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Recent Patents on Anti-cancer Drug Discovery

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https://www.readbyqxmd.com/read/29268690/reduced-lipocalin-2-expression-contributes-to-vincristine-resistance-in-human-colon-cancer-cellsance-in-human-colon-cancer-cells
#1
Xiao Guo, Qin Li, Yan-Fang Wang, Tian-Yun Wang, Si-Jia Chen, Zheng-Wei Tian
BACKGROUND: Vincristine (VCR) resistance can lead to cancer chemotherapy failure. Although changes in gene expression are responsible for drug resistance, the specific identities and roles of these genes remain unclear. OBJECTIVE: In this study, we aimed to identify differentially expressed genes and mechanisms of VCR resistance in colorectal cancer (CRC) cells. METHODS: A VCR-resistant CRC cell line (HCT-8/VCR) was established, and differentially expressed proteins between HCT-8 and HCT-8/VCR cells were screened using a human cytokine array; the results were confirmed by reverse transcription polymerase chain reaction and western blotting...
December 21, 2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/29210664/advances-in-the-discovery-of-anthraquinone-based-anticancer-agents
#2
Alexander Tikhomirov, Alexander Shtil, Andrey Shchekotikhin
BACKGROUND: The anthracene-9,10-dione (anthraquinone) derivatives represent an exceptionally valuable class in anticancer drug development. An outstanding antitumor potency of the anthracycline antibiotics attracted the attention of medicinal chemists since the discovery of these chemotypes. The prominent anthraquinone-based drugs doxorubicin, mitoxantrone as well as more recent epirubicin, idarubicin, and valrubicin are successfully used in chemotherapy of hematological malignancies and solid tumors...
December 6, 2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/29205122/parp-inhibitors-in-epithelial-ovarian-cancer
#3
Kristin N Taylor, Ramez N Eskander
Background Ovarian cancer remains the most common lethal gynecologic malignancy. The therapeutic gains with use of traditional cytotoxic chemotherapy in advanced stage disease remain limited, reflecting the need for novel therapies. Poly(ADP-ribose) polymerase (PARP) inhibitors have recently demonstrated a significant therapeutic effect in patients with recurrent, high grade serous ovarian cancer, both in the treatment of existing disease and in prolonging the disease-free interval. Objective The purpose of this article is to discuss PARP inhibitor use in patients with advanced stage ovarian cancer, and to extensively review the existing clinical literature and related patents...
December 3, 2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/29189178/targeting-mevalonate-pathway-in-cancer-treatment-repurposing-of-statins
#4
Federica Iannelli, Rita Lombardi, Maria Rita Milone, Biagio Pucci, Simona De Rienzo, Alfredo Budillon, Francesca Bruzzese
BACKGROUND: Modifications of lipid metabolism have been progressively accepted as a hallmark of tumor cells and in particular, an elevated lipogenesis has been described in various types of cancers. OBJECTIVE: Important or deregulated activity of the mevalonate pathway has been demonstrated in different tumors and a wide range of studies have suggested that tumor cells are more dependent on the unceasing availability of mevalonate pathway metabolites than their non-malignant complements...
November 29, 2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/29189177/brain-cancer-implication-to-disease-therapeutic-strategies-and-tumor-targeted-drug-delivery-approaches
#5
Viral Shah, Pratiksha Kochar
BACKGROUND: Cancer is one of the leading causes of morbidity and mortality worldwide. Brain cancer is identified as one of the most formidable forms of cancer due to several hurdles posed by the anatomy and physiology of the brain on the therapeutic strategies employed for treating brain cancer. Poor prognosis and high relapse rate further aggravate the situation leading to the high mortality rate in brain cancer. OBJECTIVE: The present review gives a brief insight on different aspects of brain cancer by elucidating its types, causative factors, associated symptoms, diagnostic techniques, treatment strategies and limitations of current treatment strategies...
November 29, 2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/29119937/use-of-human-dihydroorotate-dehydrogenase-hdhodh-inhibitors-in-autoimmune-diseases-and-new-perspectives-in-cancer-therapy
#6
Marco L Lolli, Stefano Sainas, Agnese C Pippione, Marta Giorgis, Donatella Boschi, Franco Dosio
BACKGROUND: Human dihydroorotate dehydrogenase (hDHODH, EC 1.3.5.2), a flavin-dependent mitochondrial enzyme involved in de novo pyrimidine biosynthesis, is a validated therapeutic target for the treatment of autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. However, human DHODH inhibitors have also been investigated as treatment for cancer, parasite infections (i.e. malaria) and viruses as well as in the agrochemicals industry. OBJECTIVE: An overview of current knowledge of hDHODH inhibitors and their potential uses in diseases where hDHODH is involved...
November 8, 2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/29119938/adenosine-receptor-ligands-on-cancer-therapy-a-review-of-patent-literature
#7
Carmen Diniz, Joana Beatriz Sousa, Paula Fresco, Jorge Goncalves
BACKGROUND: Adenosine is a purine, with an adenine group and a ribose sugar, formed endogenously by ATP catabolism both intracellularly and extracellularly. Among the medicinal features of adenosine and of its receptors (A1, A2A, A2B and A3), anticancer activity has been an intense field of research. The anticancer potential of adenosine receptor ligands has been brought forefront of research and evidenced in innumerous research articles and patents. OBJECTIVE: The present review focuses on the patent literature from 2002 onwards (2002-2017)...
