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Discovery Of Dna Binding Anticancer Drugs That Target Oncogenic Transcription Factors Associated With Human Breast Cancer
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Book Synopsis Discovery of DNA Binding Anticancer Drugs That Target Oncogenic Transcription Factors Associated With Human Breast Cancer by :
Download or read book Discovery of DNA Binding Anticancer Drugs That Target Oncogenic Transcription Factors Associated With Human Breast Cancer written by and published by . This book was released on 2001 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: This proposal is designed to develop sequence specific DNA binding polyamides as an approach for specifically inhibiting Her2/neu expression, a gene that is over expressed in human breast cancers. The approach is to design polyamides that are optimized for targeting the binding of ESX a transcription factor which up regulates Her2/neu by binding to its consensus site within the Her2/neu promoter. Active agents are tested for their ability to inhibit Her2/neu expression in both cell free and cellular system & A number of polyamides were identified as being effective inhibitors of ESX complex formation and their ability to block complexes was analyzed in detail. None of the agents were effective at preventing expression in cells. A series of fluorescently labeled polyamides representing structural diverse compounds were tested for their ability to localize in the nucleus of live cells. No agent was found to localize in the nucleus even at relatively high concentrations or for incubations times up to several days. Studies are underway to develop a new generation of polyamides that posses not only the ability to effectively target the HER2/neu promoter under cell free conditions but also to function effectively on nuclear DNA targets in intact cells.
Book Synopsis Small-Molecule Transcription Factor Inhibitors in Oncology by : Khondaker Miraz Rahman
Download or read book Small-Molecule Transcription Factor Inhibitors in Oncology written by Khondaker Miraz Rahman and published by Royal Society of Chemistry. This book was released on 2018-09-06 with total page 214 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book highlights recent progress in the development of small-molecule inhibitors of oncogenic transcription factors and is relevant for postgraduates, researchers and practitioners.
Book Synopsis DNA Binding Drugs Targeting the Regulatory DNA Binding Site of the ETS Domain Family Transcription Factor Associated With Human Breast Cancer by :
Download or read book DNA Binding Drugs Targeting the Regulatory DNA Binding Site of the ETS Domain Family Transcription Factor Associated With Human Breast Cancer written by and published by . This book was released on 1999 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: The goal of this project is to test and to develop a new class of drugs, polyamide, which can selectively and effectively inhibit the function of transcription factors whose aberrant regulation of gene expression is associated with human breast cancer. The Her2/neu oncogene promoter is selected as a model for this study. The key approach is to prevent the binding of two transcription factors, ESX and AP-2, to the consensus DNA binding sites contained within the Her2/neu promoter resulting in inhibition of transcription factor function. If successful, the drugs will be able to prevent the targeted transcription factors from binding to DNA and thus they cannot enhance the activity of the proteins associated with the cancer cell. These new types of drugs have potential to be designed specifically to block the cellular proteins that are implicated in human breast cancers. Not only will these drugs have the potential to become a new type of anticancer agent they may also be used as tools to identify other proteins involved in breast cancer.
Author :Nicholas B. La Thangue Publisher :Springer Science & Business Media ISBN 13 :1592591531 Total Pages :358 pages Book Rating :4.5/5 (925 download)
Book Synopsis Targets for Cancer Chemotherapy by : Nicholas B. La Thangue
Download or read book Targets for Cancer Chemotherapy written by Nicholas B. La Thangue and published by Springer Science & Business Media. This book was released on 2002-04-03 with total page 358 pages. Available in PDF, EPUB and Kindle. Book excerpt: In Targets for Cancer Chemotherapy: Transcription Factors and Other Nuclear Proteins, a panel of leading basic researchers, pharmaceutical scientists, and clinical oncologists explain in detail the therapeutically-relevant protein targets that contribute to cancer pathology and spell out their implications for cancer drug discovery and clinical application. The authors identify and illuminate selected transcription factor oncoproteins and tumor suppressors, together with nuclear proteins that are central to the phenotype of the tumor cell involved in chromatin control. The emphasis is on new targets and approaches to cancer treatment derived from the cancer cell cycle, gene control targets, and angiogenesis.
