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Anti-cancer Drugs

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https://www.readbyqxmd.com/read/30204596/preclinical-testing-of-5-amino-1-1r-2s-3s-4r-2-3-dihydroxy-4-methylcyclopentyl-1h-imidazole-4-carboxamide-a-potent-protein-kinase-c-%C3%AE-inhibitor-as-a-potential-prostate-carcinoma-therapeutic
#1
André H Apostolatos, Christopher A Apostolatos, Wishrawana S Ratnayake, Anthony Neuger, Samer Sansil, Marie Bourgeois, Mildred Acevedo-Duncan
Protein kinase C-iota (PKC-ι) is an oncogene overexpressed in many cancer cells including prostate, breast, ovarian, melanoma, and glioma. Previous in-vitro studies have shown that 5-amino-1-((1R,2S,3S,4R)-2,3-dihydroxy-4-methylcyclopentyl)-1H-imidazole-4-carboxamide (ICA-1s), a PKC-ι specific inhibitor, is effective against some cancer cell lines by decreasing cell growth and inducing apoptosis. To assess ICA-1s as a possible therapeutic, in-vivo studies using a murine model were performed. ICA-1s was tested for stability in blood serum and results demonstrated that ICA-1s was stable in human plasma at 25 and 37°C over a course of 2 h...
September 10, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/30198914/effects-of-9-cis-retinoic-acid-on-the-proliferation-and-apoptosis-of-cutaneous-t-cell-lymphoma-cells
#2
Hua Yang, Yue Tao, Mengli Zhang, Pengcheng Ma, Lingjun Li, Qingchun Diao
The vitamin A derivative 9-cis-retinoic acid (9-cis-RA) has been used for the treatment and prevention of cutaneous T-cell lymphoma (CTCL). However, the precise mechanism by which 9-cis-RA treatment ameliorates CTCL remains elusive. Our research shows that 9-cis-RA inhibits proliferation and induces apoptosis in CTCL cells in a dose-dependent and time-dependent manner. 9-Cis-RA also induced G0/G1 cell cycle arrest by downregulation of cyclin D1. We confirmed that 9-cis-RA significantly decreased phosphorylation of JAK1, STAT3, and STAT5 and downregulated Bcl-xL and cyclin D1, indicating that 9-cis-RA inhibited the activation of JAK/STAT signaling...
September 6, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/30169424/bacillomycin-d-c16-triggers-apoptosis-of-gastric-cancer-cells-through-the-pi3k-akt-and-foxo3a-signaling-pathways
#3
Fuxing Lin, Jie Yang, Umair Muhammad, Jing Sun, Zhenghua Huang, Wei Li, Fengxia Lv, Zhaoxin Lu
Bacillomycin D can inhibit the growth of Aspergillus ochraceus in food samples. In addition, it can induce apoptosis in and inhibit the proliferation of cancer cells, although the details of this mechanism are unknown. In this study, we separated bacillomycin D-C14, D-C15, D-C16 monomers from the Bacillus subtilis strain fmbJ. The bacillomycin D monomers containing longer fatty acid chains better induced apoptosis in Bgc-823, Sgc-7901, and Hgc-27 gastric cancer cells. The Bgc-823 cell line was the most sensitive...
August 30, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/30134286/cetirizine-and-thalidomide-synergistically-inhibit-mammary-tumorigenesis-and-angiogenesis-in-7-12-dimethylbenz-a-anthracene-treated-rats
#4
Ilya D Ionov, Nicholas P Gorev, Larissa A Roslavtseva, David D Frenkel
OBJECTIVE: Cetirizine (CET) and thalidomide (THA) have been previously found to influence angiogenesis. The present study aimed to assess the ability of these drugs to influence mammary carcinogenesis in rats. MATERIALS AND METHODS: Sixty Sprague-Dawley female rats, aged 8 weeks, received 15 mg of 7,12-dimethylbenz(a)anthracene (DMBA) intragastrically. CET and THA (1.0 and 3.0 mg/kg, respectively) were administered orally for 118 days after DMBA administration...
