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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, Zhe-Sheng 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. METHOD: 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...
March 5, 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
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 metastatic cancer patients benefiting from Tamoxifen as an effective anti-hormonal agent in adjuvant therapy, a noticeable number of patients tend to develop resistance. As a result, forming effective approaches in the successful treatment of Tamoxifen resistance in relation to breast cancer requires a comprehensive understanding of the complex signaling pathways and their underlying crosstalks involved...
March 5, 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 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...
February 26, 2018: Recent Patents on Anti-cancer Drug Discovery
Mohit Sharma, Smitha Sammith 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...
February 26, 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 it's inhibition can be one target for design 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...
February 19, 2018: Recent Patents on Anti-cancer Drug Discovery
Suncica Bjelica, Juan Francisco Santibanez
BACKGROUND: IL-17A is a founding member of the IL-17 family that has been implicated in the pathogenesis of inflammatory-associated diseases such as cancer and autoimmune disease. In cancer, IL-17A participates in many key events for tumor development, in part by affecting innate and adaptive immune system and also by direct modulation of many pro-tumor events. Moreover, IL-17A dysregulation at the site of inflammation is associated with rheumatoid arthritis, multiple sclerosis, psoriasis, among others...
February 19, 2018: Recent Patents on Anti-cancer Drug Discovery
Silvia Martina Ferrari, Ilaria Ruffilli, Marco Centanni, Camilla Virili, Gabriele Materazzi, Magdalini Alexopoulou, Mario Miccoli, Alessandro Antonelli, Poupak Fallahi
BACKGROUND AND OBJECTIVE: Lenvatinib is an oral, multitargeted tyrosine kinase inhibitor (TKI) of vascular endothelial growth factor receptors (VEGFR1-VEGFR3), fibroblast growth factor receptors (FGFR1-FGFR4), platelet-derived growth factor receptor (PDGFR)α, rearranged during transfection (RET), and v-kit (KIT) signaling networks implicated in tumor angiogenesis. METHOD: Here we review the scientific literature about lenvatinib in the treatment of thyroid cancer...
February 19, 2018: Recent Patents on Anti-cancer Drug Discovery
Monireh Mohsenzadegan, Farhad Seif, Mohammad Morad Farajollahi, Majid Khoshmirsafa
BACKGROUND: Tumor cells may be expressed as a result of oxidative stress. The extent of oxidative stress correlates with aggressive and metastatic potency of cancer. OBJECTIVE: One simple way to control prostate cancer is through chemoprevention which refers to the administration of natural or synthetic agents to block, reverse, or delay the process of carcinogenesis. The most chemopreventive agents are antioxidants in the nature. METHODS: In this review, we summarized the effects of dietary antioxidants with a focus on their molecular mechanisms and possible roles in the treatment of prostate cancer cells...
February 13, 2018: Recent Patents on Anti-cancer Drug Discovery
Theodosis Kalamatianos, Despoina Denekou, George Stranjalis, Evangelia Papadimitriou
BACKGROUND: Glioblastoma (GBM) is the most aggressive and common brain tumor in adults, currently lacking effective life-prolonging and recurrence-preventing therapy; median survival of GBM patients stands at only 14-16 months. Increasing lines of evidence indicate that Anaplastic lymphoma kinase (ALK), a druggable tyrosine kinase receptor over-expressed in GBM, represents a potential therapeutic target in this tumor. OBJECTIVE: An overview of the state of the art and the existing recent patents regarding potential exploitation of ALK as a therapeutic target and/or diagnostic/prognostic factor in GBM...
January 15, 2018: Recent Patents on Anti-cancer Drug Discovery
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
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...
2018: Recent Patents on Anti-cancer Drug Discovery
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
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
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
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...
November 20, 2017: Recent Patents on Anti-cancer Drug Discovery
Romeo G Mihaila
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 mini-review was achieved using the articles published in PubMed in the last two years and the new patents made in this field...
November 20, 2017: Recent Patents on Anti-cancer Drug Discovery
Zahra Shaghaghi, Seyed Jalal Hosseinimehr
BACKGROUND: Epidermal Growth Factor Receptor (EGFR) is overexpressed in a variety of cancers and is associated with poor prognosis, low survival rate, and resistance of 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 are related to synergistic effects of EGFR inhibitors and ionizing radiation in the treatment of various cancers...
November 20, 2017: Recent Patents on Anti-cancer Drug Discovery
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...
November 20, 2017: Recent Patents on Anti-cancer Drug Discovery
Qing-Yuan Lan, Yan-Le Zhi, Hao Heng, Jie-Yi Tian, Xiao-Xing Guo, Hai-Chun Liu, Ya-Dong Chen, Tao Lu, Shuai Lu
BACKGROUND: FLT3 is a member of receptor tyrosine kinase III family, mainly expressed in hematopoietic cells. The aberrant expression and function of FLT3 are strongly related to leukemia, especially acute myeloid leukemia. Its varieties of amino-acid residues mutations, such as FLT3-ITDs and -TKDs, can induce constant proliferation of hematological tumor cells with poor prognosis. Hence FLT3 serves as a promising target in AML chemotherapy. OBJECTIVE: This review focused on the progress of FLT3 inhibitors study including those that have entered clinical trials or were reported in numerous patents all over the world...
November 20, 2017: Recent Patents on Anti-cancer Drug Discovery
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