovarian cancer in vivo and in vitro. Read More

View Article and Full-Text PDF
November 2020

Co-Delivery of Docetaxel and Curcumin via Nanomicelles for Enhancing Anti-Ovarian Cancer Treatment.

Int J Nanomedicine 2020 3;15:9703-9715. Epub 2020 Dec 3.

Department of Neurosurgery and Institute of Neurosurgery, State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University and Collaborative Innovation Center for Biotherapy, Chengdu 610041, People's Republic of China.

Introductions: Ovarian cancer is a stubborn malignancy of gynecological system with a high mortality rate. Docetaxel (DTX), the second-generation of anti-tumor drug Taxane, has shown superior efficacy over classic paclitaxel (PTX) in certain cancers. However, its clinical application is hindered by poor bioavailability. Read More

View Article and Full-Text PDF
December 2020

Chloroquine reverses chemoresistance via upregulation of p21 and autophagy inhibition in ovarian cancer.

Cell Death Dis 2020 12 4;11(12):1034. Epub 2020 Dec 4.

Department of Obstetrics and Gynecology, Samsung Medical Center, Sungkyunkwan University School of Medicine, Seoul, Republic of Korea.

Overcoming drug-resistance is a big challenge to improve the survival of patients with epithelial ovarian cancer (EOC). In this study, we investigated the effect of chloroquine (CQ) and its combination with cisplatin (CDDP) in drug-resistant EOC cells. We used the three EOC cell lines CDDP-resistant A2780-CP20, RMG-1 cells, and CDDP-sensitive A2780 cells. Read More

View Article and Full-Text PDF
December 2020

Structural optimization and biological evaluation for novel artemisinin derivatives against liver and ovarian cancers.

Eur J Med Chem 2021 Feb 7;211:113000. Epub 2020 Nov 7.

Chinese Academy of Sciences, State Key Laboratory of Drug Research and CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Shanghai, PR China; University of Chinese Academy of Sciences, Number 19A Yuquan Road, Beijing, 100049, PR China. Electronic address:

An increasing number of artemisinin (ARS) and its derivatives have been reported for their potential therapeutic value of human cancer. However, their therapeutic potencies are limited owing to their poor pharmacokinetic profiles. Our previous studies showed that a lead compound ARS4 originated from incorporating the pharmacophore of the approved chemotherapeutic agent melphalan into the basic skeleton of artemisinin with a succinic linker exhibited an excellent toxicity to human ovarian cancer cells and low cytotoxicity to normal cells. Read More

View Article and Full-Text PDF
February 2021

TIPE1 impairs ovarian tumor growth by promoting caspase-dependent apoptosis.

Oncol Lett 2020 Dec 15;20(6):365. Epub 2020 Oct 15.

Department of Gynecology and Obstetrics, Center for Reproductive Medicine, Nanfang Hospital, Southern Medical University, Guangzhou, Guangdong 510515, P.R. China.

Tumor necrosis factor-α-induced protein 8-like 1 (TIPE1) functions as a tumor suppressor in several types of cancer, including lung and breast cancer. The present study aimed to determine the level of expression and the function of TIPE1 in ovarian cancer. TIPE1 expression was determined in tissue microarrays and ovarian cancer cells, and these data were analyzed to assess the association between TIPE1 expression and prognosis in patients with ovarian cancer. Read More

View Article and Full-Text PDF
December 2020

Potential and mechanism of mebendazole for treatment and maintenance of ovarian cancer.

Gynecol Oncol 2021 Jan 31;160(1):302-311. Epub 2020 Oct 31.

Stephenson Cancer Center, University of Oklahoma Health Sciences Center, Oklahoma City 73104, OK, USA; Department of Obstetrics and Gynecology, Section of Gynecologic Oncology, College of Medicine, University of Oklahoma Health Sciences Center, Oklahoma City 73104, OK, USA. Electronic address:

Objective: Mebendazole and other anti-parasitic drugs are being used off-prescription based on social media and unofficial accounts of their anti-cancer activity. The purpose of this study was to conduct a controlled evaluation of mebendazole's therapeutic efficacy in cell culture and in vivo models of ovarian cancer. The majority of ovarian cancers harbor p53 null or missense mutations, therefore the effects of p53 mutations and a mutant p53 reactivator, PRIMA-1 (APR246) on mebendazole activity were evaluated. Read More

View Article and Full-Text PDF
January 2021

Combination of metformin and RG7388 enhances inhibition of growth and induction of apoptosis of ovarian cancer cells through the PI3K/AKT/mTOR pathway.

