Read Books Online and Download eBooks, EPub, PDF, Mobi, Kindle, Text Full Free.
Discovery Of Peptidomimetric Antagonists Of Estrogen Receptor Coactivator Interactions A Novel Strategy To Combat Tamoxifen Drug Resistance
Download Discovery Of Peptidomimetric Antagonists Of Estrogen Receptor Coactivator Interactions A Novel Strategy To Combat Tamoxifen Drug Resistance full books in PDF, epub, and Kindle. Read online Discovery Of Peptidomimetric Antagonists Of Estrogen Receptor Coactivator Interactions A Novel Strategy To Combat Tamoxifen Drug Resistance ebook anywhere anytime directly on your device. Fast Download speed and no annoying ads. We cannot guarantee that every ebooks is available!
Book Synopsis Discovery of Peptidomimetric Antagonists of Estrogen Receptor - Coactivator Interactions: A Novel Strategy to Combat Tamoxifen Drug Resistance by :
Download or read book Discovery of Peptidomimetric Antagonists of Estrogen Receptor - Coactivator Interactions: A Novel Strategy to Combat Tamoxifen Drug Resistance written by and published by . This book was released on 2001 with total page 6 pages. Available in PDF, EPUB and Kindle. Book excerpt: There exists an urgent need for new drugs that halt the progression of tamoxifen-resistant breast cancers. The recent discovery of peptides that block interactions between tamoxifen-bound estrogen receptors (ER) and steroid receptor coactivator (SRC) proteins bearing an MFDFF peptide motif represents an important initial step toward this goal.' Since peptides do not possess sufficient metabolic stability and cellular permeability to be investigated in animal models of drug-resistant breast cancers, our laboratory is working to identify metabolically stable and cell permeable pepto id (N-alkylglycine) peptidomimetics that block interactions between SRC proteins and tamoxifen-bound ERs. We are working to employ combinatorial chernical methods and rational design to discover compounds that inhibit gene expression activated by tamoxifen-bound ERs in cell culture. These compounds have the potential to allow future evaluation of this strategy in animal models of tamoxifen resistant breast cancer.
Book Synopsis Discovery at the Interface by : David Hudson Lee
Download or read book Discovery at the Interface written by David Hudson Lee and published by . This book was released on 2015 with total page 85 pages. Available in PDF, EPUB and Kindle. Book excerpt: For the past four decades, endocrine ligand-based inhibitor, Tamoxifen (TaM) has been administered as an effective treatment for ER[alpha] positive breast tumors of both premenopausal stage and postmenopausal stage. However, many ER[alpha] positive breast tumors are intrinsically resistant to TaM and other endocrine therapies, despite the tumor having high expression of ER[alpha], and the tumors that are not intrinsically resistant will eventually acquire resistance in advanced stage of tumor progression. The mechanisms of resistance has not been clearly understood, but it is suggested that coregulator proteins of ER[alpha] may play a crucial role in ligand-independent pathways of ER[alpha] transactivation. It has been shown that (i) calmodulin, a ubiquitous Ca2+ sensor protein, is significantly overexpressed in breast tumors; (ii) ER[alpha] and ERE complex formation requires calmodulin directly binding to ER[alpha], and is also required for the activation of an estrogen responsive promoter. The hinge region of ER[alpha] has been shown to participate as an allosteric binding site in the interaction between Estrogen Receptor alpha and calmodulin. Ca2+ -calmodulin directly binds to ER alpha in the hinge region, residues 298 - 317. In search of a novel anti-cancer agent, a library of interaction profiles of human ER-EF hand protein complexes was generated, and S100P was identified as potential targets due to the finding that S100P shares a high degree of sequence and structural homology with Calmodulin. Our objective is to develop peptidomimetics and small molecules to block ER-S100P interactions using drug discovery approach. A series of S100P peptides were designed and synthesized based on the interaction profiles of ER-EF hand protein complexes. Using the fold information and contact regions obtained in silico, 3D structures of ER-S100P protein complexes were reconstructed. These structures of ER best represent the conformational state sensed by the specific interacting partner. ER-S100P complex is distinct from CaM. The lack of the connective peptidic region between the EF hand pairs in S100P attributed to less interaction coverage than CaM. The identified ER conformation-sensing regions of the interacting EF hand proteins were used to develop a library of top peptidomimetics targeting the interfaces of ER-S100P interactions. We have evaluated their ability to block specific ER-S100 interactions inhibit cancer cell proliferation and ER-mediated transcription of target genes. The peptide P1 (GGGFIVFVG) derived from S100P 74-78 significantly decreased estrogen induced cell proliferation of MCF-7 cells, whereas, peptide P2 derived from S100P 74-81 (GGGFIVFVAAIG) did not. Pharmacophores from peptide P1-ER interactions was used to design high-affinity peptidomimetics and small molecules. The ensemble of ER-EF hand protein complexes generated by our integrated proteomics-assisted protein interaction profiling will shed light on the linger issue of hormone independent activation of ER at the molecular level and novel therapeutics targeting ER-S100P interactions, and warrants further studies with respect to its prognostic, predictive and potentially therapeutic value.
