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Recent Patents on Anti-cancer Drug Discovery

Maricruz Anaya-Ruiz, Cindy Bandala, Gerardo Landeta, Patricia Martínez-Morales, Jose Lino Zumaquero-Rios, Jorge Sarracent-Pérez, Martin Perez-Santos
BACKGROUND: Cancer is one of the leading causes of death in the world and it is necessary to develop new strategies for its treatment because most therapies have limited access to many types of tumors, as well as low therapeutic efficacy and high toxicity. OBJECTIVE: The present review aims to provide to identify recent patents of drug delivery nanostructured systems that may have application in improving cancer treatment. METHOD: Recent patents regarding the drug delivery nanostructured systems for cancer treatment were obtained from the patent databases of the six main patent offices of the world: United States Patent and Trademark Office, European Patent Office, World Intellectual Property Organization, Japan Patent Office, State Intellectual Property Office of China and Korean Intellectual Property Office...
October 31, 2018: Recent Patents on Anti-cancer Drug Discovery
Spandana Rajendra Kopalli, Tae-Bong Kang, Kwang-Ho Lee, Sushruta Koppula
BACKGROUND: In the last few decades, cancer immunotherapy has been extensively researched, and novel checkpoint signaling mechanisms involving programmed death (PD)-1 and PD-ligand 1 (PD-L1) receptors have been targeted. The PD-1/PD-L1 binding and interaction play a critical role in the development of malignancies. OBJECTIVE: The present review focuses on recent patents on the pharmacological and biological cancer-regulating properties of PD-1/PD-L1 inhibitors involved in immunotherapeutic cancer drug development...
October 29, 2018: Recent Patents on Anti-cancer Drug Discovery
Weidong Li, Xueying Sun
BACKGROUND: Solid tumors often contain hypoxic microenvironments due to abnormal vasculatures and outweighing demands of oxygen. Cancer cells rely on anaerobic respiration, leading to sequential acidic microenvironments. Hypoxic and acidic microenvironments cause genetic instability and activate signaling pathways, contributing to cancer progression and drug therapy resistance, and have become targets for developing novel anti-cancer agents. OBJECTIVE: This article reviews recent advances in the development of novel anti-cancer drugs targeting hypoxic and acidic microenvironments...
August 30, 2018: Recent Patents on Anti-cancer Drug Discovery
Hidayat Hussain, Rene Csuk, Ivan R Green, Najeeb Ur Rehman, Ghulam Abbas, Wahid Hussain
Withanolides are C-28 ergostane steroids known to demonstrate some very interesting therapeutic properties. Numerous withanolides have been isolated from a variety of different plant species and can be employed to treat various types of cancers. Withanolides are indeed capable of demonstrating excellent anticancer, anti-inflammatory, and neuroprotective activities. Additionally, libraries of prepared withaferin A analogs incorporating an acyl, sulphate, amide and aldehyde functionality have demonstrated the most potential response potentials...
August 8, 2018: Recent Patents on Anti-cancer Drug Discovery
A E Shchekotikhin, Georgy Y Nadysev, Alexander S Tikhomirov, Lyubov G Dezhenkova
BACKGROUND: Heliomycin (resistomycin), an antibiotic with broad spectra of biological activities including antimicrobial, antifungal, antiviral, and antiproliferative. However, an extremely low solubility in aqueous media and in the majority of organic solvents limits its practical application. OBJECTIVE: Due to a high practical potential of heliomycin new routes of structural modification are strongly required to improve its solubility. CONCLUSION: The patent claims a series of 4-aminomethyl derivatives of heliomycin as well as a pharmaceutical composition based on it...
July 23, 2018: Recent Patents on Anti-cancer Drug Discovery
Zsuzsanna Suba
BACKGROUND: The pharmaceutical development of endocrine disruptors could not achieve appropriate advances in the field of anticancer fight. OBJECTIVE: Considerations on the principles of currently used endocrine therapies. METHODS: Comparison of the results of genetic studies being performed on breast cancer cells treated with estrogens, synthetic estrogens and antiestrogens. RESULTS: In breast cancer cells, increased estrogen concentrations amplify ER-signaling via a synergistic upregulation of both liganded and unliganded ER-activations and increased aromatase expression...
July 20, 2018: Recent Patents on Anti-cancer Drug Discovery
Sara Petrillo, Emanuela Tolosano, Luca Munaron, Tullio Genova
Massive vessel recruitment is required to sustain rapid tumor growth by delivering oxygen and nutrients. Current strategies to counteract angiogenesis are mostly aimed at reducing tumor vessel density. However, many of these drugs have been shown to trigger hypoxia, thus exacerbating tumor aggressiveness. Promising results come from a completely different approach based on the "normalization" of the endothelial layer and the consequent improvement of the vascular function. Since endothelial metabolism has proved essential in the regulation of the angiogenic switch, many recent patents focus on agents able to inhibit specific metabolic pathways in tumor-associated endothelial cells (TECs) in order to provide vessel normalization...
