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Recent Patents on Anti-cancer Drug Discovery

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https://www.readbyqxmd.com/read/28482792/poly-adp-ribosyl-polymerase-1-inhibitors-a-patent-review
#1
Mengda Cao, Xi Sun, Yanjun Zhou, Wen Huang, Ling Meng, Ji-Fu Wei
BACKGROUND: Poly (ADP-ribosyl) polymerase 1 (PARP1) is important in maintaining genomic stability, repairing DNA damage, and regulating transcriptional processes. Altered PARP1 activity is associated with a multitude of pathologies especially cancer. The broad application prospects of PARP1 inhibitors attract many well-known pharmaceutical companies, which promotes the development of PARP1 inhibitors. Objective:Present review aims to introduce PARP1 inhibitors by their structures and try to point out future development direction of PARP1 inhibitors...
May 8, 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
#2
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/28443515/indication-of-bevacizumab-for-cerebral-radiation-necrosis
#3
Hongqing Zhuang, Xiangkun Yuan, Zhiyong Yuan, Ping Wang
BACKGROUND: The effect of bevacizumab (BVZ) for cerebral radiation necrosis (CRN) was clear. However, the indications of BVZ had no reports. OBJECTIVE: The aim of the paper was to investigate the indications of BVZ for CRN. METHODS: Fourteen CRN patients (confirmed by imaging diagnosis)who underwent BVZ treatment between June 2011 and December 2014 were analyzed. BVZ was administered (5 mg/kg body weight) once every three to four weeks for at least three cycles...
April 25, 2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/28440207/epithelial-mesenchymal-transition-in-cancer-progression-preventive-phytochemicals
#4
Soorya Parathodi Illam, Arunaksharan Narayanankutty, Shaji Edappilly Mathew, Remya Valsalakumari, Rosemol M Jacob, Achuthan Chathrattil Raghavamenon
BACKGROUND: Epithelial-Mesenchymal Transition (EMT) is the conversion of epithelial cells into mesenchymal phenotype generally observed during embryogenesis and wound healing as well as in malignant transformation. Several signaling pathways and transcription factors associated with EMT have been explored. Dietary phytochemicals are multi-targeted agents that interfere with these pathways, assume preventive potential against pathologic EMT. OBJECTIVE: Present review aims to provide a detailed description on the nature, characteristics of EMT in physiological and pathophysiological conditions and the scope of phytochemicals in its prevention...
April 24, 2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/28440206/role-of-foxm1-in-the-progression-and-epithelial-to-mesenchymal-transition-of-gastrointestinal-cancer
#5
Jing Zhang, Yangyang Niu, Chen Huang
Background and Objective:Gastrointestinal (GI) cancer, characterized by its leading mortality, is one of the most common cancers worldwide. The underlying mechanisms contributing to epithelial to mesenchymal transition (EMT) and metastasis of GI cancer is poorly understood. It is well known that a great number of transcription factors including FoxM1, KLF4, STAT3 and so forth, are associated with the process of EMT and have also been strongly implicated in the proliferation, migration, and invasion of GI cancer cells...
April 24, 2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/28440205/in-vitro-collapsing-colon-cancer-cells-by-selectivity-of-disulfiram-loaded-charge-switchable-nanoparticles-against-cancer-stem-cells
#6
Marwa Muhammad Abu-Serie, Fatma Hassan El-Rashidy
BACKGROUND: Different strategies against colon cancer are accompanied by treatment failure, because of drug toxicity toward normal cells and cancer stem cells (CSCs) resistance. However, previous patent evaluated liposome that encapsulated inhibitor of CSCs' aldehyde dehydrogenase (ALDH)1; disulfiram, for targeting breast CSCs. Liposome has disadvantages due to its hydrophobicity. OBJECTIVES: Designing hydrophilic nanoparticles have selectivity to release disulfiram in CC cells rather than in normal colonocytes based on variation in microenvironment between normal and cancer cells...
April 24, 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
#7
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/28245776/activating-mutations-of-esr1-brca1-and-cyp19-aromatase-genes-confer-tumor-response-in-breast-cancers-treated-with-antiestrogens
#8
Zsuzsanna Suba
BACKGROUND: Four decades of erroneous breast cancer therapy with antiestrogens yielded the chaotic mixture of manifestations of artificial ER-inhibition and compensatory activating ER-mutations together with unreckonable tumor responses. OBJECTIVE: Due to the confusions between the anticancer and carcinogenic impacts of antiestrogens and synthetic estrogens, the old principle needs to be revised as concerns ER-signaling induced DNA-damage and breast cancer development...