Book Synopsis Targeted Intracellular Drug Delivery by Receptor Mediated Endocytosis by : Padma V. Devarajan
Download or read book Targeted Intracellular Drug Delivery by Receptor Mediated Endocytosis written by Padma V. Devarajan and published by Springer Nature. This book was released on 2019-11-09 with total page 560 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book elaborates on drug delivery targeting via intracellular delivery, specifically through the Receptor Mediated Endocytosis (RME) approach, due to the involvement of cellular receptors in various grave diseases. Targeted delivery relies on two basic approaches, passive and active targeting. While passive targeting approaches have shown great promise, the improved selectivity achieved with active targeting approaches has resulted in significantly higher efficacy. Interestingly there are numerous strategies for active targeting, many of which are already highlighted in , Targeted Drug Delivery: Concepts and Applications. Nevertheless an exciting and practical strategy for active targeting, which could enable high intracellular delivery, is through exploitation of RME. Cells in the body express receptors to enable various physiological and biochemical processes. As a result, many of these receptors are overexpressed in pathological conditions, or newer receptors expressed due to defective cellular functioning. RME is based on exploitation of such receptors to achieve intracellular delivery. While targeted delivery can have manifold applications, in this book we focus on two major and challenging therapeutic areas; i) Cancer and ii) Infectious Diseases. Targeted Intracellular Drug Delivery by Receptor Medicated Endocytosis discusses the major receptors that are useful for targeted delivery for these afflictions. A major section of this book is dedicated to details regarding their occurrence and location, the recognition domain of the receptor, structure activity relationship of substrate /ligand for selective binding, ligands explored, antagonists for ligand binding and relevance of these aspects for therapy of cancer and infectious diseases. These facets are elucidated with the help of specific examples from academic research and also emphasize commercial products, wherever relevant. In vitro cellular models relied on for assessing receptor mediated cellular targeting and in vivo models depicting clinical efficacy are focused on in a separate section. Finally, we briefly discuss the regulatory and toxicity issues that may be associated specifically with the RME approach of intracellular drug delivery.
Book Synopsis Drug Discovery and Development by : Omboon Vallisuta
Download or read book Drug Discovery and Development written by Omboon Vallisuta and published by BoD – Books on Demand. This book was released on 2015-06-03 with total page 332 pages. Available in PDF, EPUB and Kindle. Book excerpt: It is very important for scientists all over the globe to enhance drug discovery research for better human health. This book demonstrates that various expertise are essential for drug discovery including synthetic or natural drugs, clinical pharmacology, receptor identification, drug metabolism, pharmacodynamic and pharmacokinetic research. The following 5 sections cover diverse chapter topics in drug discovery: Natural Products as Sources of Leading Molecules in Drug Discovery; Oncology and Drug Discovery; Receptors Involvement in Drug Discovery; Management and Development of Drugs against Infectious Diseases; Advanced Methodology.
Book Synopsis An Introduction to Medicinal Chemistry by : Graham L. Patrick
Download or read book An Introduction to Medicinal Chemistry written by Graham L. Patrick and published by Oxford University Press, USA. This book was released on 2013-01-10 with total page 814 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume provides an introduction to medicinal chemistry. It covers basic principles and background, and describes the general tactics and strategies involved in developing an effective drug.
