Preface ......................................................... v
Contributors ................................................... xi
Part I. In Vitro Chemical Genetic Screening
1 Identification of Therapeutic Small-Molecule Leads in
Cultured Cells Using Multiplexed Pathway Reporter Readouts ... 3
Ozlem Kulak, Kiyoshi Yamaguchi, and Lawrence Lum
2 Applying the Logic of Genetic Interaction to Discover Small
Molecules That Functionally Interact with Human Disease
Alleles ..................................................... 15
Ari D. Brettman, Pauline H. Tan, Khoa Tran, and Stanley
Y. Shaw
3 Construction and Application of a Photo-Cross-Linked
Chemical Array .............................................. 29
Yasumitsu Kondoh, Kaori Honda, and Hiroyuki Osada
4 High Content Screening for Modulators of Cardiac
Differentiation in Human Pluripotent Stem Cells ............. 43
Sean Spiering, Herman Davidovics, Paul J. Bushway, Mark
Mercola, and Erik Willems
5 Small-Molecule High-Throughput Screening Utilizing
Xenopus Egg Extract ......................................... 63
Matthew R. Broadus, P. Renee Yew, Stephen R. Hann, and
Ethan Lee
Part II. In Vivo Chemical Genetic Screening
6 Fission Yeast-Based High-Throughput Screens for PKA Pathway
Inhibitors and Activators ................................... 77
Ana Santos de Medeiros, Grace Kwak, Jordan Vanderhooft,
Sam Rivera, Rachel Gottlieb, and Charles S. Hoffman
7 A Method for High-Throughput Analysis of Chronological
Aging in Schizosaccharomyces pombe .......................... 93
Jessica Stephan and Ann E. Ehrenhofer-Murray
8 Protocols for the Routine Screening of Drug Sensitivity
in the Human Parasite Trichomonas vaginalis ................ 103
Manal J. Natto, Anthonius A. Eze, and Harry P. de Koning
9 Chemical Genetic Screens Using Arabidopsis thaliana
Seedlings Grown on Solid Medium ............................ 111
Thanh Theresa Dinh and Xuemei Chen
10 Small-Molecule Screening Using Drosophila Models
of Human Neurological Disorders ............................ 127
Mickael Poidevin, Feiran Zhang, and Peng Jin
11 High-Throughput Small-Molecule Screening in
Caenorhabditis elegans ..................................... 139
Sunitha Rangaraju, Gregory M. Solis, and Michael
Petrascheck
12 Whole-Organism Screening for Modulators of Fasting
Metabolism Using Transgenic Zebrafish ...................... 157
Philipp Gut and Didier Y.R. Stainier
13 High Content Screening for Modulators of Cardiovascular
or Global Developmental Pathways in Zebrafish .............. 167
Charles H. Williams and Charles C. Hong
Part III. Small Molecules in Chemical Biology
14 Extraction Methods of Natural Products from Traditional
Chinese Medicines .......................................... 177
Jingyu Zhang, Jianying Han, Ayokunmi Oyeleye, Miaomiao
Liu, Xueting Liu, and Lixin Zhang
15 Bioassay-Guided Identification of Bioactive Molecules
from Traditional Chinese Medicines ......................... 187
Jianying Han, Jingyu Zhang, Wenni He, Pet Huang, Ayokunmi
Oyeleye, Xueting Liu, and Lixin Zhang
16 NMR Screening in Fragment-Based Drug Design: A Practical
Guide ...................................................... 197
Hai-Young Kim and Daniel F. Wyss
17 Practical Strategies for Small-Molecule Probe Development
in Chemical Biology ........................................ 209
Jonathan E. Hempel and Charles C. Hong
18 Principal Component Analysis as a Tool for Library Design:
A Case Study Investigating Natural Products, Brand-Name
Drugs, Natural Product-Like Libraries, and Drug-Like
Libraries .................................................. 225
Todd A. Wenderski, Christopher F. Stratton, Renato
A. Bauer, Felix Kopp, and Derek S. Tan
19 Small-Molecule Library Screening by Docking with PyRx ...... 243
Sargis Dallakyan and Arthur J. Olson
Part IV. Small Molecule Target Identification
20 Fluorous Photoaffinity Labeling to Probe Protein-Small
Molecule Interactions ...................................... 253
Weigang Huang and Qisheng Zhang
21 Identification of the Targets of Biologically Active
Small Molecules Using Quantitative Proteomics .............. 263
Gloria Vendrell-Navarro, Andreas Brockmeyer, Herbert
Waldmann, Petra Janning, and Slava Ziegler
22 Drug Affinity Responsive Target Stability (DARTS) for
Small-Molecule Target Identification ....................... 287
Melody Y. Pai, Brett Lomenick, Heejun Hwang, Robert
Schiestl, William McBride, Joseph A. Loo, and Jing Huang
23 Chemical Genomic Profiling via Barcode Sequencing to
Predict Compound Mode of Action ............................ 299
Jeff S. Piotrowski, Scott W. Simpkins, Sheena C. Li,
Raamesh Deshpande, Sean J. McIlwain, Irene M. Ong,
Chad L. Myers, Charlie Boone, and Raymond J. Andersen
24 Image-Based Prediction of Drug Target in Yeast ............. 319
Shinsuke Ohnuki, Hiroki Okada, and Toshikazu Ohya
Index ......................................................... 329
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