Phosphatase Modulators

Phosphatase Modulators
José Luis Millán
Release at: 2013
Pages: 327
First Edition
File Size: 6 MB
File Type: pdf
Language: English

Description of Phosphatase Modulators

The book Phosphatase Modulators for decades, medicinal chemistry efforts, including target validation, small-molecule screening, structure–activity relationships, and lead optimization, were terms and activities largely restricted to scientists working at large pharmaceutical companies with well established drug discovery programs. 

However, that situation changed with the implementation of the road map initiative by the National Institutes of Health in the USA, which supported the development of screening centers at academic institutions, known as the Molecular Libraries Probe Production Centers Network (MLPCN). 

Suddenly, basic scientists could be involved in the design of assays to screen for modulators of their favorite targets and develop probes to help them investigate the function of their pet protein or pathway. They could also now aspire to become involved in the development of pharmaceuticals for clinical use.

Content of Phosphatase Modulators

1 Chemical Probe Development Versus Drug Development. 1
Michael R. Jackson

2 Phosphatase High-Throughput Screening Assay Design and Selection7
Eduard A. Sergienko

3 Multisystemic Functions of Alkaline Phosphatases. 27
René Buchet, José Luis Millán, and David Magne

4 Robotic Implementation of Assays: Tissue-Nonspecific Alkaline Phosphatase (TNAP) Case Study  53
Thomas D.Y. Chung

5 Inhibitors of Tissue-Nonspecific Alkaline Phosphatase (TNAP): From Hits to Leads 85
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 . 103
Eduard A. Sergienko, Qing Sun, and Chen-Ting Ma

7 Isolation and Characteristics of Matrix Vesicles. 115
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 125
Tina Kiffer-Moreira and Sonoko Narisawa

9 Modulators of Intestinal Alkaline Phosphatase. 135
Ekaterina V. Bobkova, Tina Kiffer-Moreira, and Eduard A. Sergienko

10 New Activity Assays for ENPP1 with Physiological Substrates ATP and ADP . 145
Chen-Ting Ma and Eduard A. Sergienko

11 Structure of Acid Phosphatases155
César L. Araujo and Pirkko T. Vihko

12 Purification of Prostatic Acid Phosphatase (PAP) for Structural and Functional Studies 167
Annakaisa M. Herrala, Ileana B. Quintero, and Pirkko T. Vihko

13 Protein Tyrosine Phosphatases: Structure, Function, and Implication in Human Disease . 179
Lutz Tautz, David A. Critton, and Stefan Grotegut

14 High-Throughput Screening for Protein Tyrosine Phosphatase Activity Modulators 223
Lutz Tautz and Eduard A. Sergienko

15 Evaluating Effects of Tyrosine Phosphatase Inhibitors on T Cell Receptor Signaling 241
Souad Rahmouni, Laurence Delacroix, Wallace H. Liu, and Lutz Tautz

16 Interactor-Guided Dephosphorylation by Protein Phosphatase-1  271
Shannah Boens, Kathelijne Szekér, Aleyde Van Eynde, and Mathieu Bollen

17 Structure, Regulation, and Pharmacological Modulation of PP2A Phosphatases. 283
Caroline Lambrecht, Dorien Haesen, Ward Sents, Elitsa Ivanova,
and Veerle Janssens


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