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Third Generation EGFR Inhibitors

Third Generation EGFR Inhibitors Book
Author : Harun M. Patel,Rahul Pawara,S. J. Surana
Publisher : Elsevier
Release : 2019-03-15
ISBN : 9780081026618
Language : En, Es, Fr & De

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Book Description :

EGFR inhibitors are useful tools in cancer therapeutics, but resistance to the first generations have significantly increased, meaning a new generation of improved inhibitors are needed with better efficacy and lower toxicity. Third Generation EGFR Inhibitors: Overcoming EGFR Resistance and Toxicity Problems reviews current issues relating to the design of reversible and irreversible third generation EGFR inhibitors, highlighting the types of mutation responsible for resistance, and providing different chemical starting points for researchers to optimize and develop in designing the next generation of drugs. Beginning with an introduction to EGFR inhibitors and a review of inhibitors currently approved or in clinical trials, the book goes on to discuss current approaches in the development of both covalent irreversible and covalent reversible EGFR Inhibitors. Mechanisms of resistance to third generation inhibitors, and discovery of fourth generation allosteric C797S inhibitors are then explored before a discussion of potential future trends. Third Generation EGFR Inhibitors: Overcoming EGFR Resistance and Toxicity Problems is a guide for medicinal chemists, drug developer, and researchers investigating cancer therapeutics, supporting them in the design and development of improved analogues to overcome the problems of resistance and toxicity associated with third generation EGFR inhibitors. Includes full synthetic schemes of all approved and in-trial third generation inhibitors Highlights the emergence of fourth generation EGFR inhibitors and looks at how they may be able to overcome the constraints of third generation compounds Provides a structural correlation of third and fourth generation EGFR inhibitors and reviews both their design strategies and typical anticancer activity

Third Generation EGFR Inhibitors

Third Generation EGFR Inhibitors Book
Author : Harun M. Patel,Rahul Pawara,Sanjay J. Surana
Publisher : Elsevier
Release : 2018-11-27
ISBN : 0081026625
Language : En, Es, Fr & De

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Book Description :

Third Generation EGFR Inhibitors: Overcoming EGFR Resistance and Toxicity Problems reviews current issues relating to the design of reversible and irreversible third generation EGFR inhibitors, highlighting the types of mutation responsible for resistance, and providing different chemical starting points for researchers to optimize and develop in designing the next generation of drugs. Beginning with an introduction to EGFR inhibitors and a review of inhibitors currently approved or in clinical trials, the book goes on to discuss current approaches in the development of both covalent irreversible and covalent reversible EGFR Inhibitors. In addition, mechanisms of resistance to third generation inhibitors, and discovery of fourth generation allosteric C797S inhibitors are explored before a discussion of potential future trends. This comprehensive coverage of the design and development of improved analogues to overcome the problems of resistance and toxicity associated with third generation EGFR inhibitors makes Third Generation EGFR Inhibitors a crucial resource for medicinal chemists, drug developers, and researchers investigating cancer therapeutics. Includes full synthetic schemes of all approved and in-trial third generation inhibitors Highlights the emergence of fourth generation EGFR inhibitors and the possibilities of them overcoming constraints of third generation compounds Provides a structural correlation of third and fourth generation EGFR inhibitors, reviewing both their design strategies and typical anticancer activity

Acquired Resistance to Targeted Therapy in EGFR mutant Lung Adenocarcinoma

Acquired Resistance to Targeted Therapy in EGFR mutant Lung Adenocarcinoma Book
Author : Caroline Amalia Nebhan
Publisher : Unknown
Release : 2014
ISBN : 0987650XXX
Language : En, Es, Fr & De

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Book Description :

Download Acquired Resistance to Targeted Therapy in EGFR mutant Lung Adenocarcinoma book written by Caroline Amalia Nebhan, available in PDF, EPUB, and Kindle, or read full book online anywhere and anytime. Compatible with any devices.

Overcoming Resistance to EGFR Inhibitors in EGFR Mutant NSCLC

Overcoming Resistance to EGFR Inhibitors in EGFR Mutant NSCLC Book
Author : Anthony Faber
Publisher : Academic Press
Release : 2021-03-15
ISBN : 9780128228333
Language : En, Es, Fr & De

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Book Description :