February 27, 2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/28164756/integrin-targeted-peptide-and-peptidomimetic-drug-conjugates-for-the-treatment-of-tumors
#9
Daniela Arosio, Leonardo Manzoni, Cristina Corno, Paola Perego
BACKGROUND: Integrins are heterodimeric cell surface receptors that mediate cell-cell and cell-extracellular matrix adhesion. These molecules play a role in processes such as cell growth and proliferation, differentiation, migration, cell trafficking, besides contributing to angiogenesis and tumor development. Given their biological role, integrins have been proposed as amenable targets in medicinal chemistry. In particular, ανβ3, ανβ5, ανβ6 and α5β1, integrins involved in tumor angiogenesis and metastasis, have been the subject of studies aimed at the discovery of novel cancer therapeutics...
February 3, 2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/28137213/docking-and-qsar-studies-of-1-4-dihydropyridine-derivatives-as-anticancer-agent
#10
Shirin Mollazadeh, Jamal Shamsara, Maryam Iman, Farzin Hadizadeh
BACKGROUND: The multidrug resistance (MDR) of cancer cells has become a great barrier to the success of chemotherapy. OBJECTIVE: In this study quantitative structure activity relationship (QSAR) modeling was applied to 461,4-dihydropyridine structures (DHPs),and some selected compounds were docked. METHODS: QSAR was used to generate models and predict the MDR inhibitory activity for a series of 1,4-dihydropyridines (DHP). The DHPs were built and optimized using the Sybyl program (x1...
January 26, 2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/28067173/marine-derived-anticancer-drugs-targeting-microtubule
#11
Oindrila De, Biswa Prasun Chatterji
BACKGROUND: Microtubule dynamics play a vital role in regulating crucial cellular functions and are one of the most attractive anticancer drug targets. Microtubule targeting agents (MTAs) such as the vinca alkaloids or taxanes, although are effective for cancer therapy, have adverse side effects. Another hindrance in their development is multiple drug resistance in tumor cells. These drawbacks have urged the need to develop novel MTAs from alternative sources, with better therapeutic efficacy...
January 9, 2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/28056753/role-of-ncrnas-in-development-diagnosis-and-treatment-of-human-cancer
#12
Francisco Esteban Nicolas Molina
BACKGROUND: Since the first reports of microRNAs and the advent of new sequencing technologies, a whole new world of regulatory non-conding RNAs (ncRNAs) has revolutionized our knowledge of the RNA dimension. Thousands of functional non-coding transcripts has been identified and grouped into new classes of ncRNAs attending to their origin and function. Despite of the fact that we have just started to study ncRNAs, it is now clear that these new regulatory actors play an important role in most of the regulated biological processes and in almost all species...
January 5, 2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/28284026/editorial-thematic-issue-modulation-of-proteostasis-and-proteolytic-pathways-as-an-anti-cancer-strategy
#13
EDITORIAL
David M Pereira
No abstract text is available yet for this article.
2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/27881057/recent-patents-on-heat-shock-proteins-targeting-antibodies
#14
REVIEW
Joao C Fernandes, Pedro Alves
BACKGROUND: Heat shock proteins (Hsp) are major chaperone molecules that have recently emerged as cancer therapeutic targets owing to their involvement in tumor cell proliferation, differentiation, invasion and metastasis. High levels of extracellular Hsp90 and Hsp70 have been closely associated with a wide range of human cancers. Accumulating evidence suggests that the pharmacological inhibition of these molecules can play a pivotal role in non-surgical cancer treatment. Efforts have been taken to develop monoclonal antibodies (mAbs) and antibody fragments targeting extracellular Hsp90 and Hsp70, alone or conjugated with standard anticancer agents, to control several types of cancer, such as breast, colon, prostate or melanoma...
