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Arginase: Structure, Function, and Therapeutic Targeting

  • 1st Edition, Volume 740 - December 8, 2026
  • Latest edition
  • Editor: Luigi Di Costanzo
  • Language: English

Arginase: Structure, Function, and Therapeutic Targeting, Volume 740 in the Methods in Enzymology series, provides a comprehensive, methodology-driven perspective on arginase rese… Read more

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Description

Arginase: Structure, Function, and Therapeutic Targeting, Volume 740 in the Methods in Enzymology series, provides a comprehensive, methodology-driven perspective on arginase research spanning molecular, biochemical, and translational domains. Chapters in this new release include Expression, Purification, and Structural Characterization of Human and Leishmania Arginase with Comparative Analysis of Structures from the Protein Data Bank, Synthesis of First-Generation Arginase Inhibitors, Computational and Structure-Guided Design of Arginase Inhibitors, Metal Substitution in Arginase: Experimental Approaches to Study Metal-Dependent Catalysis, Therapeutic Arginase Formulations: PEGylation, Stability, and Advanced Delivery Systems, and much more.

Additional chapters cover Dual ARG1/ARG2 Inhibition: Experimental and Structural Strategies for Inhibitor Design and Optimization, Synthesis of Second-Generation Arginase Inhibitors, Cryo-EM Workflow and Structural Characterization of Arginase–Antibody Complexes, Development and Validation of an Electrochemical Assay for Arginase Activity, Experimental and Structural Analysis of H. pylori Arginase in Gastric Immune Evasion, Agmatinase and Alternative Arginine Utilization Pathways in Bacteria: Biochemical and Functional Perspectives, Catalytic Diversification of the Arginase Fold: Structural and Mechanistic Insights from DcsB, Beyond Arginase: Structural Biology of the Extended Guanidinase Family, Plant Arginase: Structural and Functional Roles in Nitrogen Metabolism, and much more.

Key features

  • Provides comprehensive coverage of arginase from structure and mechanism to therapeutic targeting
  • Includes methodology-driven chapters that emphasize experimental design, reproducibility, and analytical approaches
  • Integrates academic and industry perspectives on inhibitor development, antibody-based and protein-based strategies, and translational applications

Readership

Biochemists, structural biologists, enzymologists, and medicinal chemists working on enzyme mechanisms and drug discovery. It will also be valuable to researchers in metabolism, pharmacology, and translational medicine, as well as clinicians and industry scientists interested in targeting arginine metabolism in cardiovascular, immune, and metabolic diseases, and advanced students in biochemistry and related fields.

Table of contents

Section I: Molecular and Structural Approaches to Arginase Function and Inhibition

Chapter 1: Expression, Purification, and Structural Characterization of Human and Leishmania Arginase
E. D'Antonio, L.F. Di Costanzo, D.W. Christianson
Chapter 2: Systematic Structural Analysis of Arginase and the Expanded Arginase-Fold Superfamily Using the Protein Data Bank
L.F. Di Costanzo, D.W. Christianson, E. D'Antonio
Chapter 3: Synthesis of First-Generation Arginase Inhibitors
F. Sodano
Chapter 4: Computational and Experimental Strategies for the Discovery of Non-Boronic Arginase I Inhibitors
S. Gathiaka, and L.F. Di Costanzo
Chapter 5: Computational and Structure-Guided Design of Arginase Inhibitors
M.A. Fumagalli
Chapter 6: Metal Substitution in Arginase: Experimental Approaches to Study Metal-Dependent Catalysis
G.P. Georgiou

Section II: Advanced Therapeutic Strategies and Analytical Methods for Arginase

Chapter 7: Therapeutic Arginase Formulations: PEGylation, Stability, and Advanced Delivery Systems
L. Sloan, M. Rudebeck

Chapter 8: Dual ARG1/ARG2 Inhibition: Experimental and Structural Strategies for Inhibitor Design and Optimization
M. Grzybowski

Chapter 9: Synthesis of Second and Third-Generation Arginase Inhibitors
F. Sodano

Chapter 10: Cryo-EM Workflow and Structural Characterization of Arginase–Antibody Complexes
G. Scapin

Chapter 11: Development and Validation of an Electrochemical Assay for Arginase Activity
A. Miglione, L. Di Costanzo, S. Cinti

Section III: Clinical, Metabolic, and Translational Aspects of Arginase

Chapter 12: Experimental and Structural Analysis of H. pylori Arginase in Gastric Immune Evasion
A.K. Sau

Chapter 13: Alternative Arginine Utilization Pathways in Bacteria: Identifying and Assaying Agmatinase and Agmatine Deiminase Activity
J. French

Chapter 14: Arginase Deficiency and Urea Cycle Disorders: Clinical and Metabolic Management
N. Brunetti-Pierri

Chapter 15: Inborn Errors of Metabolism and Arginine Pathways: Experimental and Clinical Approaches
A. Schulze

Chapter 16: Arginine Metabolism and Protein Balance: Experimental Approaches in Human Physiology
M. P. K. J. Engelen

Chapter 17: Arginase in Cardiovascular and Vascular Inflammatory Disease
W. Durante


Section IV: Evolutionary and Functional Diversity of Arginase and Related Enzymes


Chapter 18: Catalytic Diversification of the Arginase Fold: Structural and Mechanistic Insights from DcsB
Y. Matoba

Chapter 19: Plant Arginase: Structural and Functional Roles in Nitrogen Metabolism
B. Sekula

Product details

  • Edition: 1
  • Latest edition
  • Volume: 740
  • Published: December 8, 2026
  • Language: English

About the editor

LC

Luigi Di Costanzo

Luigi F. Di Costanzo is a structural chemist and biochemist specializing in structural biology, enzymology, and protein science, with a focus on metalloenzymes and structure-based approaches to enzyme function and inhibition. He earned his Ph.D. in Chemistry from the Università degli Studi di Trieste (Italy) and completed postdoctoral training at the University of Pennsylvania, where he contributed to foundational studies on enzyme structure and inhibitor design.

His research centers on the three-dimensional structure and mechanism of enzymes, with extensive experience in macromolecular crystallography, including structure determination, refinement, and analysis of protein–ligand complexes. His work integrates structural, biochemical, and biophysical approaches to understand enzyme function and guide therapeutic targeting.

In addition to his research, he served for over a decade as a biocurator with the Worldwide Protein Data Bank (wwPDB) at the RCSB PDB (Rutgers University), contributing to the validation and annotation of more than 7,500 macromolecular structures. This work supported the integrity and reproducibility of structural biology data used by the global scientific community, including structural datasets that have contributed to the development of machine learning approaches to protein structure prediction, such as AlphaFold.

His broader expertise includes multiscale structural characterization through complementary imaging and analytical techniques, including X-ray micro–computed tomography (µCT), linking atomic-level structure to complex biological systems, as well as contributions to community data resources, including the Protein Design Archive. As editor of the Methods in Enzymology volume “Arginase: Structure, Function, and Therapeutic Targeting,” he brings together structural, metabolic, and translational perspectives to advance the field.