Rational Drug Design: Methods and Protocols

Author:   Yi Zheng
Publisher:   Humana Press Inc.
Edition:   Softcover reprint of the original 1st ed. 2012
Volume:   928
ISBN:  

9781493959006


Pages:   230
Publication Date:   23 August 2016
Format:   Paperback
Availability:   Manufactured on demand   Availability explained
We will order this item for you from a manufactured on demand supplier.

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Rational Drug Design: Methods and Protocols


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Author:   Yi Zheng
Publisher:   Humana Press Inc.
Imprint:   Humana Press Inc.
Edition:   Softcover reprint of the original 1st ed. 2012
Volume:   928
Weight:   0.641kg
ISBN:  

9781493959006


ISBN 10:   149395900
Pages:   230
Publication Date:   23 August 2016
Audience:   Professional and scholarly ,  Professional & Vocational
Format:   Paperback
Publisher's Status:   Active
Availability:   Manufactured on demand   Availability explained
We will order this item for you from a manufactured on demand supplier.

Table of Contents

On Setting up and Assessing Docking simulations for Virtual Screening.-Virtual Ligand Screening Combined with NMR to Identify Dvl PDZ Domain Inhibitors Targeting the Wnt Signaling.-Rational Design of Rho GTPase Targeting Inhibitors.-Rational Design of Peptide Ligands Against a Glycolipid by NMR Studies.-A Combinatorial Strategy for the Acquisition of Potent and Specific Protein Tyrosine Phosphatase Inhibitors.-Identification of Allosteric Inhibitors of p21-Activated Kinase.-Using a Modified Yeast Two-hybrid System to Screen for Chemical GEF Inhibitors.-Random Mutagenesis of Peptide Aptamers As An Optimization Strategy for Inhibitor Screening.-A Screening Strategy for Trapping the Inactive Conformer of a Dimeric Enzyme with a Small Molecule Inhibitor.-Use of a Fluorescent ATP Analog to Probe the Allosteric Conformational Change in the Active Site of the Protein Kinase PDK1.-Affinity Purification of Protein Kinases that Adopt a Specific Inactive Conformation.-Determination of the Kinetics and Thermodynamics of Ligand Binding to a Specific Inactive Conformation in Protein Kinases.-Purification and Specific Assays for Measuring APE-1 Endonuclease Activity.-An in vitro Screening to Identify Drug Resistant Mutations for Target-directed Chemotherapeutic Agents.-Utilizing AntagomiR (anti-sense microRNA) to Knock Down microRNA in Murine Bone Marrow Cells.-Synthesis, Conjugation, and Labeling of Multifunctional pRNA Nanoparticles for Specific Delivery of siRNA, Drugs and Other Therapeutics to Target Cells.-Mouse Models for Tumor Metastasis.Rational Design of Peptide Ligands Against a Glycolipid by NMR Studies.-A Combinatorial Strategy for the Acquisition of Potent and Specific Protein Tyrosine Phosphatase Inhibitors.-Identification of Allosteric Inhibitors of p21-Activated Kinase.-Using a Modified Yeast Two-hybrid System to Screen for Chemical GEF Inhibitors.-Random Mutagenesis of Peptide Aptamers As An Optimization Strategy for Inhibitor Screening.-A Screening Strategy for Trapping the Inactive Conformer of a Dimeric Enzyme with a Small Molecule Inhibitor.-Use of a Fluorescent ATP Analog to Probe the Allosteric Conformational Change in the Active Site of the Protein Kinase PDK1.-Affinity Purification of Protein Kinases that Adopt a Specific Inactive Conformation.-Determination of the Kinetics and Thermodynamics of Ligand Binding to a Specific Inactive Conformation in Protein Kinases.-Purification and Specific Assays for Measuring APE-1 Endonuclease Activity.-An in vitro Screening to Identify Drug Resistant Mutations for Target-directed Chemotherapeutic Agents.-Utilizing AntagomiR (anti-sense microRNA) to Knock Down microRNA in Murine Bone Marrow Cells.-Synthesis, Conjugation, and Labeling of Multifunctional pRNA Nanoparticles for Specific Delivery of siRNA, Drugs and Other Therapeutics to Target Cells.-Mouse Models for Tumor Metastasis.

Reviews

From the reviews: This book covers some of the tools and techniques involved in rational drug design with a series of case studies designed to act as a compendium of methods and protocols intended for readers to adopt or modify. ... The book would therefore make interesting reading to any student or investigator looking to gain a wider appreciation of strategies and activities across different disciplines or unfamiliar projects in the early drug discovery phase as well as the primary target audience of organic/medicinal chemists and molecular biologists. (Stefan Kavanagh, BTS Newsletter - The British Toxicology Society, Issue 43, Winter, 2013)


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