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Recent Patents on Anti-cancer Drug Discovery

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
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
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
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
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
David M Pereira
No abstract text is available yet for this article.
2017: Recent Patents on Anti-cancer Drug Discovery
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
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
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
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
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
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
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
Alexander A Shtil
No abstract text is available yet for this article.
2016: Recent Patents on Anti-cancer Drug Discovery
Maryam Iman, Seyede Samaneh Mostafavi, Seyed Shahriar Arab, Sadegh Azimzadeh, Mansour Poorebrahim
BACKGROUND: Recent studies have shown that the high mortality of patients with colorectal cancer (CRC) is related to its ability to spread the surrounding tissues, thus there is a need for designing and developing new drugs. OBJECTIVE: Here, we proposed a combinational therapy strategy, an inhibitory peptide in combination with miRNA targeting, for modulating CRC metastasis. In this study, some of the recent patents were also reviewed. METHODS: After data analysis with GEO2R and gene annotation using DAVID server, regulatory interactions of differentially expressed genes (DEGs) were obtained from STRING, GeneMANIA, KEGG and TRED databases...
2016: Recent Patents on Anti-cancer Drug Discovery
Lina Yu, Jun Ma, Jichun Han, Bo Wang, Xiaoyu Chen, Caixia Gao, Defang Li, Qiusheng Zheng
BACKGROUND: Recent patent of licochalcone B (LCB) as an antiinflammatory agent has been developed. Emerging evidence shows that LCB may be a promising alternative compound with anti-cancer activities. However, the anticancer mechanism of LCB in MCF-7 cells has not been fully investigated. OBJECTIVE: We aimed to unearth the anti-cancer effect and mechanism of LCB in MCF-7 cells. METHOD: Cell proliferation activity and cell-cycle progression were determined by sulforhodamine B assay and flow cytometry, respectively...
2016: Recent Patents on Anti-cancer Drug Discovery
Marco Scianna, Luca Munaron
BACKGROUND: Cancer is a heterogeneous disease, which is based on an intricate network of processes at different spatiotemporal scales, from the genome to the tissue level. Hence the necessity for the biomedical and pharmaceutical research to work in a multiscale fashion. In this respect, a significant help derives from the collaboration with theoretical sciences. Mathematical models can in fact provide insights into tumor-related processes and support clinical oncologists in the design of treatment regime, dosage, schedule and toxicity...
2016: Recent Patents on Anti-cancer Drug Discovery
Maryam Iman, Zeynab Khansefid, Asghar Davood
BACKGROUND: Ribonucleotide Reductase (RNR) is an important anticancer chemotherapy target. It has main key role in DNA synthesis and cell growth. Therefore several RNR inhibitors, such as hydroxyurea, have entered the clinical trials. Based on our proposed mechanism, radical site of RNR protein reacts with hydroxyurea in which hydroxyurea is converted into its oxidized form compound III, and whereby the tyrosyl radical is converted into a normal tyrosine residue. OBJECTIVE: In this study, docking and molecular dynamics simulations were used for proposed molecular mechanism of hydroxyurea in RNR inhibition as anticancer agent...
2016: Recent Patents on Anti-cancer Drug Discovery
Chie Hoon Song, Janghyeok Yoon, Namuk Ko, Jeung-Whan Han
BACKGROUND: Epigenetics is a biomedical novelty in drug design and disease control whose mechanisms play a significant role in transferring environmental signals to determine patterns of gene expression. Systematic identification of the main trends in epigenetics patenting activity provides insights into fundamental building blocks of this research field and policy guidance to funding agencies. OBJECTIVE: The review aims at providing a comprehensive overview of the research and development trend in epigenetics by mapping the knowledge structure in patent landscape...
2016: Recent Patents on Anti-cancer Drug Discovery
Jun-He Zhang, Ai-Ling Du, Li Wang, Xiao-Yin Wang, Jian-Hui Gao, Tian-Yun Wang
BACKGROUND: Gene therapy is a promising approach for the treatment of various cancers. However, most viral vectors used for this purpose carry risks, including potential integration into the host genome. OBJECTIVE: We addressed this issue in the present study by constructing an episomal lentiviral vector using the .-interferon matrix attachment region to express the microRNA -145(miR-145), and examining the effect of miR-145 overexpression on human esophageal carcinomas (EC) cells...
2016: Recent Patents on Anti-cancer Drug Discovery
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