May 27, 2018: Recent Patents on Anti-cancer Drug Discovery
Lanhong Zheng, Yixin Xu, Xiukun Lin, Zhixin Yuan, Minghua Liu, Shousong Cao, Fuming Zhang, Robert J Linhardt
BACKGROUND: Marine environment constitutes an almost infinite resource for novel anticancer drugs discovery. The biodiversity of marine organisms provides a rich source for the discovery and development of novel anticancer peptides in the treatment of human cancer. Marine peptides represent a new opportunity to obtain lead compounds in biomedical field, particularly for cancer therapy. OBJECTIVE: Providing an insight of the recent progress of patented marine peptides and presenting information about the structures and mechanistic mode of anticancer activities of these marine peptides...
April 29, 2018: Recent Patents on Anti-cancer Drug Discovery
Gloria Mittica, Eleonora Ghisoni, Gaia Giannone, Sofia Genta, Massimo Aglietta, Anna Sapino, Giorgio Valabrega
BACKGROUND: Treatment of Epithelial Ovarian Cancer (EOC), historically based on surgery and platinum doublet chemotherapy, is associated with high risk of relapse and poor prognosis for recurrent disease. In this landscape, the innovative treatment with PARP inhibitors (PARPis) demonstrated an outstanding activity in EOC, and is currently changing clinical practice in BRCA mutant patients. OBJECTIVES: To highlight the mechanism of action, pharmacokinetics, clinical activity, indications and current strategies of development of Olaparib, Niraparib, Rucaparib, Talazoparib and Veliparib, the 5 most relevant PARPis...
March 5, 2018: Recent Patents on Anti-cancer Drug Discovery
Shuonan Su, Huanli Xu, Xiaoliang Chen, Gan Qiao, Ammad A Farooqi, Ye Tian, Ru Yuan, Xiaohui Liu, Cong Li, Xiao Li, Ning Wu, Xiukun Lin
BACKGROUND: CS5931, a novel marine peptide, was extracted and purified from the sea squirt Ciona savignyi. Our previous studies showed that recombinant CS5931 can significantly inhibit tumor growth both in vitro and in vivo. However, its molecular targets have not been elucidated. METHODS: The target of the recombinant CS5931 was identified by pull-down/SDS-PAGE/MS approaches and confirmed by Western blot and surface plasmon resonance analysis. Transwell experiments were used to detect whether the recombinant CS5931 inhibited cancer migration and invasion via enolase 1...
2018: Recent Patents on Anti-cancer Drug Discovery
Zeynab Khansefid, Asghar Davood, Maryam Iman, Mahdi Fasihi
BACKGROUND: Hydroxyurea (HU) is used to treat cancer. HU has a short half-life due to its small molecular weight and high polarity, therefore a high dosage of the drug should be used which introduces side effects and more rapid development of resistance. OBJECTIVE: The objective of the current study is to design new lipophilic analogues of hydroxyurea with higher stability and better cell penetration. The designed compounds were synthesized and then evaluated in terms of their cytostatic activities against two human cell lines...
2018: Recent Patents on Anti-cancer Drug Discovery
Kamel Laribi, Mustapha Alani, Catherine Truong, Alix Baugier de Materre
OBJECTIVE: Mature T-cell lymphomas are a heterogeneous group of T-cell malignancies with a poor outcome. The discovery of new molecular biomarkers has led to the emergence of new drugs in recent years that target various signaling pathways. METHODS: We examined all pertinent published patents through 2015 that analyzed novel methods for the diagnosis and treatment of T cell lymphoma, as well as related published and unpublished studies. Selection criteria were established before data collection...
2018: Recent Patents on Anti-cancer Drug Discovery
Maricruz Anaya-Ruiz, Cindy Bandala, Patricia Martinez-Morales, Gerardo Landeta, Rebeca D Martinez-Contreras, Nancy Martinez-Montiel, Martin Perez-Santos
BACKGROUND: Despite dramatic advances in cancer treatment that lead to long-term survival, there is an increasing number of patients presenting with clinical manifestations of cerebral metastasis in breast cancer, for whom only palliative treatment options exist. OBJECTIVE: The present review based on researches aims to provide identification of recent patens of breast cancer brain metastasis that may have application in improving cancer treatment. METHODS: Recent patents regarding the breast cancer brain metastasis were obtained from USPTO patent databases, Esp@cenet, Patentscope and Patent Inspiration®...
