Qiong Tang, Huiting Wen, Haoyue Hu, Xiaoli Chen, Shuxiu Xu, Li Fan, Longyang Liu, Jing Li
{"title":"Circ_0070203 Promotes Epithelial-mesenchymal Transition in Ovarian Serous Cystadenocarcinoma through miR-370-3p/TGFβR2 Axis","authors":"Qiong Tang, Huiting Wen, Haoyue Hu, Xiaoli Chen, Shuxiu Xu, Li Fan, Longyang Liu, Jing Li","doi":"10.2174/1574892818666230328124804","DOIUrl":"https://doi.org/10.2174/1574892818666230328124804","url":null,"abstract":"Introduction: Circular RNAs (circRNAs) are important biological molecules associated with the pathogenesis of multiple cancers. Objective: This work aimed to investigate the function and molecular mechanism of circ_0070203 in high-grade serous ovarian cystadenocarcinoma (HGSOC). Methods: circRNA microarray was conducted to detect the circ_0070203 expression in HGSOC tissues. Bioinformatics analysis was used to find the binding sites between circ_0070203, miR- 370-3p and TGFβR2. Real-time quantitative reverse transcription PCR (RT-qPCR) was executed to detect the expressions of circ_0070203, miR-370-3p and TGFβR2 in HGSOC tissues and SKOV3 cells. Dual-luciferase reporter gene assay was used to validate the relationships between miR-370-3p and circ_0070203 or TGFβR2. Besides, transwell assays were conducted to assess the migrative, invasive abilities of ovarian cancer (OC) cells. Western blotting was adopted to detect the expression of epithelial-mesenchymal transition (EMT)-related proteins. The related patents were also studied during the research. Results: Circ_0070203 and TGFβR2 were upregulated, while miR-370-3p was downregulated in FIGO stage Ⅲ-Ⅳ HGSOC tissues and SKOV-3 cell lines. circ_0070203 overexpression changed the expression of other EMT-related proteins and enhanced the migrative, invasive abilities of OC cells, while silencing circ_0070203 worked oppositely. Mechanistically, circ_0070203 could upregulate TGFβR2 expression in OC cells via sponging miR-370-3p. Conclusion: Circ_0070203 could promote the epithelial-mesenchymal transition, invasion, and metastasis of HGSOC via regulating the miR-370-3p/TGFβR2 axis. Our findings provided a potential biomarker for HGSOC therapy.","PeriodicalId":20774,"journal":{"name":"Recent patents on anti-cancer drug discovery","volume":"28 2","pages":""},"PeriodicalIF":2.8,"publicationDate":"2023-04-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138525243","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Ivan Pereira Lopes, Bianca Souza Bagatela, Andrey Pereira Lopes, Elaine Ferreira Silveira, Giuliana Petri, José Francisco Ramos Santos, Matheus Moreira Perez, Glaucia Luciano da Veiga, Beatriz da Costa Aguiar Alves, Fábio Ferreira Perazzo, David Feder, Fernando Luiz Affonso Fonseca
{"title":"Preclinical Effects Of Melatonin On The Development Of Ehrlich's Tumor: A Biochemical, Cognitive, And Molecular Approach.","authors":"Ivan Pereira Lopes, Bianca Souza Bagatela, Andrey Pereira Lopes, Elaine Ferreira Silveira, Giuliana Petri, José Francisco Ramos Santos, Matheus Moreira Perez, Glaucia Luciano da Veiga, Beatriz da Costa Aguiar Alves, Fábio Ferreira Perazzo, David Feder, Fernando Luiz Affonso Fonseca","doi":"10.2174/1574892818666230223160858","DOIUrl":"10.2174/1574892818666230223160858","url":null,"abstract":"<p><strong>Background: </strong>It has already been shown that melatonin is an antitumoral molecule that affects malignant cells via some mechanisms. The benefit played by this hormone on cancer is due to its antioxidant effects.</p><p><strong>Objective: </strong>This study aimed to evaluate the preclinical effects of melatonin in mice with the Ehrlich ascites tumor.</p><p><strong>Methods: </strong>Twenty Balb/ c male mice with Ehrlich tumor were treated with different melatonin doses. Their inflammatory and oxidative stress were accessed by gene expression. Hepatotoxicity and hematological parameters were also evaluated through biochemical analyses. Animal welfare was analysed weekly from the categories guided by the NC3Rs.</p><p><strong>Results: </strong>Gene expression analyses have shown that only Tnfα and Sod1 were expressed in all groups studied. Only the M-3 group showed increased Tnfα expression compared to the control. All groups treated with melatonin showed decreased Sod1 expression compared to the control. No signs of hepatotoxicity were caused by any of the melatonin doses used in the treatment.</p><p><strong>Conclusion: </strong>In animals with Ehrlich´s tumor treated with melatonin, a decrease in oxidative stress, an amelioration in welfare and in cognitive tasks could be observed, even if the treatment has not reduced the size of the tumor itself. In parallel with the already patented use of melatonin in the treatment of sleep disorders or chronic kidney disease, our results propose its use to improve the general well-being of breast cancer patients.