Book Synopsis Gene Regulation and Therapeutics for Cancer by : Surinder K. Batra
Download or read book Gene Regulation and Therapeutics for Cancer written by Surinder K. Batra and published by CRC Press. This book was released on 2021-03-22 with total page 315 pages. Available in PDF, EPUB and Kindle. Book excerpt: Differential gene regulation and targeted therapy are the critical aspects of several cancers. This book covers specific gene regulation and targeted therapies in different malignancies. It offers a comprehensive assessment of the transcriptional dysregulation in cancer, and considers some examples of transcriptional regulators as definitive oncogenic drivers in solid tumors, followed by a brief discussion of transcriptional effectors of the programs they drive, and discusses its specific targets. Most targeted therapeutics developed to date have been directed against a limited set of oncogenic drivers, exemplified by those encoding cell surface or cytoplasmic kinases that function in intracellular signaling cascades.
Book Synopsis Fundamentals of Tissue Engineering and Regenerative Medicine by : Ulrich Meyer
Download or read book Fundamentals of Tissue Engineering and Regenerative Medicine written by Ulrich Meyer and published by Springer Science & Business Media. This book was released on 2009-02-11 with total page 1049 pages. Available in PDF, EPUB and Kindle. Book excerpt: "Fundamentals of Tissue Engineering and Regenerative Medicine" provides a complete overview of the state of the art in tissue engineering and regenerative medicine. Tissue engineering has grown tremendously during the past decade. Advances in genetic medicine and stem cell technology have significantly improved the potential to influence cell and tissue performance, and have recently expanded the field towards regenerative medicine. In recent years a number of approaches have been used routinely in daily clinical practice, others have been introduced in clinical studies, and multitudes are in the preclinical testing phase. Because of these developments, there is a need to provide comprehensive and detailed information for researchers and clinicians on this rapidly expanding field. This book offers, in a single volume, the prerequisites of a comprehensive understanding of tissue engineering and regenerative medicine. The book is conceptualized according to a didactic approach (general aspects: social, economic, and ethical considerations; basic biological aspects of regenerative medicine: stem cell medicine, biomolecules, genetic engineering; classic methods of tissue engineering: cell, tissue, organ culture; biotechnological issues: scaffolds; bioreactors, laboratory work; and an extended medical discipline oriented approach: review of clinical use in the various medical specialties). The content of the book, written in 68 chapters by the world’s leading research and clinical specialists in their discipline, represents therefore the recent intellect, experience, and state of this bio-medical field.
Book Synopsis Preclinical Development Handbook by : Shayne Cox Gad
Download or read book Preclinical Development Handbook written by Shayne Cox Gad and published by John Wiley & Sons. This book was released on 2008-03-21 with total page 1352 pages. Available in PDF, EPUB and Kindle. Book excerpt: A clear, straightforward resource to guide you through preclinical drug development Following this book's step-by-step guidance, you can successfully initiate and complete critical phases of preclinical drug development. The book serves as a basic, comprehensive reference to prioritizing and optimizing leads, dose formulation, ADME, pharmacokinetics, modeling, and regulations. This authoritative, easy-to-use resource covers all the issues that need to be considered and provides detailed instructions for current methods and techniques. Each chapter is written by one or more leading experts in the field. These authors, representing the many disciplines involved in preclinical toxicology screening and testing, give you the tools needed to apply an effective multidisciplinary approach. The editor has carefully reviewed all the chapters to ensure that each one is thorough, accurate, and clear. Among the key topics covered are: * Modeling and informatics in drug design * Bioanalytical chemistry * Absorption of drugs after oral administration * Transporter interactions in the ADME pathway of drugs * Metabolism kinetics * Mechanisms and consequences of drug-drug interactions Each chapter offers a full exploration of problems that may be encountered and their solutions. The authors also set forth the limitations of various methods and techniques used in determining the safety and efficacy of a drug during the preclinical stage. This publication should be readily accessible to all pharmaceutical scientists involved in preclinical testing, enabling them to perform and document preclinical safety tests to meet all FDA requirements before clinical trials may begin.