Biochem Biophys Res Commun 2020 12 10;533(4):665-671. Epub 2020 Oct 10.

Department of Obstetrics and Gynecology, Shandong Qianfoshan Hospital, Cheeloo College of Medicine, Shandong University, Jinan, Shandong, 250014, China. Electronic address:

Ovarian cancer is a gynecological cancer that has the highest mortality rate and is often resistant to conventional treatments. Therefore, development of new therapies is essential. Metformin (MET), which is the priority drug for treatment of type 2 diabetes, has received increasing attention because of its anti-tumor effects. Read More

View Article and Full-Text PDF
December 2020

A first-in-class CDK4 inhibitor demonstrates in vitro, ex-vivo and in vivo efficacy against ovarian cancer.

Gynecol Oncol 2020 12 18;159(3):827-838. Epub 2020 Sep 18.

Drug Discovery and Development, Cancer Research Institute and Clinical and Health Sciences, University of South Australia, Australia. Electronic address:

Introduction: Cyclin-dependent kinases 4 and 6 (CDK4/6) are fundamental drivers of the cell cycle and are involved in the initiation and progression of various cancers. Deregulation of the CDK4/6-cyclin D-retinoblastoma (Rb) pathway is common in ovarian cancer and is associated with an aggressive phenotype and poor prognosis. Patients with advanced ovarian cancer whose tumor demonstrates Rb-positivity, a low expression of p16 and overexpression of cyclin D1 are most likely to benefit from CDK4/6 inhibition. Read More

View Article and Full-Text PDF
December 2020

Co-drug delivery of regorafenib and cisplatin with amphiphilic copolymer nanoparticles: enhanced antitumor cancer therapy in nursing care.

Zhe Zhou

Drug Deliv 2020 Dec;27(1):1319-1328

Department of Oncology, Huaihe Hospital of Henan University, Kaifeng, China.

Cancers continue to be the second leading cause of death worldwide. Despite the development and improvement of surgery, chemotherapy and radiotherapy in cancer management, effective tumor ablation strategies are still in need due to high cancer patient mortality. Hence, we have established a new approach to achieve treatment-actuated modifications in a tumor microenvironment by using synergistic activity between two potential anticancer drugs. Read More

View Article and Full-Text PDF
December 2020

Discovery and Development of SPR519 as a Potent, Selective, and Orally Bioavailable Inhibitor of PI3Kα and mTOR Kinases for the Treatment of Solid Tumors.

J Med Chem 2020 10 23;63(19):11121-11130. Epub 2020 Sep 23.

Sphaera Pharma Pte. Ltd., 038988, Singapore.

Herein, we report the identification and preclinical profile of a lead compound , () as an equally potent dual inhibitor of PI3Kα and mTOR kinases. exhibits an EC of low sub-micromolar range among various tested cancer cell lines such as A2780 (0.23 μM), PC3 (0. Read More

View Article and Full-Text PDF
October 2020

The Natural Product Fucoidan Inhibits Proliferation and Induces Apoptosis of Human Ovarian Cancer Cells: Focus on the PI3K/Akt Signaling Pathway.

Cancer Manag Res 2020 23;12:6195-6207. Epub 2020 Jul 23.

Department of Gynecology, Jining First People's Hospital, Jining 272000, People's Republic of China.

Objective: Ovarian cancer (OC) is the leading cause of death among gynecological tumors; however, no effective treatment is currently available. Fucoidan, which is extracted from marine algae, has significant anti-cancer effects. The aim of this study was to determine the effects of fucoidan on the proliferation and apoptosis of OC cells through inhibition of the PI3K/Akt signaling pathway. Read More

View Article and Full-Text PDF

CD166 promotes the cancer stem-like properties of primary epithelial ovarian cancer cells.