Overcoming Resistance to EGFR Inhibitors in EGFR Mutant NSCLC, Volume 17 presents updated information on how EGFR mutant lung cancers evolve to evade EGFR inhibitors, clinical strategies that identify these mechanisms, and how to implement newer therapeutic strategies to combat resistance and improve patient survival. As resistance to EGFR inhibitors is often through re-activation of MEK/ERK and PI3K pathways, or through loss of cell death responses, there is much overlap with resistance to targeted therapies in other paradigms, such as BRAF inhibitors in BRAF mutant melanoma, and HER2 inhibitors in HER2 amplified breast cancer. This book is a valuable resource for cancer researchers, clinicians, graduate students and other members of the biomedical field who are interested in promising treatments for lung cancer. Presents historical context on how NSCLC and SCLC has been treated, with an emphasis on NSCLC and how the concept of EGFR inhibitors has been implemented Discusses critical resistant mechanisms seen in the clinic to 1st, 2nd and 3rd generation EGFR inhibitors Encompasses the current state of affairs in clinical trials to address resistance

Frontiers in Anti Cancer Drug Discovery Volume 11

Frontiers in Anti Cancer Drug Discovery  Volume 11 Book
Author : Atta-ur-Rahman ,Muhammad Iqbal Choudhary
Publisher : Bentham Science Publishers
Release : 2020-09-01
ISBN : 9811422125
Language : En, Es, Fr & De

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Book Description :

Frontiers in Anti-Cancer Drug Discovery is a book series devoted to publishing the latest advances in anti-cancer drug design and discovery. In each volume, eminent scientists contribute reviews relevant to 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 book series should prove to be of interest to all pharmaceutical scientists involved in research in anti-cancer drug design and discovery. The book 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 eleventh volume of the series focuses on reviews on targeted therapies and drug delivery systems. This volume covers the following topics: - PI3K/Akt/mTOR Pathway in Acute Lymphoblastic Leukemia Targeted Therapies - Polymeric Nanomedicines in Treatment of Breast Cancer: Review of Contemporary Research - Treatment of Lung Cancer in the New Era - Oral Administration of Cancer Chemotherapeutics Exploiting Self-Nanoemulsifying Drug Delivery System: Recent Progress and Application - Targeting Approaches for the Diagnosis and Treatment of Cancer.

A Beginner s Guide to Targeted Cancer Treatments

A Beginner s Guide to Targeted Cancer Treatments Book
Author : Elaine Vickers
Publisher : John Wiley & Sons
Release : 2018-05-08
ISBN : 1119126835
Language : En, Es, Fr & De

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Book Description :

The accessible guide to the principles behind new, more targeted drug treatments for cancer Written for anyone who encounters cancer patients, cancer data or cancer terminology, but have no more than a passing knowledge of cell biology. A Beginner's Guide to Targeted Cancer Treatments provides an understanding of how cancer works and the many new treatments available. Using over 100 original illustrations, this accessible handbook covers the biology and mechanisms behind a huge range of targeted drug treatments, including many new immunotherapies. Dr Vickers translates a complex and often overwhelming topic into something digestible and easily understood. She also explains what cancer is, how it behaves and how our understanding of cancer has changed in recent years. Each chapter takes the reader through how new cancer drugs work and their benefits and limitations. With the help of this book, readers will be able to better understand more complex, in-depth articles in journals and books and develop their knowledge. This vital resource: Offers the latest insights into cancer biology Provides a broad understanding of how targeted cancer treatments work Describes many of the new immunotherapy approaches to cancer treatment, such as checkpoint inhibitors and CAR-modified T cells Helps readers feel confident discussing treatment options with colleagues and patients Provides an overview of which treatments are relevant to each of the most common solid tumours and haematological cancers, and the rationale behind them Demystifies the jargon – terms such as the EMT, cancer stem cells, monoclonal antibodies, kinase inhibitors, angiogenesis inhibitors etc. Explains the resistance mechanisms to many new treatments, including issues such as the way cancer cells diversify and evolve and the complex environment in which they live

Clinical Applications of Circulating Tumor DNA Analysis

Clinical Applications of Circulating Tumor DNA Analysis Book
Author : Jacob John Chabon
Publisher : Unknown
Release : 2018
ISBN : 0987650XXX
Language : En, Es, Fr & De

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Book Description :