Book Synopsis Cancer Drug Resistance by : Beverly A. Teicher
Download or read book Cancer Drug Resistance written by Beverly A. Teicher and published by Springer Science & Business Media. This book was released on 2007-11-09 with total page 611 pages. Available in PDF, EPUB and Kindle. Book excerpt: Leading experts summarize and synthesize the latest discoveries concerning the changes that occur in tumor cells as they develop resistance to anticancer drugs, and suggest new approaches to preventing and overcoming it. The authors review physiological resistance based upon tumor architecture, cellular resistance based on drug transport, epigenetic changes that neutralize or bypass drug cytotoxicity, and genetic changes that alter drug target molecules by decreasing or eliminating drug binding and efficacy. Highlights include new insights into resistance to antiangiogenic therapies, oncogenes and tumor suppressor genes in therapeutic resistance, cancer stem cells, and the development of more effective therapies. There are also new findings on tumor immune escape mechanisms, gene amplification in drug resistance, the molecular determinants of multidrug resistance, and resistance to taxanes and Herceptin.
Book Synopsis Developing Novel Anticancer DNA-binding Drugs to Disrupt ETS-Mediated Transcription Associated with Breast Cancer: Use of the C-fos Serum Response Element as a Model System by :
Download or read book Developing Novel Anticancer DNA-binding Drugs to Disrupt ETS-Mediated Transcription Associated with Breast Cancer: Use of the C-fos Serum Response Element as a Model System written by and published by . This book was released on 2002 with total page 56 pages. Available in PDF, EPUB and Kindle. Book excerpt: Disregulated transcription factor (TF)-mediated activation of gene expression can play a key role in oncogenesis, especially in breast cancer, preventing TF/DNA interactions using small molecule DNA-reactive agents may decrease oncogenic gene expression and potentially halt cancer development. Our goal is to improve DNA-binding drugs' abilities to inhibit specific TF/DNA interactions using the human c-fos promoter's serum response element (SRE) as a target. In an effort to improve drug effectiveness, the novel minor groove-binding fluorescent microgonotropens (FMGTs) were developed. These A/T selective bisbenzimidazole-based agents have polyamine tails that contact DNA's phosphodiester backbone, allowing them to bind with very high affinity. We explored the potential of these agents to inhibit TF/DNA complex formation in a series of increasingly complex assays in the c-fos model and assessed whether their ability to contact both grooves makes them more effective than classical minor groove-binding drugs. Analyzing these agents using a well-defined gene regulatory element has provided insight into the relationship between their chemical structure and biological activities. Notably, our studies revealed that one agent, L2, was the only FMGT to inhibit endogenous c-fos gene expression. L2 is therefore a promising lead candidate for future drug design studies.
Book Synopsis Frontiers in Anti-Cancer Drug Discovery by : Atta-ur-Rahman
Download or read book Frontiers in Anti-Cancer Drug Discovery written by Atta-ur-Rahman and published by Bentham Science Publishers. This book was released on 2015-05-05 with total page 280 pages. Available in PDF, EPUB and Kindle. Book excerpt: “Frontiers in Anti-Cancer Drug Discovery” is an Ebook series devoted to publishing the latest and the most important advances in Anti-Cancer drug design and discovery. Eminent scientists write contributions on all areas of rational drug design and drug discovery including medicinal chemistry, in-silico drug design, combinatorial chemistry, high-throughput screening, drug targets, recent important patents, and structure-activity relationships. The Ebook series should prove to be of interest to all pharmaceutical scientists involved in research in Anti-Cancer drug design and discovery. Each volume is devoted to the major advances in Anti-Cancer drug design and discovery. The Ebook series is essential reading to all scientists involved in drug design and discovery who wish to keep abreast of rapid and important developments in the field. The fifth volume of the series features chapters on the following topics: -Nutraceuticals and natural food products for cancer treatment -Pharmacogenomics in Anti-cancer treatment -Cancer stem cells -Potassium channel targeting for brain tumor treatment -Sorafenib in the management of hepatocellular carcinoma …and more.
Book Synopsis Novel Anticancer Drug Protocols by : John K. Buolamwini
Download or read book Novel Anticancer Drug Protocols written by John K. Buolamwini and published by Springer Science & Business Media. This book was released on 2008-02-01 with total page 349 pages. Available in PDF, EPUB and Kindle. Book excerpt: We are in an exciting era in the war against cancer, with real prospects for novel anticancer drugs that are cancer cell-specific without the toxicities that have been the hallmark of conventional cytotoxic cancer chemotherapy. Advances in cancer cell biology fueled by the molecular biology revolution have resulted in the uncovering of many novel potential molecular targets for cancer therapy. New anticancer drug discovery and development is now largely focused on exploiting these new molecular targets, which encompass oncogenes, tumor s- pressor genes, and their gene products, as well as targets involved in tumor angiogenesis, metastasis, survival, and longevity mechanisms. Exploitation of some of these targets has already yielded fruits and introduced new paradigms of molecularly targeted cancer therapy into the clinic, namely, protein kinase in- bition by antibodies or small molecules, exemplified by Herceptin® (trastuzumab), a humanized antibody targeted against the HER-2 growth factor receptor tyrosine kinase for the treatment of metastatic breast cancer; and Gleevec, a small molecule bcr-abl kinase inhibitor for the treatment of chronic myel- enous leukemia.