BMB Rep 2020 Dec;53(12):622-627

Departments of Physiology, School of Medicine, Pusan National University, Yangsan 50612, Korea; Research Institute of Convergence Biomedical Science and Technology, Pusan National University Yangsan Hospital, Yangsan 50612, Korea.

Cancer stem cells (CSCs) or tumor-initiating cells are thought to play critical roles in tumorigenesis, metastasis, drug resistance, and tumor recurrence. For the diagnosis and targeted therapy of CSCs, the molecular identity of biomarkers or therapeutic targets for CSCs needs to be clarified. In this study, we identified CD166 as a novel marker expressed in the sphereforming CSC population of A2780 epithelial ovarian cancer cells and primary ovarian cancer cells. Read More

View Article and Full-Text PDF
December 2020

Novel NHC-coordinated ruthenium(II) arene complexes achieve synergistic efficacy as safe and effective anticancer therapeutics.

Eur J Med Chem 2020 Oct 12;203:112605. Epub 2020 Jul 12.

The First Affiliated Hospital, Key Laboratory of Combined Multi-Organ Transplantation, Ministry of Public Health, School of Medicine, Zhejiang University, Hangzhou, 310003, PR China. Electronic address:

There is an urgent need for more effective, less toxic cancer therapy agents. Motivated by this need, we synthesized a small panel of N-heterocyclic carbene (NHC)-coordinated ruthenium(II) arene complexes Ru1-Ru6 with the formula [Ru(p-cymene)(L)Cl]PF (L = NHC ligand with varying substituents). Cell-based in vitro studies revealed that despite the structural similarity, Ru1-Ru6 exhibited distinct cytotoxic activities against cancer cells. Read More

View Article and Full-Text PDF
October 2020

Acid-sensitive PEGylated paclitaxel prodrug nanoparticles for cancer therapy: Effect of PEG length on antitumor efficacy.

J Control Release 2020 10 17;326:265-275. Epub 2020 Jul 17.

Key Laboratory of Functional Polymer Materials of Ministry of Education, State Key Laboratory of Medicinal Chemical Biology and Institute of Polymer Chemistry, College of Chemistry, Nankai University, Tianjin 300071, China.. Electronic address:

Paclitaxel is one of the most widely used anticancer agents, but strong side effects and low bioavailability limit its clinical efficacy. The use of tumor microenvironment-responsive prodrugs is promising to solve these problems, and a smart linkage is crucial to achieve the efficient release of paclitaxel from such prodrugs in tumor. Herein, an acid-responsive acetone-based acyclic ketal linkage is used to construct paclitaxel prodrugs with different length of poly(ethylene glycol) (PEG). Read More

View Article and Full-Text PDF
October 2020

Natural compound Tan-I enhances the efficacy of Paclitaxel chemotherapy in ovarian cancer.

Ann Transl Med 2020 Jun;8(12):752

College of Science, Sichuan Agricultural University, Ya'an, China.

Background: Paclitaxel is a widely used clinical first line chemotherapy drug for ovarian carcinoma. Tanshinone I (Tan-I) is one of the vital fat-soluble components, which derived from Chinese herbal medicine, Salvia miltiorrhiza Bunge. Herein, we evaluated whether Tan-I could enhance the efficacy of ovarian cancer to chemotherapy of Paclitaxel. Read More

View Article and Full-Text PDF

New Organometallic Ruthenium(II) Compounds Synergistically Show Cytotoxic, Antimetastatic and Antiangiogenic Activities for the Treatment of Metastatic Cancer.

Chemistry 2020 Nov 6;26(66):15170-15182. Epub 2020 Oct 6.

The First Affiliated Hospital, Key Laboratory of Combined Multi-Organ Transplantation, Ministry of Public Health, School of Medicine, Zhejiang University, Hangzhou, 310003, P.R. China.