Circulating tumor DNA (ctDNA) represents an exquisitely specific biomarker due to the fact that tumors harbor somatic mutations that are not present in other cell-types in the body. We begin with a review of the existing methodologies and applications of ctDNA, highlighting studies that illustrate the diverse clinical utility of ctDNA. Next we focus on a method for ctDNA detection developed by our lab called Cancer Personalized Profiling by Deep Sequencing (CAPP-Seq). CAPP-Seq is a targeted next-generation sequencing approach for ctDNA detection that does not require patient specific optimization and is amenable to a variety of cancer types. We first employ CAPP-Seq based ctDNA analysis to study resistance mechanisms in 43 non-small cell lung cancer (NSCLC) patients treated with the third-generation EGFR tyrosine kinase inhibitor (TKI) rociletinib. Multiple resistance mechanisms were present in 46% of patients after treatment with front-line EGFR TKIs, representing a previously unrecognized high frequency of molecular heterogeneity of resistance mechanisms following treatment with EGFR TKIs. Rociletinib resistance recurrently involved MET, EGFR, PIK3CA, ERRB2, KRAS and RB1. We observed a novel EGFR L798I mutation, and EGFR C797S, which arises in ~1/3 of patients treated with another third-generation inhibitor (osimertinib), was observed in only one patient. Increased MET copy number was the most frequent rociletinib resistance mechanism and patients with multiple pre-existing mechanisms (i.e. T790M and MET) experienced inferior responses. Congruently, rociletinib-resistant xenografts developed MET amplification that could be overcome with the MET inhibitor crizotinib. These results underscore the importance of tumor heterogeneity in NSCLC and the clinical utility of ctDNA-based resistance mechanism assessment. Next we apply ctDNA analysis to a less common cancer type, Leiomyosarcoma (LMS). LMS is a soft-tissue sarcoma that represents a tumor type with a heterogeneous spectrum of genomic abnormalities. As such, targeting hotspot mutations in a narrow genomic region for ctDNA detection is suboptimal. For this reason we developed a combinatorial approach that integrates different sequencing protocols for the orthogonal detection of single nucleotide variants (SNVs), small indels and copy number alterations (CNAs) in ctDNA. We employed CAPP-Seq for the analysis of SNVs and indels, together with a genome-wide interrogation of CNAs by Genome Representation Profiling (GRP). We profiled 28 longitudinal plasma samples and 25 tumor specimens from 7 patients with LMS. We detected ctDNA in 6 of 7 of these patients with > 98% specificity for mutant allele fractions down to a level of 0.01%. We found that ctDNA quantitation by CAPP-Seq and GRP was highly concordant, and the combination of these methods allows for more comprehensive monitoring of ctDNA by profiling a wide spectrum of tumor-specific markers. Through analysis of multiple tumor specimens from individual patients we observed evidence for both spatial and temporal tumor heterogeneity that was reflected in ctDNA profiles. This strategy allows for comprehensive monitoring of a broad spectrum of tumor-specific markers in plasma and may be clinically useful not only in LMS but in other tumor types that lack recurrent genomic alterations.

Chemoinformatics Approaches to Structure and Ligand Based Drug Design

Chemoinformatics Approaches to Structure  and Ligand Based Drug Design Book
Author : Adriano D. Andricopulo,Leonardo L. G. Ferreira
Publisher : Frontiers Media SA
Release : 2019-02-05
ISBN : 2889457443
Language : En, Es, Fr & De

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Book Description :

Chemoinformatics is paramount to current drug discovery. Structure- and ligand-based drug design strategies have been used to uncover hidden patterns in large amounts of data, and to disclose the molecular aspects underlying ligand-receptor interactions. This Research Topic aims to share with a broad audience the most recent trends in the use of chemoinformatics in drug design. To that end, experts in all areas of drug discovery have made their knowledge available through a series of articles that report state-of-the-art approaches. Readers are provided with outstanding contributions focusing on a wide variety of topics which will be of great value to those interested in the many different and exciting facets of drug design.

Targeted Therapies for Lung Cancer

Targeted Therapies for Lung Cancer Book
Author : Ravi Salgia
Publisher : Springer
Release : 2019-06-26
ISBN : 3030178323
Language : En, Es, Fr & De

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Book Description :

This book contextualizes translational research and provides an up to date progress report on therapies that are currently being targeted in lung cancer. It is now well established that there is tremendous heterogeneity among cancer cells both at the inter- and intra-tumoral level. Further, a growing body of work highlights the importance of targeted therapies and personalized medicine in treating cancer patients. In contrast to conventional therapies that are typically administered to the average patient regardless of the patient’s genotype, targeted therapies are tailored to patients with specific traits. Nonetheless, such genetic changes can be disease-specific and/or target specific; thus, the book addresses these issues manifested in the somatically acquired genetic changes of the targeted gene. Each chapter is written by a leading medical oncologist who specializes in thoracic oncology and is devoted to a particular target in a specific indication. Contributors provide an in-depth review of the literature covering the mechanisms underlying signaling, potential cross talk between the target and downstream signaling, and potential emergence of drug resistance.