Book Synopsis Molecules Engineered Against Oncogenic Proteins and Cancer by : E. J. Corey
Download or read book Molecules Engineered Against Oncogenic Proteins and Cancer written by E. J. Corey and published by John Wiley & Sons. This book was released on 2023-09-06 with total page 404 pages. Available in PDF, EPUB and Kindle. Book excerpt: Molecules Engineered Against Oncogenic Proteins and Cancer A comprehensive review of the latest molecular advances in cancer treatment Featuring 91 total small molecule kinase/KRAS inhibitors, 80 of which are FDA-approved, Molecules Engineered Against Oncogenic Proteins and Cancer documents the recent scientific advances that have transformed one of medicine’s most challenging areas—cancer treatment. Most of these inhibitors specifically block oncogene-induced carcinogenic proteins with results that have dramatically advanced the treatment of cancer. In addition, the structural formulas of more than 100 kinase/KRAS inhibitors in clinical trials are presented. With a very well-known chemist as an author, Molecules Engineered Against Oncogenic Proteins and Cancer includes information on: Each molecule’s structure, function of the kinase target and relevance to cancer, the drug discovery process, and molecular details of drug action Mutated protein kinases as oncoproteins and targets for inhibition, along with the details of discovery for each antitumor antikinase agent History of oncoprotein inhibitors and their role in advancing the treatment and understanding of cancer The discovery process as a whole, effective strategies for innovation, ongoing challenges, and a glimpse of the future of the field Combining the most significant recent discoveries in a unique and useful way, Molecules Engineered Against Oncogenic Proteins and Cancer is an essential resource for researchers and students in bioscience, medicine, chemistry, and oncology as well as for those at industrial companies involved in therapeutic discovery.
Book Synopsis Oncogene-Directed Therapies by : Janusz W. Rak
Download or read book Oncogene-Directed Therapies written by Janusz W. Rak and published by Springer Science & Business Media. This book was released on 2002-12-03 with total page 487 pages. Available in PDF, EPUB and Kindle. Book excerpt: Prominent investigators and clinicians summarize in a balanced blend of fundamental science, basic research, experimental therapeutics, and early clinical experiences, what is known about oncogenes and oncogenesis, and describe how that knowledge can be used to treat the cancer. The contributors explain how, why, and under what conditions certain proteins acquire the ability to transform eukaryotic cells, and detail the crucial biological consequences of this oncogenic transformation, particularly for cellular mitogenesis, survival, differentiation, migration, proteolysis, or angiogenic competence. Their articles thoroughly explicate the premises, principles, techniques, and approaches to oncogene targeting in various types of human cancer by using signal transduction inhibitors, immunological targeting methods, and antisense gene therapy.
Book Synopsis The Molecular Basis of Human Cancer by : William B. Coleman
Download or read book The Molecular Basis of Human Cancer written by William B. Coleman and published by Springer Science & Business Media. This book was released on 2001-08-10 with total page 580 pages. Available in PDF, EPUB and Kindle. Book excerpt: Internationally renowned basic and clinical scientists provide an account of our best current understanding of the genetics of cancer. These authoritative contributors describe in detail each of the known molecular mechanisms governing neoplastic transformation in the breast, prostate, lung, liver, colon, and skin, and in the leukemias and lymphomas. Their discussion illuminates both recent developments and established concepts in epidemiology, molecular techniques, oncogenesis, and mutation mechanisms, as well as the chemical, viral, and physical mechanisms in cancer induction.
Book Synopsis DNA and DNA-interacting Proteins as Anticancer Drug Targets by : Chandanamalie Punchihewa
Download or read book DNA and DNA-interacting Proteins as Anticancer Drug Targets written by Chandanamalie Punchihewa and published by . This book was released on 2006 with total page 280 pages. Available in PDF, EPUB and Kindle. Book excerpt: DNA is both the oldest and newest of targets for cancer therapy. While it is already being targeted by many anticancer drugs in the clinic, the development of sequence-specific DNA binders has brought it back to the limelight as a valuable anticancer drug target.
