Next generation kinase inhibitors moving beyond the ATP binding/catalytic sites /: moving beyond the ATP binding/catalytic sites. (2020)

• Record Type: Book
• Further Information: Note: Paul Shapiro, editor.
• Other Names: Shapiro, Paul
• Contents: Intro -- Preface -- Contents -- Contributors -- Introduction to Kinases, Cellular Signaling, and Kinase Inhibitors -- Historical Overview of Protein Kinases and Targeted Inhibition -- Overview of Protein Kinase Signaling Pathways -- Overview of Protein Kinase Structural Features -- References -- Overview of Current Type I/II Kinase Inhibitors -- Introduction -- FDA-Approved Kinase Inhibitors: Type I and II Mechanisms of Action -- Type I Binding Modes -- Type II Binding Modes -- Successes and Limitations -- References Avoiding or Co-Opting ATP Inhibition: Overview of Type III, IV, V, and VI Kinase Inhibitors -- Part A: Type III Kinase Inhibitors -- Part B: Type IV Kinase Inhibitors -- Part C: Type V Kinase Inhibitors -- Part D: Type VI Kinase Inhibitors -- References -- Protein Kinase Interactions with Regulatory and Effector Proteins -- Introduction -- Docking Interactions Between Protein Kinases and Other Proteins -- MAP Kinase Interactions Through the DRS -- MAP Kinase Interactions Through the FRS -- Conclusions -- References -- Developing Kinase Inhibitors Using Computer-Aided Drug Design Approaches Introduction -- Basic Concepts of CADD and Typical CADD Methods -- Applications of CADD Methods for Kinase Inhibitor Development -- Extracellular-Signal-Regulated Kinases (ERK) -- P38 MAP Kinase -- P56 T Cell Tyrosine Kinase (Lck) -- Summary -- References -- A Toolbox of Structural Biology and Enzyme Kinetics Reveals the Case for ERK Docking Site Inhibition -- ERK Overview -- The D-Recruitment Site -- The F-Recruitment Site -- Docking Sites in Catalysis -- The Story of Ets-1 -- Steady-State Kinetics -- Presteady-State Kinetics -- Mutational Studies -- Structural Insights Mechanisms of Docking Site Inhibition -- Reversible Inhibition -- Covalent Inhibition -- Noncatalytic Effects -- Docking Site Inhibitor Development -- Current DRS Inhibitors -- Hydrophobic Groove and CD Domain Inhibitors -- ED Domain Inhibitors -- Current FRS Inhibitors -- The Future of Docking Site Inhibitors -- Summary -- References -- Novel Stabilized Peptide Inhibitors of Protein Kinases -- Introduction -- Targeting Receptor Tyrosine Kinase Dimerization with Stapled Peptides -- Targeting the Extracellular Region of EGFR with Constrained Peptides Targeting the Intracellular Region of EGFR with Stapled Peptides -- RTKs as Peptide Inhibitor Targets -- Disruption of Spatiotemporal Regulation of Kinases with Stapled Peptides -- A Kinase Anchoring Proteins (AKAPs) -- Functional Aspects of AKAP Complexes -- Targeting AKAP Complexes -- Targeting PKA RII Anchoring by AKAPs -- Targeting PKA RI Anchoring by AKAPs -- Targeting AKAP Complexes Beyond PKA Interactions -- Pseudosubstrate Inhibition of Kinases with Stabilized Peptides -- Kinase Pseudosubstrate Interactions -- Protein Kinase Inhibitor (PKI) as a Pseudosubstrate
• Publisher Details: Cham : Springer
• Publication Date: 2020
• Extent: 1 online resource
• Subjects: 572/.792; Protein kinases -- Inhibitors; Protein kinases -- Inhibitors; Electronic books; Electronic books
• Languages: English
• ISBNs: 9783030482831; 3030482839
• Related ISBNs: 3030482820; 9783030482824
• Access Rights: Legal Deposit; Only available on premises controlled by the deposit library and to one user at any one time; The Legal Deposit Libraries (Non-Print Works) Regulations (UK).
• Access Usage: Restricted: Printing from this resource is governed by The Legal Deposit Libraries (Non-Print Works) Regulations (UK) and UK copyright law currently in force.