</p>","PeriodicalId":20774,"journal":{"name":"Recent patents on anti-cancer drug discovery","volume":" ","pages":""},"PeriodicalIF":2.8,"publicationDate":"2023-02-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10775223","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Patent Selections","authors":"","doi":"10.2174/157489281801221017111423","DOIUrl":"https://doi.org/10.2174/157489281801221017111423","url":null,"abstract":"","PeriodicalId":20774,"journal":{"name":"Recent patents on anti-cancer drug discovery","volume":"23 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136062380","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Meet the Editorial Board Member","authors":"Xi Ming Yuan","doi":"10.2174/157489281801221017095113","DOIUrl":"https://doi.org/10.2174/157489281801221017095113","url":null,"abstract":"","PeriodicalId":20774,"journal":{"name":"Recent patents on anti-cancer drug discovery","volume":"1 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136062379","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Soghra Farzipour, Z. Shaghaghi, A. Salari, Fatemeh Jalali, M. Alvandi, Nasim Zarei polgardani
{"title":"Targeting ferroptosis as a new approach for radiation protection and mitigation","authors":"Soghra Farzipour, Z. Shaghaghi, A. Salari, Fatemeh Jalali, M. Alvandi, Nasim Zarei polgardani","doi":"10.2174/1574892818666230119153247","DOIUrl":"https://doi.org/10.2174/1574892818666230119153247","url":null,"abstract":"\u0000\u0000Radiation-induced normal cell toxicity (RINCT) is a major factor to consider while treating any ailment with radiotherapy. Clinical irradiation of tumors necessitates an understanding of the potential efficacy of radiation protective agents in reducing radiation damage to healthy tissues and their effects on tumor tissue radiosensitivity. Ferroptosis is a relatively new form of iron-dependent cell death that has been linked to a variety of disease pathologies. The key mediators of ferroptosis have been identified as lipid peroxidation and iron metabolism. Lipid peroxidation is the result of a reaction between reactive oxygen (ROS) and reactive nitrogen species (RNS) with phosphatidylethanolamine-containing polyunsaturated fatty acids (PUFAs). Ferroptosis inhibitors have been demonstrated to have anti-inflammatory effects in animal models of disease. It was recently shown that ionizing radiation (IR) generates severe ferroptosis, a critical component of RT-mediated normal cell toxicity. These findings support the use of ferroptosis inhibitor treatments for the treatment of radiation normal cell toxicity. Targeting lipid metabolic substrates and controlling ferroptosis by radiation could reduce toxicity and improve clinical outcomes. In this study, we address the relationships between radiotherapy and various types of radiation-induced cell death, and we discuss the interactions between ferroptosis and other kinds of controlled cell death generated by radiotherapy, and we investigate combination treatment options targeting ferroptosis in radiotherapy. This review will be a foundation for future research on ferroptosis in radiotherapy. Additionally, the relevant patents on ferroptosis inhibitors with various therapeutic potentials have been discussed.\u0000","PeriodicalId":20774,"journal":{"name":"Recent patents on anti-cancer drug discovery","volume":" ","pages":""},"PeriodicalIF":2.8,"publicationDate":"2023-01-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49145502","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"The Non-Hodgkin Lymphoma Treatment and Side Effects: A Systematic Review and Meta-Analysis.","authors":"Alice Barros Câmara, Igor Augusto Brandão","doi":"10.2174/1574892818666230117151757","DOIUrl":"10.2174/1574892818666230117151757","url":null,"abstract":"<p><strong>Objective: </strong>This paper aims to review studies regarding side effects found during Non-Hodgkin Lymphoma treatment, to suggest the drug class most associated with these effects, as well as the most prevalent side effect grade.</p><p><strong>Methods: </strong>This review is registered in PROSPERO (IDCRD42022295774) and followed the PICOS strategy and PRISMA guidelines. The search was carried out in the databases PubMed/MEDLINE, Scientific Electronic Library Online, and DOAJ. Medical Subject Headings Terms were used and quantitative studies with conclusive results regarding side effects during the non-Hodgkin lymphoma treatment were selected. Patent information was obtained from google patents.</p><p><strong>Results: </strong>Monoclonal antibodies were the main drug class associated with side effects during NHL therapy. The combination of Rituximab (Rituxan®; patent EP1616572B) and iInotuzumab (Besponsa®; patent EP1504035B3) was associated with a higher incidence of thrombocytopenia (p<0.05), while the combination of Rituximab and Venetoclax (Venclexta®; patent CN107089981A) was associated with a higher incidence of neutropenia (p<0.05) when compared to Bendamustine combinations (Treanda ™; patent US20130253025A1). Meta-analysis revealed a high prevalence of grade 3-4 neutropenia and thrombocytopenia in men. Finally, Americans and Canadians experienced a higher prevalence of these side effects, when compared to others nationalities (p<0.05).