Protein kinases as drug targets by Gerhard MГјller

Cover of: Protein kinases as drug targets | Gerhard MГјller

Published by Wiley-VCH, John Wiley [distributor] in Weinheim, Chichester .

Written in English

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Subjects:

  • Development,
  • Protein Kinase Inhibitors,
  • Antineoplastic agents,
  • Inhibitors,
  • Drug Delivery Systems,
  • Protein kinases,
  • Therapeutic use,
  • Drug Discovery

Edition Notes

Book details

Statementedited by Bert Klebl, Gerhard Müller, and Michael Hamacher
SeriesMethods and principles in medicinal chemistry -- 49
ContributionsWiley online library
Classifications
LC ClassificationsRM666.E548 P76 2011
The Physical Object
Format[electronic resource] /
ID Numbers
Open LibraryOL25566717M
ISBN 103527633472, 3527633480, 3527317902
ISBN 109783527633470, 9783527633487, 9783527317905
OCLC/WorldCa729724693

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"In summary, Protein Kinases as Drug Targets is an excellent book that can be highly recommended to both experts and novices in the various disciplines in this field of research; lecturers searching for comprehensive drug discovery stories will also be happy to find numerous instructive examples.".

"In summary, Protein Kinases as Drug Targets is an excellent book that can be highly recommended to both experts and novices in the various disciplines in this field of research; lecturers searching for comprehensive drug discovery stories will also be happy to find numerous instructive examples." (ChemMedChem, 1 December ) From the PublisherAuthor: Bert Klebl.

Protein Kinases as Drug Targets - Ebook written by Bert Klebl, Gerhard Müller, Michael Hamacher, Raimund Mannhold, Hugo Kubinyi, Gerd Folkers. Read this book using Google Play Books app on your PC. "In summary, Protein Kinases as Drug Targets is an excellent book that can be highly recommended to both experts and novices in the various disciplines in this field of research; lecturers searching for comprehensive Protein kinases as drug targets book discovery stories will also be happy to find numerous instructive examples." (ChemMedChem, 1 December )Author: Bert Klebl.

"In summary, Protein Kinases as Drug Targets is an excellent book that can be highly recommended to both experts and novices in the various disciplines in this field of research; lecturers searching for comprehensive drug discovery stories will also be happy to find numerous instructive examples." (ChemMedChem, 1 December )Manufacturer: Wiley-VCH.

Protein Kinases as Drug Targets Volume 49 of Methods and Principles in Medicinal Chemistry: Editors: Bert Klebl, Gerhard Müller, Michael Hamacher: Contributors: Raimund Mannhold, Hugo Kubinyi, Gerd. Protein Kinases as Drug Targets, Volume 1st Edition.

by Bert Klebl (Editor), Gerhard Müller (Editor), Michael Hamacher (Editor), Raimund Mannhold (Series Editor), Hugo Kubinyi (Series Editor), Gerd Folkers (Series Editor) & 3 more.

ISBN ISBN Protein Kinases in Drug Discovery, Volume discusses the latest information on protein kinases and how they modify other proteins by chemically adding phosphate groups to them.

New chapters in this release include Transport Proteins and AMPs: Implications in Human Disease, Protein kinase CK2 inhibition as a pharmacological strategy, Emerging role of Protein kinase in diabetes mellitus: From Mechanism to therapy, Dual Roles of ATP-binding site in Protein Kinases: Orthosteric.

Title: Kinases as Drug Targets in Inflammation: In Vitro and In Vivo Target Validation and Expression Profiling VOLUME: 6 ISSUE: 1 Author(s):Tatjana Clarissa Gust and Arne Affiliation:Schering AG, CRBA Inflammation,Müllerstr.

Berlin, Germany. Keywords:Mitogen Activated Protein (MAP) Kinases, Phosphoinositide 3-Kinases, Syk-Family Kinases, siRNA transfection, Protein Arrays.

Reasonably, protein Protein kinases as drug targets book inhibitor drugs target and act upon signaling pathways that have gone awry in a given cancer, whereas all traditional chemotherapy drugs work on cell division and growth mostly leading to the destruction of healthy cells as the main problems in treatment of cancer patients.