November 7, 2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/29090670/the-epithelial-mesenchymal-transition-pathway-in-two-cases-with-gastric-metastasis-originating-from-breast-carcinoma-one-with-a-metachronous-primary-gastric-cancer
#8
Simona Gurzu, Laura Banias, Tivadar Bara, Istvan Feher, Tivadar Jr Bara, Ioan Jung
BACKGROUND: Metastases to the stomach are extremely rare and the metastatic pathway is not well understood. OBJECTIVE: To present two unusual gastric metastases and a review of the literature regarding the pathway of epithelial mesenchymal transition (EMT) in the metastatic cells. METHOD: The clinicopathological aspects of the two cases were presented in the light of the most recent patents. Data about patents were obtained from the online databases PubMed, World Intellectual Property Organization (WIPO) and Google patents...
November 1, 2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/29086701/nucleic-acid-sensing-machinery-targeting-innate-immune-system-for-cancer-therapy
#9
Sandra Iurescia, Daniela Fioretti, Monica Rinaldi
• Background Nucleic acid sensing is an essential strategy employed by the innate immune system to detect both pathogen-derived nucleic acids and self-DNA released by host apoptotic or necrotic cells. The presence of nucleic acids that gain access to the cytoplasm is perceived by mammalian cells as "stranger" or "danger" signals that triggers a myriad of immunological responses. Recent publications have highlighted the importance of nucleic acid sensing machinery as mediator of innate and adaptive immunity, and cGAS, STING and RIG-I agonists have been validated as immuno-oncology agents in cancer therapy...
October 30, 2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/29076433/nlrp3-inflammasome-activation-inhibitors-in-inflammation-associated-cancer-immunotherapy-an-update-on-the-recent-patents
#10
Spandana Rajendra Kopalli, Tae-Bong Kang, Kwang-Ho Lee, Sushruta Koppula
BACKGROUND: Inflammasomes are recognized as key regulators in innate immunity from the pathogenic to endogenous danger signals. Although controlled activation of inflammasome is highly beneficial, dysregulation of inflammasome activation plays central role in various autoimmune, inflammatory disorders and aid in promoting various forms of cancers in humans such as breast cancer, fibrosarcoma, gastric carcinoma, and lung metastasis. NLRP3 inflammasome activation has been emerged as a topic of interest and is under profound investigation for its involvement in multiple forms of cancers...
October 26, 2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/28971778/strategies-to-tackle-radiation-resistance-by-penetrating-cancer-stem-cell-line-of-scrimmage
#11
So-Yeon Park, Ji-Young Kim, Youngsoo Jun, Jeong-Seok Nam
BACKGROUND: Radiation therapy has become a common therapy for cancer patients and largely improved therapeutic outcomes. However, recurrence after radiation therapy is still a major unsolved concern of cancer patients. The cancer stem cells (CSCs), a small sub-population with capacity of self-renewal and differentiation into diverse types of cancer cells, are considered as strong drivers of metastasis, resistance, and recurrence. OBJECTIVE: We overview the mechanisms behind the radiation resistance of CSCs, and introduce recent patents with the potential to overcome such an obstacle...
October 3, 2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/28969581/molecular-modelling-of-berberine-derivatives-as-inhibitors-of-human-smoothened-receptor-and-hedgehog-signalling-pathway-using-a-newly-developed-algorithm-on-anti-cancer-drugs
#12
Parham Jabbarzadeh Kaboli, Mohammad Bazrafkan, Patimah Ismail, King-Hwa Ling
BACKGROUND: Protoberberine isoquinoline alkaloids are found in many plant species. They consist of a diverse class of secondary metabolites with many pharmacologically active members, such as different derivatives of berberine already patented. In the development of approximately 20-25% of all cancers, altered hedgehog (Hh) signalling is involved where the smoothened (Smo) transmembrane receptor triggers Hh signalling pathway towards Gli1 gene expression. OBJECTIVE: The current study aimed to model and verify the anti-Smo activity of berberine and its derivatives using a novel automated script...
September 29, 2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/28933264/from-a-better-understanding-of-the-mechanisms-of-action-of-histone-deacetylases-inhibitors-to-the-progress-of-the-treatment-of-malignant-lymphomas-and-plasma-cell-myeloma
#13
Romeo-Gabriel Mihăilă
BACKGROUND: Notable progress has been made in chemo- and immunotherapy of B-cell lymphomas, but less in the treatment of T-cell lymphomas. OBJECTIVE: Histone deacetylases inhibitors are a potentially useful therapeutic mean, as an epigenetic dysregulation is present in lymphomas, and especially in T-cell types. We aimed to study the progress made in this area. METHOD: A minireview was achieved using the articles published in PubMed in the last two years and the new patents made in this field...