August 21, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/30134285/efficacy-and-safety-of-raltitrexed-based-transarterial-chemoembolization-for-colorectal-cancer-liver-metastases
#5
Guoliang Shao, Ruibao Liu, Wenbin Ding, Ligong Lu, Wentao Li, Huicun Cao, Rong Liu, Caixia Li, Hua Xiang, Zhengqiang Yang, Jijin Yang, Jinlong Song, Jianhua Wang
The liver is the most common site of colorectal cancer metastases. The present study aimed to evaluate the efficacy and safety of transarterial chemoembolization (TACE) with raltitrexed and oxaliplatin for colorectal liver metastases in a prospective, multicenter, single-arm trial conducted in 12 hospitals from different areas in China. A total of 90 patients with colorectal liver metastases were enrolled and treated by TACE with raltitrexed 4 mg and oxaliplatin 100 mg, followed by embolotherapy with 50 mg oxaliplatin and 5-20 ml lipiodol, administered every 28 days for four cycles...
August 21, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/30134284/increased-mir-203-3p-and-reduced-mir-21-5p-synergistically-inhibit-proliferation-migration-and-invasion-in-esophageal-cancer-cells
#6
Yang Xia, Yihui Wang, Qi Wang, Maliha Ghaffar, Yuting Wang, Wang Sheng, Fang Zhang
Dysregulation of miR-203-3p and miR-21-5p has been identified in esophageal cancer (EC). The restoration of miR-203-3p and reduction of miR-21-5p were able to cause tumor suppression. Here, co-transfection of miR-203-3p mimics and miR-21-5p inhibitors led to an extraordinary increased expression of miR-203-3p and synergistically inhibited proliferation, migration, and invasion in EC cells. Moreover, we found that Ran GTPase (Ran) was dramatically inhibited in EC cells treated with the co-transfection of miR-203-3p mimics and miR-21-5p inhibitors...
August 21, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/30130258/proapoptotic-effects-of-novel-thiazole-derivative-on-human-glioma-cells
#7
Nataliya Finiuk, Olha Klyuchivska, Iryna Ivasechko, Volodymyr Hreniukh, Yuriy Ostapiuk, Yaryna Shalai, Rostyslav Panchuk, Vasyl Matiychuk, Mykola Obushak, Rostyslav Stoika, Andriy Babsky
The aim of the present study was to investigate the antiproliferative and proapoptotic actions of N-(5-benzyl-1,3-thiazol-2-yl)-3,5-dimethyl-1-benzofuran-2-carboxamide derivative (compound 5) in glioma cells in comparison with the actions of temozolomide (TMZ) and doxorubicin (Dox), used as positive controls. The antiproliferative activity of the compound 5, TMZ, and Dox on human glioblastoma U251 and human glioblastoma multiform T98G cells was measured using the MTT test. Western blot analysis, fluorescent microscopy, agarose gel retardation assay, flow cytometric analysis, and the DNA comet assay under alkaline conditions were carried out to study the effect of compound 5 on U251 cells...
August 20, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/30124494/phase-ii-clinical-trial-of-second-line-weekly-paclitaxel-plus-trastuzumab-for-patients-with-her2-positive-metastatic-gastric-cancer
#8
Yosuke Horita, Michiko Nishino, Saiho Sugimoto, Akihiko Kida, Atsuyoshi Mizukami, Masaaki Yano, Fumitaka Arihara, Koichiro Matsuda, Mitsuru Matsuda, Akito Sakai
BACKGROUND: Combination therapy with fluorouracil, platinum, and trastuzumab (Tmab) is the first-line treatment for human epidermal growth factor receptor 2 (HER2)-positive gastric cancer, and there is currently no established second-line therapy. We evaluated the efficacy and safety of weekly paclitaxel plus Tmab as second-line chemotherapy for HER2-positive gastric cancer patients. PATIENTS AND METHODS: Eligible patients were older than or equal to 20 years, had histologically confirmed gastric adenocarcinoma that was HER2 positive (immunohistochemistry 3+ or immunohistochemistry 2+ and fluorescence in-situ hybridization positive or dual color in-situ hybridization positive), and had been treated previously with chemotherapy (pretreated or not with Tmab)...