Protein kinases as drug targets. by Bert Klebl et al. Wiley-VCH pages $ Hardcover Methods and principles in medicinal chemistry; v RM Protein kinases are a large group of related enzymes that activate many kinds of proteins, thus mediating signal transduction in cell growth and differentiation.

The Cysteinome of Protein Kinases as a Target in Drug Development. Apirat Chaikuad. Nuffield Department of Clinical Medicine, Structural Genomics Consortium and Target Discovery Institute, University of Oxford, Old Road Campus Research Building, Roosevelt Drive, Oxford, OX3 7DQ UK.

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. Abstract: Identification of the key roles of protein kinases in signaling pathways leading to development of cancer has caused pharmacological interest to concentrate extensively on targeted therapies as a more specific and effective way for blockade of cancer progression.

This review will mainly focus on inhibitors targeting these key components of cellular signaling by employing a technology-based point of view.

Addeddate Identifier protein-kinases-as-drug-targets Identifier-ark ark://t9g53g73v Ocr ABBYY FineReader (Extended OCR). To Find New Cancer Drug Targets, Reorganize Kinases - Free download as .saif), Text File .txt) or read online for free. Grouping protein kinases by their reaction to drugs could reveal new cancer drug targets.

Protein kinases—a class of signaling molecules—regulate most cellular processes. When protein kinases malfunction, diseases such as cancer can result. Over the past 20 years, protein kinases have become a major class of drug targets because these signaling biomolecules are often deregulated in disease, particularly in cancer.

Today, 37 small. A growing interest in developing orally active protein-kinase inhibitors has recently culminated in the approval of the first of these drugs for clinical use.

Protein kinases have now become the second most important group of drug targets, after G-protein-coupled by:   Buy Protein Kinases as Drug Targets: 49 (Methods and Principles in Medicinal Chemistry) by Klebl, Bert, Müller, Gerhard, Hamacher, Michael, Mannhold, Raimund, Kubinyi, Hugo, Folkers, Gerd (ISBN: ) from Amazon's Book Store.

Everyday low prices and free delivery on eligible : Hardcover. Catherine Litalien, Pierre Beaulieu, in Pediatric Critical Care (Third Edition), Protein Kinases.

Protein kinases, which are located in the cytoplasm, are enzymes that phosphorylate main protein kinases are PKA, PKG, PKC, 56 and tyrosyl protein kinases (part of tyrosine kinase receptors). They are distinguished from each other by the different intracellular second messengers. against the target kinase represents the center of activities.

While this parameter seems to be a straightforward and measurable parameter, there are a variety of possibilities of how an inhibitor might be binding to a protein kinase. Potentially, these different binding modes can. Protein phosphorylation and protein ubiquitination regulate most aspects of cell life, and defects in these control mechanisms cause cancer and many other diseases.

In the past decade, protein kinases have become one of the most important classes of drug targets for the pharmaceutical industry. ProteomicsDB database, should facilitate basic, clinical, and drug discovery research and aid clinical decision-making. M any of the protein kinases encodedby the human genome have emerged as drug targets because their function is often deregulated in signaltransduc-tion networks, leading to diseases such as cancer and inflammation.

More. Protein kinases are intimately integrated in different signal transduction pathways for the regulation of cardiac function in both health and disease.

Protein kinase A (PKA), Ca2+-calmodulin-dependent protein kinase (CaMK), protein kinase C (PKC), phosphoinositide 3-kinase (PI3K) and mitogen-activated protein kinase (MAPK) are not only involved in the control of subcellular activities for.

These enzymes affect cardiac function by phosphorylating different sites engaged in the regulation of cation transport, cellular metabolism, cardiac growth and apoptosis, as well as contractile activity (Table 1) [,]. Table 1. Protein kinases and their substrates.

The sequencing of the human genome has revealed more than genes for protein kinases with often still undefined function, but huge potential for drug development.“Today protein kinase inhibitors are very much in the focus of cancer research, as these substances could arrest or at least slow down the growth of tumors,” explains at, head of the project at ProQinase GmbH.

reating protein-protein interactions as a novel and highly promising class of drug targets, this volume introduces the underlying strategies step by step, from the biology of PPIs to biophysical and computational methods for their investigation. The main part of the book describes examples of protein targets.