</p><p><strong>Conclusion: </strong>Patents regarding the use of monoclonal antibodies in NHL treatment were published in the last year. Monoclonal antibodies associated with neutropenia (grade 3-4) and thrombocytopenia, especially in North American men treated for NHL, and with an average age of 62 years demonstrated importance in this study.</p>","PeriodicalId":20774,"journal":{"name":"Recent patents on anti-cancer drug discovery","volume":" ","pages":""},"PeriodicalIF":2.8,"publicationDate":"2023-01-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10541574","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Siah2 inhibitor and the metabolic antagonist Oxamate retard colon cancer progression and downregulate PD1 expression.","authors":"Sherin Zakaria, Samar Elsebaey, Shady Allam, Walied Abdo, Alaa El-Sisi","doi":"10.2174/1574892818666230116142606","DOIUrl":"10.2174/1574892818666230116142606","url":null,"abstract":"<p><strong>Background: </strong>Solid tumors such as colon cancer are characterized by rapid and sustained cell proliferation, which ultimately results in hypoxia, induction of hypoxia-inducible factor-1α (HIF-1α), and activation of glycolysis to promote tumor survival and immune evasion. We hypothesized that a combinatorial approach of menadione (MEN) as an indirect HIF-1α inhibitor and sodium oxamate (OX) as a glycolysis inhibitor may be a promising treatment strategy for colon cancer.</p><p><strong>Objectives: </strong>We investigated the potential efficacy of this combination for promoting an antitumor immune response and suppressing tumor growth in a rat model of colon cancer.</p><p><strong>Methods: </strong>Colon cancer was induced by once-weekly subcutaneous injection of 20 mg/kg dimethylhydrazine (DMH) for 16 weeks. Control rats received the vehicle and then no further treatment (negative control) or MEN plus OX for 4 weeks (drug control). Dimethylhydrazine-treated rats were then randomly allocated to four groups: DMH alone group and other groups treated with MEN, OX, and a combination of (MEN and OX) for 4 weeks. Serum samples were assayed for the tumor marker carbohydrate antigen (CA19.9), while expression levels of HIF-1α, caspase-3, PHD3, LDH, and PD1 were evaluated in colon tissue samples by immunoassay and qRT-PCR. Additionally, Ki-67 and Siah2 expression levels were examined by immunohistochemistry.</p><p><strong>Results: </strong>The combination of MEN plus OX demonstrated a greater inhibitory effect on the expression levels of HIF-1α, Siah2, LDH, Ki-67, and PD1, and greater enhancement of caspase-3 and PHD3 expression in colon cancer tissues than either drug alone.</p><p><strong>Conclusion: </strong>Simultaneous targeting of hypoxia and glycolysis pathways by a combination of MEN and OX could be a promising therapy for inhibiting colon cancer cell growth and promoting antitumor immunity [1].</p>","PeriodicalId":20774,"journal":{"name":"Recent patents on anti-cancer drug discovery","volume":" ","pages":""},"PeriodicalIF":2.8,"publicationDate":"2023-01-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10595679","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Shailendra Singh, Chandrabose Karthikeyan, N S Hari Narayana Moorthy
{"title":"Fatty Acid Synthase (FASN): A Patent Review Since 2016-Present.","authors":"Shailendra Singh, Chandrabose Karthikeyan, N S Hari Narayana Moorthy","doi":"10.2174/1574892818666230112170003","DOIUrl":"10.2174/1574892818666230112170003","url":null,"abstract":"<p><strong>Introduction: </strong>Fatty acid synthase (FASN), is a key metabolic enzyme involved in fatty acid biosynthesis and is an essential target for multiple disease progressions like cancer, obesity, NAFLD, etc. Aberrant expression of FASN is associated with deregulated energy metabolism of cells in these diseases.</p><p><strong>Area covered: </strong>This article provides a summary of the most recent developments in the discovery of novel FASN inhibitors with potential therapeutic uses in cancer, obesity, and other metabolic disorders such as nonalcoholic fatty liver disease from 2016 to the present. The recently published patent applications and forthcoming clinical data of FASN inhibitors from both academia and the pharma industries are also highlighted in this study.