Resistance To Tyrosine Kinase Inhibitors

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Resistance to Tyrosine Kinase Inhibitors

Author : Daniele Focosi
Publisher : Springer
Page : 188 pages
File Size : 54,7 Mb
Release : 2016-11-07
Category : Medical
ISBN : 9783319460918

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Resistance to Tyrosine Kinase Inhibitors by Daniele Focosi Pdf

The volume will serve as a primer on tyrosine kinase signaling and its importance in cancer. The volume will first introduce the common denominators of small-molecule and antibody-derived inhibitors, as well as the general phenomenon of resistance. The volume will then detail resistance to the most commonly used classes of tyrosine kinase inhibitors, and will focus specific chapters on resistance to BCR-ABL1, FLT3, angiokinase family members, and ALK inhibitors.

Protein Tyrosine Kinases

Author : Doriano Fabbro,Frank McCormick
Publisher : Springer Science & Business Media
Page : 599 pages
File Size : 50,6 Mb
Release : 2007-11-13
Category : Science
ISBN : 9781592599622

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Protein Tyrosine Kinases by Doriano Fabbro,Frank McCormick Pdf

Leading researchers, from the Novartis group that pioneered Gleevec/GlivecTM and around the world, comprehensively survey the state of the art in the drug discovery processes (bio- and chemoinformatics, structural biology, profiling, generation of resistance, etc.) aimed at generating PTK inhibitors for the treatment of various diseases, including cancer. Highlights include a discussion of the rationale and the progress made towards generating "selective" low molecular-weight kinase inhibitors; an analysis of the normal function, role in disease, and application of platelet-derived growth factor antagonists; and a summary of the factors involved in successful structure-based drug design. Additional chapters address the advantages and disadvantages of in vivo preclinical models for testing protein kinase inhibitors with antitumor activity and the utility of different methods in the drug discovery and development process for determining "on-target" vs "off-target" effects of kinase inhibitors.

Tyrosine Kinases as Druggable Targets in Cancer

Author : Huan Ren
Publisher : BoD – Books on Demand
Page : 136 pages
File Size : 53,6 Mb
Release : 2019-09-25
Category : Medical
ISBN : 9781789848083

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Tyrosine Kinases as Druggable Targets in Cancer by Huan Ren Pdf

Protein tyrosine kinase (PTK) deregulation contributes to growth of cancer and many other diseases. The development of small-molecule tyrosine kinase inhibitors (TKIs) that target the deregulated PTKs, such as epidermal growth factor receptor (EGFR) in non-small-cell lung cancer (NSCLC) and Bcr-ABL in chronic myeloid leukemia (CML), has revolutionized disease management. In this book, we examine a few aspects of PTKs and cancer, considering efficacy, predictive markers to therapeutic response, limitations, and future directions in TKI treatment. In this rapidly evolving field, overcoming therapeutic resistance is most challenging, and multi-targeting directs the next-generation TKIs and combination therapy as ongoing strategies in cancer treatment.

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

Author : Yosef Yarden,Moshe Elkabets
Publisher : Springer
Page : 242 pages
File Size : 54,7 Mb
Release : 2018-03-28
Category : Medical
ISBN : 9783319679327

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Resistance to Anti-Cancer Therapeutics Targeting Receptor Tyrosine Kinases and Downstream Pathways by Yosef Yarden,Moshe Elkabets Pdf

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.

Protein Kinase Inhibitors as Sensitizing Agents for Chemotherapy

Author : Anonim
Publisher : Academic Press
Page : 292 pages
File Size : 40,9 Mb
Release : 2018-11-21
Category : Medical
ISBN : 9780128127384

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Protein Kinase Inhibitors as Sensitizing Agents for Chemotherapy by Anonim Pdf