It is noteworthy that the majority of clinical trials target only 43 protein kinases and about 50% of these inhibitors target kinases which already have approved drugs. The full potential of the human kinome as a source of new drugs has not been fully exploited since more than kinases have unknown function and 50% of all kinases are largely.

Significantly, protein kinases are the second most targeted group of drug targets, after the G-protein-coupled receptors. Since the development of the first protein kinase inhibitor, in the early s, 37 kinase inhibitors have received FDA approval. Stony Brook-led research proposes a new approach to classifying protein kinases – a class of signaling molecules – that takes account of their potential as drug targets.

Protein kinases regulate most cellular processes. When they malfunction, diseases such as cancer can result. Both drugs target tyrosine kinases; Gleevec targets the BCR-ABL tyrosine kinase, and Iressa targets the tyrosine kinase domain of the epidermal growth factor receptor.

Protein kinase inhibitors fall into four main groups: substrate-specific inhibitors, ATP-competitive inhibitors, activation inhibitors and irreversible inhibitors. Protein kinase inhibitors represent a major class of anticancer drugs, which are notoriously unspecific.

Efforts to exploit the polypharmacology of inhibitors for target deconvolution have met with little success. Our significant contribution is to apply regularized regression to kinase expression and kinase profiling on a large set of inhibitors.

By selecting a set of optimally designed. of protein kinases play causal roles in human disease, this family of enzymes has become one of the most important drug targets over the past two decades. Imatinib was approved by the United States FDA for the treatment of chronic myelogenous leukemia in ; this small molecule inhibits the BCR-Abl.

Cancer drug discovery and development RC Protein tyrosine kinases (PTKs) function as components of signal transduction pathways and play a central role in the control of cell growth, metabolism, differentiation and apoptosis.

Currently 20 different PTKs are being considered as potential therapeutic targets in oncology. Stony Brook-led research proposes a new approach to classifying protein kinases – a class of signaling molecules – that takes account of their potential as drug targets.

Protein kinases regulate most cellular processes. When they malfunction, diseases such as cancer can result. This is why certain types of protein kinases implicated in disease are desirable drug targets. Drug targets. The term "biological target" is frequently used in pharmaceutical research to describe the native protein in the body whose activity is modified by a drug resulting in a specific effect, which may be a desirable therapeutic effect or an unwanted adverse this context, the biological target is often referred to as a drug target.

Over the past 15 years protein kinases have become the pharmaceutical industry's most important class of drug target in the field of cancer. Some 20 drugs that target kinases have been approved for clinical use over the past decade, and hundreds more are undergoing clinical trials.

After G-protein-coupled receptors, protein kinases are considered the second most important class of drug targets. Abnormal kinase activities have been linked either directly or indirectly to over human diseases, particularly those which display proliferative or inflammatory characteristics.

Protein kinases are major drug targets, but the development of highly-selective inhibitors has been challenging due to the similarity of their active sites. The observation of distinct structural states of the fully-conserved Asp-Phe-Gly (DFG) loop has put the concept of conformational selection for the DFG-state at the center of kinase drug discovery.

Current chemotherapy to treat these diseases is far from ideal and many different approaches are being taken to identify new drug targets.

One family of potential drug targets are the protozoan protein kinases protein kinases Subject Category: Chemicals and Chemical Groups see more details. A protein is an approved drug target if it is the target of an approved drug, and a non-target otherwise.

In order for a protein to have any potential as a drug target it must be druggable. A druggable protein is one that possesses folds that favour interactions with small drug-like molecules, be they endogenous or extraneous, and therefore is.Kinase inhibitor discovery is a very active area as developers are exploring more deeply into designing immune-modulatory agents as single or combination therapies, tackling chronic disease indications such as inflammation and CNS disorders, as well as effectively harnessing allosteric modulators, and covalently binding compounds.

WEST LAFAYETTE, Ind. – Purdue University researchers have developed a high-throughput method for matching kinases to the proteins they phosphorylate, speeding the ability to identify multiple potential cancer drug targets. Kinases are proteins that catalyze the transfer of a phosphate group to another protein, a process called phosphorylation.

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