August 17, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/30106753/a-novel-hedgehog-inhibitor-for-the-treatment-of-hematological-malignancies
#9
Peng Lin, Yuanming He, Guodong Chen, Haikuo Ma, Jiyue Zheng, Zubin Zhang, Biyin Cao, Hongjian Zhang, Xiaohu Zhang, Xinliang Mao
The hedgehog-smoothened (HH/SMO) pathway has been proposed as a potential therapeutic target for hematological malignancies. Our previous studies designed a series of HH inhibitors with novel scaffolds distinctive from vismodegib, the first Food and Drug Administration-approved HH inhibitor for the treatment of basal-cell carcinoma and medulloblastoma. In the present study, we evaluated these HH inhibitors against blood cancers and found that HH78 displayed potent activity in suppressing the HH signaling pathway...
August 13, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/30096129/hmir-34c-3p-upregulation-inhibits-the-proliferation-of-colon-cancer-cells-by-targeting-eif3d
#10
Wenfeng Du, Honggang Cheng, Lipan Peng, Daogui Yang, Chenggang Yang
Our study desired to investigate how miR-34c-3p regulates colon cancer cell proliferation and what is the relationship between miR-34c-3p and EIF3D. HCEpiC (normal human colonic epithelial cells), SW620, HT-29, SW480, and HCT-116 (human colon cancer cells lines) were used in our study. SW620 cells were chosen and divided into blank, miR-34c-3p mimics, miR-34c-3p NC, miR-34c-3p inhibitors, Lv-EIF3D, Lv-NC, and miR-34c-3p mimics+Lv-EIF3D groups. qRT-PCR was used for the detection of miR-34c-3p and EIF3D mRNA expressions...
August 9, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/30096128/inhibition-of-bromodomain-and-extraterminal-domain-reduces-growth-and-invasive-characteristics-of-chemoresistant-ovarian-carcinoma-cells
#11
Majid Momeny, Haniyeh Eyvani, Farinaz Barghi, Seyed H Ghaffari, Sepehr Javadikooshesh, Robab H Jamadi, Fatemeh Esmaeili, Zivar Alishahi, Azam Zaghal, Davood Bashash, Fazel S Samani, Parisa Ghaffari, Ahmad R Dehpour, Seyyed M Tavangar, Kamran Alimoghaddam, Ardeshir Ghavamzadeh
Epithelial ovarian cancer (EOC) is the most lethal gynecological malignancy worldwide. Development of chemoresistance and peritoneal dissemination are the major reasons for low survival rate in the patients. The bromodomain and extraterminal domain (BET) proteins are known as epigenetic 'readers,' and their inhibitors are novel epigenetic strategies for cancer treatment. Accumulating body of evidence indicates that epigenetic modifications have critical roles in development of EOC, and overexpression of the BET family is a key step in the induction of important oncogenes...
August 9, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/30095443/osteoblastic-bone-response-mimicking-bone-progression-during-treatment-with-pembrolizumab-in-advanced-cutaneous-melanoma
#12
Francesca Comito, Valentina Ambrosini, Francesca Sperandi, Barbara Melotti, Andrea Ardizzoni
Pembrolizumab is an immune checkpoint inhibitor approved for the treatment of patients with unresectable or metastatic melanoma. Appearance of bone metastases, either osteolytic or osteoblastic, during treatment qualifies as disease progression. We report the case of a 64-year-old White woman with a metastatic melanoma undergoing second-line treatment with pembrolizumab. At first evaluation, after 3 months of therapy, computed tomography scans showed the onset of osteosclerotic lesions and a significant reduction in all the previously identified metastases; on the contrary, a fluorine-18-fluorodeoxyglucose PET showed the normalization of fluorine-18-fluorodeoxyglucose uptake in all the baseline lesions, including bone metastases...