2018: Recent Patents on Anti-cancer Drug Discovery
Huanhuan Ren, Jun Ma, Lingling Si, Boxue Ren, Xiaoyu Chen, Dan Wang, Wenjin Hao, Xuexi Tang, Defang Li, Qiusheng Zheng
BACKGROUND: Phytoestrogens have been proposed as replaceable medicines for climacteric hormone replacement therapy, on the basis of EP3138562 and US5516528. However, recent studies demonstrated that phytoestrogens might promote the proliferation of breast cancer cells, which is rooted in their estrogenic activity. Acacetin, as one phytoestrogen, has been reported to exhibit estrogenic activity. But the effect of acacetin on breast cancer cells proliferation and its mechanism has not been explored...
2018: Recent Patents on Anti-cancer Drug Discovery
Xiaofen Ni, Jiajun Chen, Fengying Lu, Zhengzhong Yuan, Xiaofeng Xu, Zhen Hu, Lei Jiang
BACKGROUND: α-Solanine, the most important and active component of Solanum nigrum, was found to have anti-cancer activity on multiple cancer cells. However, its effects on colorectal cancer (CRC) and associated molecular mechanisms remain to be further elucidated. OBJECTIVE: In this study, we investigated the anti-cancer effects of α-solanine against CRC cells in vitro and in vivo. MATERIALS & METHODS: Cell viability was measured using Cell Counting Kit-8 (CCK-8) assay; cell cycle was analyzed with a Cycletest Plus DNA Reagent Kit; cell apoptosis was detected by flow cytometer; cell migration and invasive ability was determined by Transwell assays; S100P protein expression was also analyzed by western blotting; lentiviral vectors expressing shRNA targeting the S100P gene...
2018: Recent Patents on Anti-cancer Drug Discovery
D S Xin, L Zhou, C Z Li, S Q Zhang, H Q Huang, G D Qiu, L F Lin, Y Q She, J T Zheng, C Chen, L Fang, Z S Chen, S Y Zhang
BACKGROUND: Paclitaxel (PTX) has remarkable anti-tumor activity, but it causes severe toxicities. There is an urgent need to seek an appropriate pharmacokinetic parameter of PTX to improve treatment efficacy and reduce adverse effects. OBJECTIVE: To evaluate the association of pharmacokinetic parameter TC > 0.05 of paclitaxel (PTX) and its therapeutic efficacy and toxicity in patients with solid tumors. METHODS: A total of 295 patients with ovarian cancer, esophageal cancer, breast cancer, and non-small cell lung cancer (NSCLC), who were admitted to the Tumor Hospital of Shantou University Medical College, China, were recruited for this study...
2018: Recent Patents on Anti-cancer Drug Discovery
Leila Farahmand, Sepideh Mansouri, Narges Jafarbeik-Iravani, Azin Teymourzadeh, Keivan Majidzadeh-A
BACKGROUND: Tamoxifen is widely administered for patients with estrogen receptor-positive breast cancer. Despite many patients benefiting from Tamoxifen as an effective anti-hormonal agent in adjuvant therapy, a noticeable number of patients tend to develop resistance. OBJECTIVE: The aim of this study was to shed light upon the molecular mechanisms associated with Tamoxifen resistance which can help improve current treatment strategies available for stimulating responsiveness and combating resistance...
2018: Recent Patents on Anti-cancer Drug Discovery
Yi Zhang, Liling Tang
BACKGROUND: It is increasingly evident that lncRNAs have various biological functions playing as essential regulators, getting involved in diverse cellular processes. Many of the lncRNAs show aberrant expression in cancer, which is associated with different cancer types. The dysregulation of lncRNAs has been increasingly linked to cancer carcinogenesis and progression. OBJECTIVE: Due to their tissue-specific expression and key role in cancer, lncRNAs have the potential to be novel biomarkers or effective drug targets for cancer...
2018: Recent Patents on Anti-cancer Drug Discovery
Mohit Sharma, Smitha S Shetty, Raghu Radhakrishnan
BACKGROUND: Oral submucous fibrosis is an oral potentially malignant disorder with high incidence of malignant transformation and rising global prevalence. However, the genesis of oral submucous fibrosis is still unclear despite superfluity of literature. In the background of ineffective treatment, it is necessary to decode its onset and progression before designing customized treatment regimens. OBJECTIVE: The objective of this article is to decipher the pathogenesis of oral submucous fibrosis in order to identify novel drug targets...
2018: Recent Patents on Anti-cancer Drug Discovery
Shirin Mollazadeh, Fatemeh Moosavi, Farzin Hadizadeh, Mahmoud Seifi, Javad Behravan, Maryam Iman
BACKGROUND: P-glycoprotein (P-gp) causes the efflux of cancer chemotherapy drugs from tumor cells, so its inhibition can be one target for designing and synthesis of new anticancer drugs. OBJECTIVE: In this study, new compounds of 1,4-dihydropyridine (DHP) were recommended as inhibitors of P-gp. METHODS: We synthesized new symmetrical DHP with 36% - 43% yield by the reaction of new reactants. In biological studies, these compounds have high lipophilicity, and thus low water solubility...
2018: Recent Patents on Anti-cancer Drug Discovery
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