Tyrosine Kinase Inhibitors as Sensitizing Agents for Chemotherapy, the fourth volume in the Cancer Sensitizing Agents for Chemotherapy Series, focuses on strategic combination therapies that involve a variety of tyrosine kinase inhibitors working together to overcome multi-drug resistance in cancer cells. The book discusses several tyrosine kinase inhibitors that have been used as sensitizing agents, such as EGFR, BCR-ABL, ALK and BRAF. In each chapter, readers will find comprehensive knowledge on the inhibitor and its action, including its biochemical, genetic, and molecular mechanisms' emphases. This book is a valuable source for oncologists, cancer researchers and those interested in applying new sensitizing agents to their research in clinical practice and in trials. Summarizes the sensitizing role of some tyrosine kinase inhibitors in existing research Brings recent findings in several cancer types, both experimental and clinically, with a particular emphases on underlying biochemical, genetic, and molecular mechanisms Provides an updated and comprehensive knowledge regarding the field of combinational cancer treatment

Tyrosine Kinase Inhibitors—Advances in Research and Application: 2012 Edition

Author : Anonim
Publisher : ScholarlyEditions
Page : 66 pages
File Size : 50,6 Mb
Release : 2012-12-26
Category : Medical
ISBN : 9781481611619

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Tyrosine Kinase Inhibitors—Advances in Research and Application: 2012 Edition by Anonim Pdf

Tyrosine Kinase Inhibitors—Advances in Research and Application: 2012 Edition is a ScholarlyBrief™ that delivers timely, authoritative, comprehensive, and specialized information about Tyrosine Kinase Inhibitors in a concise format. The editors have built Tyrosine Kinase Inhibitors—Advances in Research and Application: 2012 Edition on the vast information databases of ScholarlyNews.™ You can expect the information about Tyrosine Kinase Inhibitors in this eBook to be deeper than what you can access anywhere else, as well as consistently reliable, authoritative, informed, and relevant. The content of Tyrosine Kinase Inhibitors—Advances in Research and Application: 2012 Edition has been produced by the world’s leading scientists, engineers, analysts, research institutions, and companies. All of the content is from peer-reviewed sources, and all of it is written, assembled, and edited by the editors at ScholarlyEditions™ and available exclusively from us. You now have a source you can cite with authority, confidence, and credibility. More information is available at http://www.ScholarlyEditions.com/.

Primary and Acquired Resistance in Lung Cancer

Author : Rossella Bruno,Michele Simbolo,Iacopo Petrini
Publisher : Frontiers Media SA
Page : 116 pages
File Size : 42,5 Mb
Release : 2023-11-23
Category : Medical
ISBN : 9782832539392

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Primary and Acquired Resistance in Lung Cancer by Rossella Bruno,Michele Simbolo,Iacopo Petrini Pdf

Lung cancer is one of the leading causes of cancer-related death worldwide with a prevalence of advanced stage in up to 70% of cases and a five-year survival reached in only 5-10% of cases. Targeted therapies and immunotherapy have greatly improved the management of patients with advanced non-small cell lung cancer (NSCLC), particularly adenocarcinoma, and current diagnostic algorithms are based on the molecular analysis of several biomarkers necessary to tailor therapy. In detail, patients harboring sensitive driver alterations within the oncogenes EGFR, BRAF, ALK, ROS1, RET and NTRK1/2/3 can be treated with approved kinase inhibitors (KIs). In addition, drugs against MET, KRAS G12C and other markers are providing interesting results across different clinical trials. Targeted therapies have greatly improved therapeutic options for NSCLC, but resistance inevitably occurs usually after one year of treatment and some patients, although harboring sensitive alterations, never respond to treatment.

The Treatment of Myeloid Malignancies with Kinase Inhibitors, An Issue of Hematology/Oncology Clinics of North America, E-Book

Author : Ann Mullally
Publisher : Elsevier Health Sciences
Page : 128 pages
File Size : 53,5 Mb
Release : 2017-07-14
Category : Medical
ISBN : 9780323532365

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The Treatment of Myeloid Malignancies with Kinase Inhibitors, An Issue of Hematology/Oncology Clinics of North America, E-Book by Ann Mullally Pdf

This issue of Hematology/Oncology Clinics will focus on The Treatment of Myeloid Malignancies with Kinase Inhibitors. Articles will focus on: Targeting aberrant signaling in myeloid malignancies: promise versus reality; The development and use of imatinib for the treatment of chronic myelogenous leukemia; Mechanisms of resistance to ABL kinase inhibition in CML and the development of next generation ABL kinase inhibitors; Tyrosine kinase inhibitors in the treatment of systemic mastocytosis and hypereosinophilic syndrome; The development and use of JAK2 inhibitors for the treatment of myeloproliferative neoplasms (MPN); Mechanisms of resistance to JAK2 inhibitors in MPN; Kinase inhibitor screening in myeloid malignancies; and more!