August 7, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/30080692/vx-680-induces-p53-mediated-apoptosis-in-human-cholangiocarcinoma-cells
#13
Juan Liu, Cheng-Yong Qin
VX-680 is one selective small-molecule inhibitor of the Aurora kinases. It has been shown to disrupt motosis and induce apoptosis in a wide variety of tumor cell lines. However, its effect on human cholangiocarcinoma (CCA) cells remains uncharacterized. In the current study, we observed the effects of VX-680 on the human CCA (QBC939 and HCCC-9810) cell line. In cell culture, VX-680 inhibited proliferation and induced apoptosis of tumor cell growth in a dose-dependent and time-dependent manner, and exerted the most effective cytotoxicity against HCCC-9810 cells...
August 3, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/30074936/apatinib-reverses-alectinib-resistance-by-targeting-vascular-endothelial-growth-factor-receptor-2-and-attenuating-the-oncogenic-signaling-pathway-in-echinoderm-microtubule-associated-protein-like-4-anaplastic-lymphoma-kinase-fusion-gene-positive-lung-cancer
#14
Yanqiong Chen, Guoliang Ma, Cuiyun Su, Pihua Wu, Huilin Wang, Xiangqun Song, QiTao Yu, Aiping Zeng, Shaozhang Zhou
Overexpression of insulin growth factor 1 receptor (IGF-1R) and its ligand, insulin growth factor 1 (IGF-1), is related to treatment resistance and worse prognosis in many types of tumors. We reported recently that IGF-1R activation by IGF induces resistance to alectinib and stimulates the production of vascular endothelial growth factor, which indicates that IGF induces alectinib resistance and angiogenesis. This study aimed to determine the effect of bigeminal inhibition of anaplastic lymphoma kinase (ALK) and angiogenesis on human insulin growth factor 1 receptor (hIGF-1)-triggered drug resistance in echinoderm microtubule-associated protein-like 4-anaplastic lymphoma kinase (EML4-ALK)-positive lung cancer...
August 2, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/30074503/improved-outcomes-with-pembrolizumab-treatment-in-two-cases-of-double-cancer-including-non-small-cell-lung-cancer
#15
Hideyasu Yamada, Norihito Hida, Hiroaki Satoh, Tetsuya Yamagishi, Yoshinori Hiroshima, Shinichi Yoshii, Takefumi Saito, Nobuyuki Hizawa
Lung cancer is a major health concern worldwide, but new immunotherapeutic treatments for lung cancer have shown great promise and the prognosis for many severe cancers including lung cancer has been improving. In May 2017, the Food and Drug Administration approved pembrolizumab, a therapeutic antibody that blocks lymphocytic programmed death-1 (PD-1), as a first-line treatment for any solid tumor with specific genetic features. Pembrolizumab is a therapeutic antibody that blocks lymphocytic PD-1, the ligand of which (PD-L1) is expressed on tumor cells and which can prevent the immune system from recognizing and destroying tumors...
August 1, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/30063472/the-potential-of-hypericin-and-hyperforin-for-antiadhesion-therapy-to-prevent-metastasis-of-parental-and-oxaliplatin-resistant-human-adenocarcinoma-cells-ht-29
#16
Martina Šemeláková, Veronika Sačková, Peter Fedoročko
Cancer cells disseminate to other parts of the body during metastasis through the process of intravasation. The hypericin and hyperforin effect has been described to understand the signal mechanisms that stimulate or stunt cancer cell sprouting to metastasis on colon adenocarcinoma cells HT-29 and its resistant form HT-29-OxR. We focused on the key points of adhesion proteins (cadherin, integrin, selectin and syndecan) and also proteins participating in or contributing to the process of cancer cell migration and adhesion through genes expression and proteins levels...