Download or read book Cisplatin written by Bernhard Lippert and published by John Wiley & Sons. This book was released on 1999 with total page 628 pages. Available in PDF, EPUB and Kindle. Book excerpt: 30 years after its discovery as an antitumor agent, cisplatin represents today one of the most successful drugs in chemotherapy. This book is intended to reminisce this event, to take inventory, and to point out new lines of development in this field. Divided in 6 sections and 22 chapters, the book provides an up-to-date account on topics such as - the chemistry and biochemistry of cisplatin, - the clinical status of Pt anticancer drugs, - the impact of cisplatin on inorganic and coordination chemistry, - new developments in drug design, testing and delivery. It also includes a chapter describing the historical development of the discovery of cisplatin. The ultimate question - How does cisplatin kill a cell? - is yet to be answered, but there are now new links suggesting how Pt binding to DNA may trigger a cascade of cellular reactions that eventually result in apoptosis. p53 and a series of damage recognition proteins of the HMG-domain family appear to be involved. The book addresses the problem of mutagenicity of Pt drugs and raises the question of the possible relevance of the minor DNA adducts, e.g. of interstrand cross-links, and the possible use of trans-(NH3)2Pt(II)-modified oligonucleotides in antisense and antigene strategies. Our present understanding of reactions of cisplatin with DNA is based upon numerous model studies (from isolated model nucleobases to short DNA fragments) and application of a large body of spectroscopic and other physico-chemical techniques. Thanks to these efforts there is presently no other metal ion whose reactions with nucleic acids are better understood than Pt. In a series of chapters, basic studies on the interactions of Pt electrophiles with nucleobases, oligonucleotides, DNA, amino acids, peptides and proteins are reported, which use, among others, sophisticated NMR techniques or X-ray crystallography, to get remarkable understanding of details on such reactions. Reactivity of cisplatin, once bound to DNA and formerly believed to be inert enough to stay, is an emerging phenomenon. It has (not yet) widely been studied but is potentially extremely important. Medicinal bioinorganic chemistry - the role of metal compounds in medicine - has received an enormous boost from cisplatin, and so has bioinorganic chemistry as a whole. There is hardly a better example than cisplatin to demonstrate what bioinorganic chemistry is all about: The marriage between classic inorganic (coordination) chemistry and the other life sciences - medicine, pharmacy, biology, biochemistry. Cisplatin has left its mark also on areas that are generally considered largely inorganic. The subject of mixed-valance Pt compounds is an example: From the sleeping beauty it made its way to the headlines of scientific journals, thanks to a class of novel Pt antitumor agents, the so-called "platinum pyrimidine blues". In the aftermath diplatinum (III) compounds were recognized and studies in large numbers, and now an organometalic chemistry of these diplatinum (III) species is beginning to emerge. The final section of the book is concerned with new developments such as novel di- and trinuclear Pt(II) drugs with DNA binding properties different from those of cisplatin, with orally active Pt(IV) drugs which are presently in clinical studies, and with attempts to modify combinatorial chemistry in such a way that it may become applicable to fast screening of Pt antitumor drugs. The potential of including computational methods in solving questions of Pt-DNA interactions is critically dealt with in the concluding chapter.
Book Synopsis DNA Binding Drugs Targeting the Regulatory DNA Binding Site of the ETS Domain Family Transcription Factor by :
Download or read book DNA Binding Drugs Targeting the Regulatory DNA Binding Site of the ETS Domain Family Transcription Factor written by and published by . This book was released on 1998 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: Abnormally expressed ESX and AP-2 have been found in certain breast cancer cell lines that are associated with the overexpression of HER2/neu gene. Amplification and overexpression of HER2/neu is found in 20-30% of primary breast cancers and is correlated with a poor prognosis. In this study, polyamides, minor groove binding compounds, were designed to target the ESX binding site on the HER2/neu promoter to interfere with the gene expression. The effects of polyamides to inhibit the binding of ESX and DNA and associated gene expression were compared with that of distamycin. The results revealed that polyamides were more effective than distamycin to inhibit the ESX-DNA complex formation (25-200 fold). Similarly, in a cell free transcription, polyamides inhibited gene expression from the HER2/neu promoter more strongly than distatnycin. In addition, in vitro transcription time course assay indicated that polyamides constantly associated with DNA to inhibit transcription. In contrast, inhibition of transcription by distamycin was increased relative to the time of incubation. In a conclusion, sequence specific designed polyamides for selected transcription factors are potent inhibitors of transcription factor-DNA complex and transcription. This information can be utilized to futture improve drug specificity and effectiveness as abnormal transcription inhibitors.