September 19, 2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/28875828/synergistic-effect-of-epidermal-growth-factor-receptor-inhibitors-and-ionization-radiation-in-cancer-treatment
#14
Zahra Shaghaghi, Seyed Jalal Hosseinimehr
cancer cells to treatment. OBJECTIVE: This review discusses the combined effect of EGFR inhibitor and radiation therapy in cancer treatment. METHOD: The recent literature and patent applications were considered in which the role of EGFR in cancer and EGFR inhibitors, as well as the preclinical and clinical studies related to synergistic effects of EGFR inhibitors and ionizing radiation in the treatment of various cancers. RESULTS: The specific inhibition has been introduced as targeted therapy for treatment of cancers...
August 29, 2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/28786345/bet-inhibitors-as-anticancer-agents-a-patent-review
#15
Imran Ali, Gildon Choi, Kwangho Lee
BACKGROUND: Bromodomain and extra terminal (BET) family of bromodomain proteins (BRDs), comprised of four members in humans (BRD2, BRD3, BRD4, and BRDT), has emerged as a promising new cancer target class for small-molecule drug discovery. OBJECTIVE: This review discusses the patent literature of BET inhibitors (2010-2017) for the treatment of cancer and other related diseases. METHOD: BET proteins act as 'epigenetic readers' and bind to acetylated lysine residues on the tails of histones H3 and H4...
August 8, 2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/28748750/chemical-space-of-flt3-inhibitors-as-the-potential-anti-aml-drugs
#16
Qingyuan Lan, Yanle Zhi, Hao Heng, Xiaoxing Guo, Haichun Liu, Yadong Chen, Tao Lu, Shuai Lu
FLT3 is a member of receptor tyrosine kinase III family, expressed in normal bone marrow cells, early progenitor cells and hematopoietic stem cells. The aberrant expression and function of FLT3 are strongly related leukemia, especially acute myeloid leukemia. Its complex amino-acid residues mutations can induce ligand independent activation and downstream signaling transduction, leading to constant proliferation of hematological tumor cells with poor prognosis. Hence FLT3 serves as a promising target in AML chemotherapy...
July 27, 2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/28482791/3d-qsar-comfa-comsia-and-molecular-docking-studies-on-histone-deacetylase-1-selective-inhibitors
#17
Tooba Abdizadeh, Razieh Ghodsi, Farzin Hadizadeh
BACKGROUND: Histone deacetylases (HDACs) are attractive therapeutic targets for the treatment of cancer and other diseases. There are numerous published patent applications till 2017. It was claimed that novel HDACIs were optimized as potential drug candidates, designed for regional or systemic release, and created as significant inhibitors. OBJECTIVE: In the present study, 3D-QSAR and molecular docking were used to provide a theoretical basis for finding highly potent anti-tumor drugs...
May 8, 2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/28393711/emerging-drugs-for-the-treatment-of-cancer-pain-a-review-of-patent-literature-in-2014
#18
R N Brooke Anderson, Samuel Lee, Alaa Abd-Elsayed
BACKGROUND: Pain in oncology patients may be related to underlying disease process, as well as a side effect of chemotherapy and radiation. More than half of all patients with a diagnosis of cancer experience pain, which is often poorly controlled. As such, the treatment of pain in oncology patients demonstrates a significant need to develop new treatment options. OBJECTIVE: This review summarizes 35 patents on the treatment of pain among cancer patients. METHOD: A thorough literature review of all patents filed in 2014 was conducted using PubMed and http://ep...
April 6, 2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/28637419/pharmacological-inhibitors-of-nad-biosynthesis-as-potential-an-ticancer-agents
#19
Stephanie Lucas, Claire Soave, Ghazal Nabil, Zainab Sabry Othman Ahmed, Guohua Chen, Hossny Awad El-Banna, Q Ping Dou, Jian Wang
BACKGROUND: Alteration of cellular metabolism is a hallmark of cancer, which underlies exciting opportunities to develop effective, anti-cancer therapeutics through inhibition of cancer metabolism. Nicotinamide Adenine Dinucleotide (NAD+), an essential coenzyme of energy metabolism and a signaling molecule linking cellular energy status to a spectrum of molecular regulation, has been shown to be in high demand in a variety of cancer cells. Depletion of NAD+ by inhibition of its key biosynthetic enzymes has become an attractive strategy to target cancer...
2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/28595538/immune-cells-act-as-promising-targets-for-the-treatment-of-bone-metastasis
#20
Guojing Luo, Yuedong He, Qian Zhao, Xijie Yu
BACKGROUND: Bone metastasis is a common complication of certain types of cancer, and unfortunately, it is still incurable to date. Immune system is a major defence against tumor cells and bone metastasis. However, the immunodeficient mouse models are widely used in most researches of bone metastasis, thereby excluding the regulatory roles of the immune system in bone metastasis. OBJECTIVE: The aim was to provide a comprehensive overview on the cellular and molecular mechanisms by which immune cells interact with tumor cells and bone cells, as well as recent related patents...
2017: Recent Patents on Anti-cancer Drug Discovery
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