Download or read book Pharmacogenomics written by Julio Licinio and published by John Wiley & Sons. This book was released on 2009-07-30 with total page 599 pages. Available in PDF, EPUB and Kindle. Book excerpt: This work represents the first comprehensive publication in the innovative field of pharmacogenomics, a field which is set to revolutionize pharmaceutical research. In addition to renowned editors, the list of contributors is a "who-is-who" in the field. Broad coverage of all aspects of pharmacogenomics with a full presentation of applications to disease conditions is featured. Anyone involved in pharmaceutical research and drug development needs this book to keep up with this new and revolutionary approach
Book Synopsis Cyclized Helical Peptides by : Zigang Li
Download or read book Cyclized Helical Peptides written by Zigang Li and published by John Wiley & Sons. This book was released on 2021-08-23 with total page 242 pages. Available in PDF, EPUB and Kindle. Book excerpt: An important and timely guide to the progress being made on constrained helical peptides Constraint helical peptides have emerged as a solution to target previously undruggable protein-protein interactions, which feature large and complex surfaces. Cyclized Helical Peptides: Synthesis, Properties and Therapeutic Applications offers a review of the most current methodologies of constructing constrained helices. The authors noted experts on the topic include the information on the fundamental features of cyclized helical peptides and discuss their limitations. The book summarizes and explores the effects of chemical methods constructing helical peptides on helicity, binding affinity, cell penetration, and nonspecific toxicity. The book examines the therapeutic applications of the constraint helices and includes comparison with existing small molecule modulators or antibodies. Designed as a useful resource for both those outside and inside the field. Those new to the field will find a comprehensive introduction to cyclized helical peptide and those inside the field will find a deeper understanding of the topic. This important book: Offers a practical introduction to constrained helical peptides Includes all aspects of constrained helical peptides Includes information on the most recent methods that have emerged Presents a guide to help solve practical problems in the field Written for academics, pharmaceutical professional, Cyclized Helical Peptides is a comprehensive guide to the developments of constrained helical peptides.
Book Synopsis Growth Hormone Deficiency by : Laurie E. Cohen
Download or read book Growth Hormone Deficiency written by Laurie E. Cohen and published by Springer. This book was released on 2016-07-04 with total page 232 pages. Available in PDF, EPUB and Kindle. Book excerpt: Providing the most current information on the function of human growth hormone (GH) and the consequences of its deficiency, this practical yet comprehensive text is divided into three sections. Part one describes the mechanisms of GH secretion and action, including the physiology of GH and its regulation by sex steroids and thyroid hormones, the effects of both under nutrition and obesity on GH secretion, and the metabolic effects of human recombinant GH therapy. The second section covers diagnostic strategies and tests for GH deficiency in both children and adults, including MRI of the pituitary. The final section describes the different etiologies of GH deficiency, from molecular mechanisms and gene abnormalities to cranial radiation and traumatic brain injury, along with syndromes related to this deficiency. Presenting underlying mechanisms and pathologies, as well as diagnostic methods, Growth Hormone Deficiency will provide the most up-to-date essential information and evidence on this condition for the clinical endocrinologist.
Book Synopsis Drug Resistance in Leukemia & by : Gert-Jan L. Kaspers
Download or read book Drug Resistance in Leukemia & written by Gert-Jan L. Kaspers and published by CRC Press. This book was released on 1993-01-01 with total page 458 pages. Available in PDF, EPUB and Kindle. Book excerpt: The last ten years have seen the publication of a vast amount of data regarding cellular resistance to drugs in cancer cells. Recent studies have demonstrated that drug resistance assays appear to be predictive of clinical response and suggest that clinicians should now be considering the potential applications of these assays in the treatment of patients with hematological neoplasms. This collection of papers from the International Symposium on the Clinical Value of Drug Resistance Assays in Leukemia and Lymphoma, Amsterdam, 1992, provides a state-of-the-art discussion on drug resistance assays and their role in the design and individualization of treatment protocols.