July 30, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/29994802/the-anticancer-effects-of-pharmacological-inhibition-of-autophagy-in-acute-erythroid-leukemia-cells
#17
Alireza Kazemi, Mohammadreza Sadri, Mohammad Houshmand, Narjes Yazdi, Mahin Nikougoftar Zarif, Ali Anjam-Najmedini, Rezvan Tavakoli, Mohammad Ojaghi, Mansoureh Ajami, Monireh Ajami, Amir Atashi
Although recent studies have reported different aspects of autophagy, from pro-survival to pro-death roles of this process in malignant cells, the underlying mechanisms by which autophagy inhibitors contribute toward the induction of programmed cell death in cancerous cells are still unclear. In the present study, we have attempted to explore some of the molecular features of pharmacological inhibition of autophagy in TF-1 cells (an acute erythroid leukemia model). Our findings indicated that ara-C induces autophagy (with alteration of LC3B, p62, and Beclin-1) in the cells; however, targeting autophagy by 3-methyladenine and chloroquine significantly increased caspase-dependent apoptosis and the sub-G1 compartment in ara-C-treated cells...
July 9, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/30157040/rita-induces-apoptosis-in-p53-null-k562-leukemia-cells-by-inhibiting-stat5-akt-and-nf-%C3%AE%C2%BAb-signaling-pathways
#18
Rashideh N Mobaraki, Maryam Karimi, Fatemeh Alikarami, Elham Farhadi, Ali Amini, Davood Bashash, Mostafa Paridar, Parviz Kokhaei, Mohammad R Rezvani, Ahmad Kazemi, Majid Safa
Targeting oncogenic signaling pathways by small molecules has emerged as a potential treatment strategy for cancer. reactivation of p53 and induction of tumor cell apoptosis (RITA) is a promising anticancer small molecule that reactivates p53 and induces exclusive apoptosis in tumor cells. Less well appreciated was the possible effect of small molecule RITA on p53-null leukemia cells. In this study, we demonstrated that RITA has potent antileukemic properties against p53-null chronic myeloid leukemia (CML)-derived K562 cells...
October 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/30119131/plumbagin-inhibits-the-proliferation-of-nasopharyngeal-carcinoma-6-10b-cells-by-upregulation-of-reactive-oxygen-species
#19
Baisen Li, Xiuhui Gu, Mingbo Wu, Ye Zhao, Jie Yang, Li Feng, Junjie Gou, Linyi Chen, Ting Li, Linpeng Li, Lan Wang, Li Zhu, Kun Zhang
Plumbagin (PLB) is the primary component of the traditional Chinese medicine Baihua Dan, and possesses anti-infection and anticancer effects, with the ability to enhance the sensitivity of tumor cells to radiation therapy. However, the anticancer effect of PLB on nasopharyngeal carcinoma and the underlying mechanisms remain unclear. In this study, we investigated the anticancer effects of PLB on nasopharyngeal carcinoma 6-10B cells and clarified its molecular mechanisms in vitro. The results showed that PLB was effective against 6-10B cells proliferation in a dose-dependent manner by inducing G2/M phase cell cycle arrest...
October 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/30096127/imatinib-induced-drug-reaction-with-eosinophilia-and-systemic-symptoms-in-solid-tumors-a-patient-with-dermatofibrosarcoma-protuberans-and-successful-desensitization-management
#20
Eytan Ben-Ami, Maria C Castells, Nathan T Connell, Anna E Rutherford, Katherine A Thornton
Drug reaction with eosinophilia and systemic symptoms (DRESS) is a severe, potentially life-threatening drug-induced hypersensitivity reaction, characterized by cutaneous eruptions, fever, diffuse lymphadenopathy, along with hypereosinophilia, and elevated liver function tests, which in severe cases may lead to fulminant hepatic failure and death. Although DRESS syndrome has been associated with over 50 different drugs including imatinib, it has never been reported in association with imatinib treatment in solid tumors...
October 2018: Anti-cancer Drugs
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