Allogeneic Stem Cell Transplantation

Author : Hillard M. Lazarus,Mary J. Laughlin
Publisher : Springer Science & Business Media
Page : 881 pages
File Size : 42,7 Mb
Release : 2010-03-02
Category : Medical
ISBN : 9781597454780

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Allogeneic Stem Cell Transplantation by Hillard M. Lazarus,Mary J. Laughlin Pdf

Since the original publication of Allogeneic Stem Cell Transplantation: Clinical Research and Practice, Allogeneic hematopoietic stem cell transplantation (HSC) has undergone several fast-paced changes. In this second edition, the editors have focused on topics relevant to evolving knowledge in the field in order to better guide clinicians in decision-making and management of their patients, as well as help lead laboratory investigators in new directions emanating from clinical observations. Some of the most respected clinicians and scientists in this discipline have responded to the recent advances in the field by providing state-of-the-art discussions addressing these topics in the second edition. The text covers the scope of human genomic variation, the methods of HLA typing and interpretation of high-resolution HLA results. Comprehensive and up-to-date, Allogeneic Stem Cell Transplantation: Clinical Research and Practice, Second Edition offers concise advice on today's best clinical practice and will be of significant benefit to all clinicians and researchers in allogeneic HSC transplantation.

BCR-ABL Tyrosine Kinase Inhibitors—Advances in Research and Application: 2012 Edition

Author : Anonim
Publisher : ScholarlyEditions
Page : 69 pages
File Size : 46,7 Mb
Release : 2012-12-26
Category : Medical
ISBN : 9781481611299

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BCR-ABL Tyrosine Kinase Inhibitors—Advances in Research and Application: 2012 Edition by Anonim Pdf

BCR-ABL Tyrosine Kinase Inhibitors—Advances in Research and Application: 2012 Edition is a ScholarlyBrief™ that delivers timely, authoritative, comprehensive, and specialized information about BCR-ABL Tyrosine Kinase Inhibitors in a concise format. The editors have built BCR-ABL Tyrosine Kinase Inhibitors—Advances in Research and Application: 2012 Edition on the vast information databases of ScholarlyNews.™ You can expect the information about BCR-ABL Tyrosine Kinase Inhibitors in this eBook to be deeper than what you can access anywhere else, as well as consistently reliable, authoritative, informed, and relevant. The content of BCR-ABL Tyrosine Kinase Inhibitors—Advances in Research and Application: 2012 Edition has been produced by the world’s leading scientists, engineers, analysts, research institutions, and companies. All of the content is from peer-reviewed sources, and all of it is written, assembled, and edited by the editors at ScholarlyEditions™ and available exclusively from us. You now have a source you can cite with authority, confidence, and credibility. More information is available at http://www.ScholarlyEditions.com/.

A Closer Look at Kinase Inhibition

Author : Alex Tompson
Publisher : Unknown
Page : 128 pages
File Size : 52,6 Mb
Release : 2020-04-14
Category : Electronic
ISBN : 1536169730

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A Closer Look at Kinase Inhibition by Alex Tompson Pdf

The book opens with a discussion on the roles of various tyrosine kinases inhibitors and molecular mechanisms of acquired resistance to tyrosine kinase inhibitor drugs therapy in colon-rectal cancer. The authors summarise host cell and viral protein kinases, the progress in their use, and the repurposing of approved kinase inhibitors as broad-spectrum antivirals. The key kinases, namely CLK1, DYRK1A, CDK5, GSK3 and CK1, are analysed as data indicate that targeting these proteins may have therapeutic promise against Alzheimer's disease.