In this study, we newly designed and synthesized a small library of ten structurally related C,N-cyclometalated ruthenium(II) complexes containing various pyridine-functionalized NHC ligand and chelating bipyridyl ligands (e.g., 2,2'-bipyridine, 5,5'-dimethyl-2,2'-bipyridine, and 1,10-phenanthroline (phen)). Read More

View Article and Full-Text PDF
November 2020

Exploring the In Vivo and In Vitro Anticancer Activity of Rhenium Isonitrile Complexes.

Inorg Chem 2020 Jul 7;59(14):10285-10303. Epub 2020 Jul 7.

Department of Chemistry and Chemical Biology, Cornell University, Ithaca, New York 14853, United States.

The established platinum-based drugs form covalent DNA adducts to elicit their cytotoxic response. Although they are widely employed, these agents cause toxic side-effects and are susceptible to cancer-resistance mechanisms. To overcome these limitations, alternative metal complexes containing the rhenium(I) tricarbonyl core have been explored as anticancer agents. Read More

View Article and Full-Text PDF

The Novel Zinc Finger Protein 587B Gene, ZNF587B, Regulates Cell Proliferation and Metastasis in Ovarian Cancer Cells in vivo and in vitro.

Cancer Manag Res 2020 26;12:5119-5130. Epub 2020 Jun 26.

Department of Clinical Pharmacology, Xiangya Hospital, Central South University, Changsha 410008, People's Republic of China.

Background: The zinc finger protein 587B () is a novel cisplatin-sensitive gene that was identified in our previous research by using a genome-scale CRISPR-Cas9 knockout library in ovarian cancer (OC) cell lines. belongs to the C2H2-type zinc finger protein (ZFP) family. Many ZFP protein could inhibit tumor development and malignancy. Read More

View Article and Full-Text PDF

SPTBN1 suppresses the progression of epithelial ovarian cancer via SOCS3-mediated blockade of the JAK/STAT3 signaling pathway.

Aging (Albany NY) 2020 06 8;12(11):10896-10911. Epub 2020 Jun 8.

Department of Gynecology, Obstetrics and Gynecology Hospital, Fudan University, Shanghai 200011, China.

SPTBN1 plays an anticancer role in many kinds of tumors and participates in the chemotherapeutic resistance of epithelial ovarian cancer (EOC). Here, we reported that lower SPTBN1 expression was significantly related to advanced EOC stage and shorter progression-free survival. SPTBN1 expression was also higher in less invasive EOC cell lines. Read More

View Article and Full-Text PDF

Sulforaphane enhances the cisplatin sensitivity through regulating DNA repair and accumulation of intracellular cisplatin in ovarian cancer cells.

Exp Cell Res 2020 08 11;393(2):112061. Epub 2020 May 11.

Department of Clinical Epidemiology, Shengjing Hospital of China Medical University, Shenyang, China. Electronic address:

Objectives: Cisplatin is commonly applied as anticancer agent for various cancers, including ovarian cancer. Unfortunately, the drug resistance frequently occurred which obstructing the effect of cisplatin on tumors. The goal of our research was to investigate the reversal actions and the potential mechanisms of sulforaphane (SFN) on cisplatin resistance in ovarian carcinoma. Read More

View Article and Full-Text PDF

Discovery of novel heat shock protein (Hsp90) inhibitors based on luminespib with potent antitumor activity.

Bioorg Med Chem Lett 2020 06 2;30(12):127165. Epub 2020 Apr 2.

Laboratory of Medicinal Chemistry, College of Pharmacy, Seoul National University, Seoul 08826, South Korea. Electronic address:

A series of isosteric surrogates of the 4-phenyl group in luminespib were investigated as new scaffolds of the Hsp90 inhibitor for the discovery of novel antitumor agents. Among the synthesized surrogates of isoxazole and pyrazole, compounds 4a, 5e and 12b exhibited potent Hsp90 inhibition in ATPase activity and Her2 degradation assays and significant antitumor activity in A2780 and HCT116 cell lines. Animal studies indicated that compared to luminespib, their activities were superior in A2780 or NCI-H1975 tumor xenograft models. Read More

View Article and Full-Text PDF