2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/27881056/recent-patents-on-proteasome-inhibitors-of-natural-origin
#15
REVIEW
Daniela Correia da Silva, Paula B Andrade, Vera Ribeiro, Patricia Valentao, David M Pereira
BACKGROUND: The proteasome is the major proteolytic site on the eukaryotic cell, degrading most of its short-lived or misfolded polypeptides. The ubiquitin-proteasome pathway has been found to play a fundamental role in the development of several pathologies, from cancer to neurodegenerative diseases, or even retroviral infections. Nature remains a powerful source for the discovery of bioactive compounds. Recently, a number of molecules of natural origin, as well as natural product derivatives, have been described as proteasome inhibitors...
2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/27809750/chaperoning-the-cancer-the-proteostatic-functions-of-the-heat-shock-proteins-in-cancer
#16
REVIEW
Sepideh Vahid, Daksh Thaper, Amina Zoubeidi
BACKGROUND: Protein homeostasis (proteostasis) is vital for the survival of cells in physiological and pathological conditions. Particularly, cancer cells are in constant state of cellular stress due to rapid proliferation and decreased quality control in proteosynthesis and therefore, are exceedingly dependent on the homeostasis pathways. Among the complex biological mechanisms regulating proteostasis are the highly conserved molecular chaperones, heat shock proteins (HSPs). HSPs assist cell survival by catalysing the proper folding of proteins, modulation of the apoptotic machinery and finally regulating the protein degradation machinery, providing either the stability or the degradation of selected proteins under stress conditions...
2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/27804867/medicinal-chemistry-insights-into-novel-hdac-inhibitors-an-updated-patent-review-2012-2016
#17
REVIEW
Peng Zhan, Xueshun Wang, Xinyong Liu, Takayoshi Suzuki
BACKGROUND: Many laboratories have made intensive efforts to develop potent, selective, and orally bioavailable HDAC inhibitors (HDACIs). Novel HDACIs are being developed with the objective of improving potency and selectivity against specific types of cancers or non-cancer diseases. OBJECTIVE: This updated patent review is an attempt to compile the work of various researchers of HDACIs from 2012 to mid 2016, and to enlighten and surprise both newcomers in this field and devoted medicinal chemists...
2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/27784232/melissa-of-cinalis-and-vitamin-e-as-the-potential-therapeutic-candidates-for-reproductive-toxicity-caused-by-anti-cancer-drug-cisplatin-in-male-rats
#18
Maryam Iman, Mostafa Araghi, Toktam Heidari, Vahid Mohammadi
BACKGROUND: High doses of Cisplatin (CP) can disrupt the normal functioning of various tissues such as ovaries and testis. In almost all the patients, spermiotoxicity of CP causes temporary or permanent azoospermia. OBJECTIVE: In this study, the defensive effect of Melissa of cinalis and vitamin E against testicular injuries caused by CP in male rats was evaluated. METHOD: Thirty six male rats were distributed into 6 groups. Group 1 was used as the negative control...
2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/27739356/contribution-of-latin-american-countries-to-cancer-research-and-patent-generation-recent-patents
#19
REVIEW
Martin Perez-Santos, Maricruz Anaya-Ruiz, Cindy Bandala
BACKGROUND: Data mining publications and patent data can provide decision support for scientists, inventors and industry in the field of cancer research. OBJECTIVE: The main objective of this article it to identify trends of research and patent generation productivity originating from Latin American countries in the field of cancer. METHOD: Publications were collected from the Scopus, Web of Science, PubMed database; and patents were collected from Latipat Espacenet databases...
2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/27697069/kinase-inhibitor-indole-derivatives-as-anticancer-agents-a-patent-review
#20
REVIEW
Anuj K Rathi, Riyaz Syed, Vijay Singh, Han-Seung Shin, Rahul V Patel
Cancer accounts for a number of deaths each year. Consequently, prevention of this deadly disease is more challenging and hence the invention of new anticancer agents is of utmost importance. The current review elaborates the importance of indole designs as patented in the form of anticancer druglike molecules targeting different cites of biological arena. Specific attention was given to kinases such as platelet-derived growth factor receptor, vascular endothelial growth factor receptor and fibroblast growth factor receptor, Bruton's tyrosine kinase, anaplastic lymphoma kinase, Janus kinase, cyclin-dependent kinase aurora kinases A, B and C, checkpoint kinases, protein kinase R, Pim kinases, phosphoinositide 3- kinase, altered proteins kinases, polo-like kinase and many more...
2017: Recent Patents on Anti-cancer Drug Discovery
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