Overcoming Resistance to EGFR Inhibitors in EGFR-Mutant NSCLC

Author : Anthony Faber
Publisher : Academic Press
Page : 150 pages
File Size : 55,9 Mb
Release : 2023-01-30
Category : Science
ISBN : 9780128228340

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Overcoming Resistance to EGFR Inhibitors in EGFR-Mutant NSCLC by Anthony Faber Pdf

Overcoming Resistance to EGFR Inhibitors in EGFR Mutant NSCLC 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

Kinase Drug Discovery

Author : Richard A. Ward,Frederick Goldberg
Publisher : Royal Society of Chemistry
Page : 333 pages
File Size : 52,7 Mb
Release : 2012
Category : Medical
ISBN : 9781849731744

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Kinase Drug Discovery by Richard A. Ward,Frederick Goldberg Pdf

Kinase drug discovery remains an area of significant interest across academia and in the pharmaceutical industry. There are now around 13 FDA approved small molecule drugs which target kinases and many more compounds in various stages of clinical development. Although there have been a number of reviews/publications on kinase research, this book fills a gap in the literature by considering the current and future opportunities and challenges in targeting this important family of enzymes. The book is forward-looking and identifies a number of hot topics and key areas for kinase drug discovery over the coming years. It includes contributions from highly respected authors with a combined experience in the industry of well over 200 years, which has resulted in a book of great interest to the kinase field and across drug discovery more generally. Readers will gain a real insight into the huge challenges and opportunities which this target class has presented drug discovery scientists. The many chapters cover a wide breadth of topics, are well written and include high quality colour and black and white images. Topics covered include an outline of how medicinal chemistry has been able to specifically exploit this unique target class, along with reflections on the mechanisms of kinases inhibitors. Also covered is resistance to kinase inhibitors caused by amino acid mutations, case studies of kinase programs and reviews areas beyond protein kinases and beyond the human kinome. Also described are modern approaches to finding kinase leads and the book finishes with a reflection of how kinase drug discovery may progress over the coming years.

Successful Drug Discovery, Volume 3

Author : J¿nos Fischer,Christian Klein,Wayne E. Childers
Publisher : John Wiley & Sons
Page : 472 pages
File Size : 42,5 Mb
Release : 2018-06-05
Category : Medical
ISBN : 9783527343034

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Successful Drug Discovery, Volume 3 by J¿nos Fischer,Christian Klein,Wayne E. Childers Pdf

With its focus on drugs so recently introduced that they have yet to be found in any other textbooks or general references, the information and insight found here makes this a genuinely unique handbook and reference. Following the successful approach of the previous volumes in the series, inventors and primary developers of successful drugs from both industry and academia tell the story of the drug's discovery and describe the sometimes twisted route from the first drug candidate molecule to the final marketed drug. The 11 case studies selected describe recent drugs ranging across many therapeutic fields and provide a representative cross-section of present-day drug developments. Backed by plenty of data and chemical information, the insight and experience of today's top drug creators makes this one of the most useful training manuals that a junior medicinal chemist may hope to find. The International Union of Pure and Applied Chemistry has endorsed and sponsored this project because of its high educational merit.

Small Molecules in Oncology

Author : Uwe M. Martens
Publisher : Springer Science & Business Media
Page : 242 pages
File Size : 52,8 Mb
Release : 2010-01-14
Category : Medical
ISBN : 9783642012228

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Small Molecules in Oncology by Uwe M. Martens Pdf

Extensive research into the molecular mechanisms of cancer disease has heralded a new age of targeted therapy. In malignant cells, key proteins that are crucial to tumor growth and survival are now being targeted directly with rationally designed inhibitors. Apart from monoclonal antibodies, small molecule therapeutics such as oncogenic protein kinase inhibitors are attracting a vast amount of investigational attention. This textbook, written by acknowledged experts, provides a broad overview of the small molecules currently used for the treatment of malignant diseases and discusses interesting novel compounds that are in the process of clinical development to combat cancer.