Book Synopsis Basic Science of Cancer by : Gary D. Kruh
Download or read book Basic Science of Cancer written by Gary D. Kruh and published by Springer Science & Business Media. This book was released on 2012-12-06 with total page 288 pages. Available in PDF, EPUB and Kindle. Book excerpt: In recent years, great strides have been made in the field of cancer research. Now, with Basic Science of Cancer, a range of interrelated topics such as tumor suppressor genes, apoptosis, transcriptional regulation, pharmacology of anticancer drugs, cytogenetic techniques, oncogenes, and signal transduction are thoroughly addressed. Written for oncologists and healthcare professionals, this new comprehensive reference also discusses modern research techniques used to investigate the molecular etiology and treatment of human cancer. Topics are described using nontechnical terms. Together, complete reference listings and over 200 illustrations provide an extensive, yet introductory, look into the complex field of cancer.
Book Synopsis Evaluation of DNA Binding as Inhibitors of ESX, and ETS Domain Transcription Factor Associated with Breast Cancer: Effects of ESX/DNA Complex Disruption by : Stephanie J. Leslie
Download or read book Evaluation of DNA Binding as Inhibitors of ESX, and ETS Domain Transcription Factor Associated with Breast Cancer: Effects of ESX/DNA Complex Disruption written by Stephanie J. Leslie and published by . This book was released on 1999 with total page 16 pages. Available in PDF, EPUB and Kindle. Book excerpt: DNA binding agents are being evaluated for their ability to disrupt transcription factor binding to DNA and down regulate cancer associated gene expression. Target gene is HER2/neu, which is overexpressed in 30% of breast cancers. Drugs with different modes of binding as well as different sequence preference are being evaluated. Polyamides, a novel group of DNA binding agents with sequence specific binding, are also under evaluation. Cell-free assays such as mobility shift and cell-free transcription are being employed to assess agents' ability to disrupt transcription factor binding. Agents showing potential in cell-free assays were evaluated in whole cell assays using northern analysis. Results in mobility shift assay indicate that sequence specific binding agents inhibit transcription factor DNA complexes better the sequence preference agents by an order of magnitude. In cell-free transcription assays there is less difference between the two types of drugs. Some sequence preference agents are very effective at inhibiting gene expression in whole cells, while first generation polyamides show limited ability to diminish gene expression.
Book Synopsis Evaluation of DNA Binding Drugs as Inhibitors of ESX, and ETS Domain Transcription Factor Associated With Breast Cancer: Effects of ESX/DNA Complex Disruption by : Stephanie Leslie
Download or read book Evaluation of DNA Binding Drugs as Inhibitors of ESX, and ETS Domain Transcription Factor Associated With Breast Cancer: Effects of ESX/DNA Complex Disruption written by Stephanie Leslie and published by . This book was released on 2000 with total page 88 pages. Available in PDF, EPUB and Kindle. Book excerpt: DNA binding agents, sequence preference and sequence specific, were evaluated for their ability to inhibit ESX binding to the HER2/neu promoter and down regulate cancer associated gene expression. Cell-free mobility shift assay results revealed that the sequence specific agents to be far superior to the sequence preference agents at inhibiting transcription factor/DNA complex formation. However, cell-free transcription results did not maintain this order of potency, with each group of agent more equally effective at inhibiting HER2/neu regulated expression. Whole-cell analysis, employing techniques such as northern blot analysis and cytotoxicity. revealed no cellular activity by the sequence specific agents. Conversely, for the sequence preference agents the whole- cell studies revealed a general pattern of potency of G/C sequence preference agents compared to A/T preference agents at inhibiting cellular mRNA levels of the targeted gene HER2/neu and on cellular growth. In depth analysis has revealed polyamide 22 to be cell permeable and localize to the nucleus. Continued studies are underway to determine the nuclear target of polyamide 22 binding. Examination of the structural changes of polyamides and the resultant effect on cellular localization and biological activity are underway and could influence the continued design of these potential therapeutic agents.
