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Biomedical Sciences - Pharmacology & Toxicology | Phosphatase Modulators

Phosphatase Modulators

Series: Methods in Molecular Biology, Vol. 1053

Millán, José Luis (Ed.)

2013, X, 315 p. 75 illus., 45 illus. in color.

A product of Humana Press
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  • Serves as a "how to" manual for the initiation of drug discovery efforts
  • Provides step-by-step detail essential for reproducible results
  • Contains key tips and implementation advice from the experts

Driving further the research on mammalian alkaline phosphatase structure and function, Phosphatase Modulators collects expert contributions into one “how to” manual for basic scientists interested in initiating a drug discovery effort. While this book contains the traditional method chapters and some typical reviews on the structure and known functions of phosphatases, other contributions are meant to discuss approaches and alternatives useful in making “go/no-go” decisions in high throughput screening (HTS) and lead optimization campaigns. Many chapters focus on tissue-nonspecific alkaline phosphatase (TNAP) as well as protein phosphatases.  Written for the highly successful Methods in Molecular Biology series, chapters in this volume include the kind of detail and key implementation advice that promotes reproducible results.


Step-by-step and practical, Phosphatase Modulators offers a path to understanding many of the facets and complexities associated with undertaking a drug discovery effort and will serve as a roadmap to initiating those efforts.

Content Level » Professional/practitioner

Keywords » Drug discovery - Medicinal chemistry - Pharmaceuticals - Probe development - TNAP - Tissue-nonspecific alkaline phosphatase

Related subjects » Chemistry - Pharmacology & Toxicology

Table of contents 

1. Chemical Probe Development Versus Drug Development

            Michael R. Jackson


2. Phosphatase High-Throughput Screening Assay Design and Selection

            Eduard A. Sergienko


3. Multisystemic Functions of Alkaline Phosphatases

            René Buchet, José Luis Millán, and David Magne


4. Robotic Implementation of Assays: Tissue-Nonspecific Alkaline Phosphatase (TNAP) Case Study

            Thomas D.Y. Chung


5. Inhibitors of Tissue-Nonspecific Alkaline Phosphatase (TNAP): From Hits to Leads

            Peter Teriete, Anthony B. Pinkerton, and Nicholas D.P. Cosford


6. A Method for Direct Assessment of Tissue-Nonspecific Alkaline Phosphatase (TNAP) Inhibitors in Blood Samples

            Eduard Sergienko, Qing Sun, and Chen-Ting Ma


7. Isolation and Characteristics of Matrix Vesicles

            René Buchet, Slawomir Pikula, David Magne, and Saïda Mebarek


8. The Use of Tissue-Nonspecific Alkaline Phosphatase (TNAP) and PHOSPHO1 Inhibitors to Affect Mineralization by Cultured Cells

            Tina Kiffer-Moreira and Sonoko Narisawa


9. Modulators of Intestinal Alkaline Phosphatase

            Ekaterina V. Bobkova, Tina Kiffer-Moreira, and Eduard A. Sergienko


10. New Activity Assays for ENPP1 with Physiological Substrates ATP and ADP

            Chen-Ting Ma and Eduard Sergienko


11. Structure of Acid Phosphatases

            César L. Araujo and Pirkko T. Vihko


12. Purification of Prostatic Acid Phosphatase (PAP) for Structural and Functional Studies

            Annakaisa M. Herrala, Ileana B. Quintero, and Pirkko T. Vihko


13. Protein Tyrosine Phosphatases: Structure, Function, and Implication in Human Disease

            Lutz Tautz, David A. Critton, and Stefan Grotegut


14. High-Throughput Screening for Protein Tyrosine Phosphatase Activity Modulators

            Lutz Tautz and Eduard A. Sergienko


15. Evaluating Effects of Tyrosine Phosphatase Inhibitors on T Cell Receptor Signaling

            Souad Rahmouni, Laurence Delacroix, Wallace H. Liu, and Lutz Tautz


16. Interactor-Guided Dephosphorylation by Protein Phosphatase-1

            Shannah Boens, Kathelijne Szekér, Aleyde Van Eynde, and Mathieu Bollen


17. Structure, Regulation, and Pharmacological Modulation of PP2A Phosphatases

            Caroline Lambrecht, Dorien Haesen, Ward Sents, Elitsa Ivanova, and Veerle Janssens

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