Proteinkinase Inhibitors

Proteinkinase Inhibitors Book
Author : Stefan Laufer
Publisher : Springer Nature
Release : 2021-09-25
ISBN : 3030681807
Language : En, Es, Fr & De

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Book Description :

Download Proteinkinase Inhibitors book written by Stefan Laufer, available in PDF, EPUB, and Kindle, or read full book online anywhere and anytime. Compatible with any devices.

AACR 2016 Abstracts 1 2696

AACR 2016  Abstracts 1 2696 Book
Author : American Association for Cancer Research (AACR)
Publisher : CTI Meeting Technology
Release : 2016-03-28
ISBN : 0987650XXX
Language : En, Es, Fr & De

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Book Description :

The AACR Annual Meeting is a must-attend event for cancer researchers and the broader cancer community. This year's theme, "Delivering Cures Through Cancer Science," reinforces the inextricable link between research and advances in patient care. The theme will be evident throughout the meeting as the latest, most exciting discoveries are presented in every area of cancer research. There will be a number of presentations that include exciting new data from cutting-edge clinical trials as well as companion presentations that spotlight the science behind the trials and implications for delivering improved care to patients. This book contains abstracts 1-2696 presented on April 17-18, 2016, at the AACR Annual Meeting.

AACR 2018 Proceedings Abstracts 1 3027

AACR 2018 Proceedings  Abstracts 1 3027 Book
Author : American Association for Cancer Research
Publisher : CTI Meeting Technology
Release : 2018-04-10
ISBN : 1370257430
Language : En, Es, Fr & De

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Book Description :

Download AACR 2018 Proceedings Abstracts 1 3027 book written by American Association for Cancer Research, available in PDF, EPUB, and Kindle, or read full book online anywhere and anytime. Compatible with any devices.

Molecular Targeted Therapy of Lung Cancer

Molecular Targeted Therapy of Lung Cancer Book
Author : Yuichi Takiguchi
Publisher : Springer
Release : 2017-01-24
ISBN : 9811020027
Language : En, Es, Fr & De

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Book Description :

This book discusses the latest molecular targeted therapy of lung cancer including its evaluation and future directions. It clearly illustrates the initial dramatic effectiveness of molecular targeted therapy, recurrence of the disease, overcoming the wide variety of resistance mechanisms using new-generation molecular targeted agents and potential novel approaches. It also outlines the increasing necessity for new diagnostic technology and strategies for managing different adverse effects and novel methods for evaluating effectiveness and safety. Edited and authored by opinion leaders, Molecular Targeted Therapy of Lung Cancer provides a comprehensive overview of the disease and its treatments. It is a valuable resource for graduate students, post-doctoral fellows and faculty staff, as well as researchers involved in clinical and translational research on lung cancer, helping promote new ideas for further advances.

Kinase Drug Discovery

Kinase Drug Discovery Book
Author : Richard A. Ward,Frederick W. Goldberg
Publisher : Royal Society of Chemistry
Release : 2018-10-10
ISBN : 1788010833
Language : En, Es, Fr & De

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Book Description :

Kinase inhibition remains an area of significant interest, and growing importance, across academia and the pharmaceutical industry. There are now many marketed drugs that target kinases and a significant number of compounds are currently in various stages of clinical development. This book is a forward-looking analysis of a number of key areas for kinase inhibition in the coming years.

Next Generation Kinase Inhibitors

Next Generation Kinase Inhibitors Book
Author : Paul Shapiro
Publisher : Springer Nature
Release : 2020-07-14
ISBN : 3030482839
Language : En, Es, Fr & De

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Book Description :

Protein kinases are fascinating enzymes that maintain the proper function of nearly every task performed by the cells of the human body. By extracting a phosphate from the energy molecule ATP and linking it to another protein, protein kinases alter the structure and ultimate function of other proteins. In this way, protein kinases help monitor the extracellular environment and integrate signaling cues that, for the most part, are beneficial for human health and survival. However, protein kinases are often dysregulated and responsible for the initiation and progression of many types of cancers, inflammatory disorders, and other diseases. Thus, decades of research have revealed much about how protein kinases are regulated and approaches to inhibit these enzymes to treat disease. However, nearly 30 years since the identification of the first clinically beneficial small molecule protein kinase inhibitor, there are only a few examples where these drugs provide sustained and durable patient responses. The goal of this book is to provide biomedical scientists, graduate, and professional degree students insight into different approaches using small molecules to block specific protein kinase functions that promote disease.