</p><p><strong>Expert opinion: </strong>The implication of FASN in multiple diseases has provided an impetus for developing novel inhibitors by both pharma companies and academia. Critical analysis of the patent literature reveals the exploration of diverse molecular scaffolds to identify potential FASN inhibitors that target the different catalytic domains of the enzyme. In spite of these multifaceted efforts, only one molecule, TVB-2640, has reached phase II trials for nonalcoholic steatohepatitis (NASH) and many malignancies. However, thecombined efforts of pharma companies to produce several FASN inhibitors might facilitate the clinical translation of this unique class of inhibitors. Nevertheless, concerted efforts towards developing multiple FASN inhibitors by pharma companies might facilitate the clinical translation of this novel class of inhibitors.</p>","PeriodicalId":20774,"journal":{"name":"Recent patents on anti-cancer drug discovery","volume":" ","pages":""},"PeriodicalIF":2.8,"publicationDate":"2023-01-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9095387","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
P. Kriplani, Harinder Singh, Sweta Kamboj, Kumar Guarve
{"title":"Puerarin: an Anticancer and Anti-Inflammatory Agent","authors":"P. Kriplani, Harinder Singh, Sweta Kamboj, Kumar Guarve","doi":"10.2174/1574892818666230111152024","DOIUrl":"https://doi.org/10.2174/1574892818666230111152024","url":null,"abstract":"\u0000\u0000Puerarin is a well-known anti-inflammatory agent which has demonstrated its potential to cure numerous ailments. Though many plants are reported in the literature, still their mechanisms are unversed. In this review, numerous mechanisms of puerarin to cure cancer and other inflammatory disorders, pharmacokinetics and adverse events, and boulevards of further research are discussed.\u0000\u0000\u0000\u0000Organized research was done using ScienceDirect, PubMed, ResearchGate, Google Scholar, Google Patents and ScienceDirect Medline to quest all the available data to date on puerarin. Different keywords used were “puerarin”, “Pueraria tuberosa”, “cancer”, “anti-inflammatory”, “cardiovascular”, “IBD”, “pharmacokinetics” etc.\u0000\u0000\u0000\u0000One hundred thirty-six articles and thirteen patents were studied. Puerarin is reported to treat chronic problems like inflammation, sexual dysfunction, cardiovascular diseases and menaces such as colon, stomach, lung and breast cancer by numerous mechanisms, as these ailments do not progress via a single independent pathway.\u0000\u0000\u0000\u0000Conclusion: This article will definitely help budding researchers scrutinize the wealth of information on the therapeutic chattels of puerarin and identify the gaps that have forbidden its application as a potential molecule to cure various ailments.\u0000","PeriodicalId":20774,"journal":{"name":"Recent patents on anti-cancer drug discovery","volume":" ","pages":""},"PeriodicalIF":2.8,"publicationDate":"2023-01-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48306202","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Advances in the Treatment of Chronic Myeloid Leukemia","authors":"R. Mihăilă","doi":"10.2174/1574892818666230111115040","DOIUrl":"https://doi.org/10.2174/1574892818666230111115040","url":null,"abstract":"\u0000\u0000The treatment of chronic myeloid leukemia has progressed in recent decades, becoming a model for a disease whose pathogenesis is primarily based on a genetic mutation and has led to survivals comparable to those of the general population.\u0000\u0000\u0000\u0000This review aims to present recent therapeutic advances in this area.\u0000\u0000\u0000\u0000A mini-review was achieved using the articles published in Web of Science and PubMed between January 2021 - May 2022, and new patents were made in this field.\u0000\u0000\u0000\u0000Results: The three generations of tyrosine kinase inhibitors have transformed chronic myeloid leukemia into a manageable disorder and greatly improved the treatment results of the chronic phase, the prognosis, survival, and quality of life of patients. The therapeutic goals today include achieving a deep and lasting molecular response as soon as possible, successful treatment-free remission, and discovering and applying new therapeutic strategies to act on impaired immune modulation and dormant leukemic stem cells. The allosteric inhibitor asciminib targets the ABL myristoyl pocket, reduces Abl kinase activity, and is effective against most cells that have mutations in the ABL1 kinase domain. Progress and recommendations for achieving long-term treatment-free remission are set out. Nearly 50% of the patients who received first-line tyrosine kinase inhibitors required a change of treatment by 10 years due to intolerance or resistance to treatment. Their main side effects are presented.\u0000\u0000\u0000\u0000Obtaining a deep and persistent molecular response contributes to achieving long-term treatment-free remission.\u0000","PeriodicalId":20774,"journal":{"name":"Recent patents on anti-cancer drug discovery","volume":" ","pages":""},"PeriodicalIF":2.8,"publicationDate":"2023-01-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42533467","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}