Book Synopsis Chemometrics and Cheminformatics in Aquatic Toxicology by : Kunal Roy
Download or read book Chemometrics and Cheminformatics in Aquatic Toxicology written by Kunal Roy and published by John Wiley & Sons. This book was released on 2022-01-06 with total page 596 pages. Available in PDF, EPUB and Kindle. Book excerpt: CHEMOMETRICS AND CHEMINFORMATICS IN AQUATIC TOXICOLOGY Explore chemometric and cheminformatic techniques and tools in aquatic toxicology Chemometrics and Cheminformatics in Aquatic Toxicology delivers an exploration of the existing and emerging problems of contamination of the aquatic environment through various metal and organic pollutants, including industrial chemicals, pharmaceuticals, cosmetics, biocides, nanomaterials, pesticides, surfactants, dyes, and more. The book discusses different chemometric and cheminformatic tools for non-experts and their application to the analysis and modeling of toxicity data of chemicals to various aquatic organisms. You’ll learn about a variety of aquatic toxicity databases and chemometric software tools and webservers as well as practical examples of model development, including illustrations. You’ll also find case studies and literature reports to round out your understanding of the subject. Finally, you’ll learn about tools and protocols including machine learning, data mining, and QSAR and ligand-based chemical design methods. Readers will also benefit from the inclusion of: A thorough introduction to chemometric and cheminformatic tools and techniques, including machine learning and data mining An exploration of aquatic toxicity databases, chemometric software tools, and webservers Practical examples and case studies to highlight and illustrate the concepts contained within the book A concise treatment of chemometric and cheminformatic tools and their application to the analysis and modeling of toxicity data Perfect for researchers and students in chemistry and the environmental and pharmaceutical sciences, Chemometrics and Cheminformatics in Aquatic Toxicology will also earn a place in the libraries of professionals in the chemical industry and regulators whose work involves chemometrics.
Book Synopsis Metastasis of Breast Cancer by : R.E. Mansel
Download or read book Metastasis of Breast Cancer written by R.E. Mansel and published by Springer Science & Business Media. This book was released on 2007-06-17 with total page 439 pages. Available in PDF, EPUB and Kindle. Book excerpt: Written by experts in the subject area, the book covers a broad range of topics in the metastasis of breast cancer, from genetics, biology to clinical management. Main topics include genetic control, biology, growth factors, cell adhesion, cell motility and invasion, natures of bone metastasis, sentinel node therapies, hormonal links, new biomarkers and detection of micrometastasis and diagnosis. This timely book also covers the current treatment options.
Book Synopsis Molecular Oncology by : Frank Joseph Rauscher (III)
Download or read book Molecular Oncology written by Frank Joseph Rauscher (III) and published by Cambridge University Press. This book was released on 2014 with total page 985 pages. Available in PDF, EPUB and Kindle. Book excerpt: Reviews the origins of molecular oncology, including technologies for cancer analysis, key pathways in human malignancies, and available pharmacologic therapies.
Book Synopsis Nuclear Receptors as Drug Targets by : Eckhard Ottow
Download or read book Nuclear Receptors as Drug Targets written by Eckhard Ottow and published by Wiley-VCH. This book was released on 2008-10-13 with total page 522 pages. Available in PDF, EPUB and Kindle. Book excerpt: Edited by two experts working at the pioneering pharmaceutical company and major global player in hormone-derived drugs, this handbook and reference systematically treats the drug development aspects of all human nuclear receptors, including recently characterized receptors such as PPAR, FXR and LXR. Authors from leading pharmaceutical companies around the world present examples and real-life data from their own work.
Download or read book Prostate Cancer written by Roger S. Kirby and published by CRC Press. This book was released on 2006-01-13 with total page 1104 pages. Available in PDF, EPUB and Kindle. Book excerpt: Written by over 250 of the world's leading urologists and uro-oncologists from the USA, Canada, UK, Austria, Belgium, Finland, France, Germany, Ireland, Italy, the Netherlands and Singapore, who tackle prostate cancer on a daily basis, this comprehensive and fully up-to-date illustrated text reference covers the etiology, pathophysiology, diagnosis, management and treatment of early and advanced prostate cancer.