Resistance to Anti Cancer Therapeutics Targeting Receptor Tyrosine Kinases and Downstream Pathways

Resistance to Anti Cancer Therapeutics Targeting Receptor Tyrosine Kinases and Downstream Pathways Book
Author : Yosef Yarden,Moshe Elkabets
Publisher : Springer
Release : 2018-03-28
ISBN : 3319679325
Language : En, Es, Fr & De

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Book Description :

This volume comprehensively covers the multiplicity and diversity of mechanisms underlying patient resistance to currently approved anti-cancer drugs, including tyrosine kinase inhibitors and monoclonal antibodies, blockers of growth factor receptors and their downstream pathways, which play essential functions in cancer progression. Each chapter will cover a specific group of targets and the cognate drugs, along with molecular modes of innate and evolving resistance.

Molecular Medicine

Molecular Medicine Book
Author : Jens Kurreck,Cy Aaron Stein
Publisher : John Wiley & Sons
Release : 2016-02-16
ISBN : 3527331891
Language : En, Es, Fr & De

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Book Description :

Easy to read, yet comprehensive, this is the perfect introduction into the molecular basis of disease and the novel treatment options that have become available. The authors, Jens Kurreck and Cy Stein, have both long-standing teaching experience on the subject, one from a biologist's angle, the other with a medical background. Together, they have produced a modern textbook for courses in Molecular Medicine that incorporates modules from immunology to signaling, from virology to gene therapy, and the latest development in personalized medicine.

Virtual Drug Design

Virtual Drug Design Book
Author : Daniela Schuster,Honglin Li
Publisher : Frontiers Media SA
Release : 2020-01-13
ISBN : 2889633594
Language : En, Es, Fr & De

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Book Description :

In the current drug research environment in academia and industry, cheminformatics and virtual screening methods are well established and integrated tools. Computational tools are used to predict a compound’s 3D structure, the 3D structure and function of a pharmacological target, ligand-target interactions, binding energies, and other factors essential for a successful drug. This includes molecular properties such as solubility, logP value, susceptibility to metabolism, cell permeation, blood brain barrier permeation, interaction with drug transporters and potential off-target effects. Given that approximately 40 million unique compounds are readily available for purchase, such computational modeling and filtering tools are essential to support the drug discovery and development process. The aim of all these calculations is to focus experimental efforts on the most promising candidates and exclude problematic compounds early in the project. In this Research Topic on virtual activity predictions, we cover several aspects of this research area such as historical perspectives, data sources, ligand treatment, virtual screening methods, hit list handling and filtering.

Lung Cancer and Personalized Medicine

Lung Cancer and Personalized Medicine Book
Author : Aamir Ahmad,Shirish Gadgeel
Publisher : Springer
Release : 2015-12-14
ISBN : 3319242237
Language : En, Es, Fr & De

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Book Description :

This, the first of two volumes on personalized medicine in lung cancer, touches on the core issues related to the understanding of lung cancer—statistics and epidemiology of lung cancer—along with the incidence of lung cancer in non-smokers. A major focus of this volume is the state of current therapies against lung cancer—immune, targeted therapies against EGFR TKIs, KRAS, ALK, angiogenesis; the associated challenges, especially resistance mechanisms; and recent progress in targeted drug development based on metal chemistry. Chapters are written by some of the leading experts in the field, who provide a better understanding of lung cancer, the factors that make it lethal, and current research focused on developing personalized treatment plans. With a unique mix of topics, this volume summarizes the current state-of-knowledge on lung cancer and the available therapies.

Precision Medicine in Oncology

Precision Medicine in Oncology Book
Author : Bulent Aydogan,James A. Radosevich
Publisher : John Wiley & Sons
Release : 2020-09-23
ISBN : 1119432448
Language : En, Es, Fr & De

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Book Description :

A FRESH EXAMINATION OF PRECISION MEDICINE'S INCREASINGLY PROMINENT ROLE IN THE FIELD OF ONCOLOGY Precision medicine takes into account each patient's specific characteristics and requirements to arrive at treatment plans that are optimized towards the best possible outcome. As the field of oncology continues to advance, this tailored approach is becoming more and more prevalent, channelling data on genomics, proteomics, metabolomics and other areas into new and innovative methods of practice. Precision Medicine in Oncology draws together the essential research driving the field forward, providing oncology clinicians and trainees alike with an illuminating overview of the technology and thinking behind the breakthroughs currently being made. Topics covered include: Biologically-guided radiation therapy Informatics for precision medicine Molecular imaging Biomarkers for treatment assessment Big data Nanoplatforms Casting a spotlight on this emerging knowledge base and its impact upon the management of tumors, Precision Medicine in Oncology opens up new possibilities and ways of working – not only for oncologists, but also for molecular biologists, radiologists, medical geneticists, and others.