Literature DB >> 19807664

The pilot phase of the NIH Chemical Genomics Center.

Craig J Thomas1, Douglas S Auld, Ruili Huang, Wenwei Huang, Ajit Jadhav, Ronald L Johnson, William Leister, David J Maloney, Juan J Marugan, Sam Michael, Anton Simeonov, Noel Southall, Menghang Xia, Wei Zheng, James Inglese, Christopher P Austin.   

Abstract

The NIH Chemical Genomics Center (NCGC) was the inaugural center of the Molecular Libraries and Screening Center Network (MLSCN). Along with the nine other research centers of the MLSCN, the NCGC was established with a primary goal of bringing industrial technology and experience to empower the scientific community with small molecule compounds for use in their research. We intend this review to serve as 1) an introduction to the NCGC standard operating procedures, 2) an overview of several of the lessons learned during the pilot phase and 3) a review of several of the innovative discoveries reported during the pilot phase of the MLSCN.

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Year:  2009        PMID: 19807664      PMCID: PMC2989597          DOI: 10.2174/156802609789753644

Source DB:  PubMed          Journal:  Curr Top Med Chem        ISSN: 1568-0266            Impact factor:   3.295


  43 in total

1.  The first orally active low molecular weight agonists for the LH receptor: thienopyr(im)idines with therapeutic potential for ovulation induction.

Authors:  N C R van Straten; G G Schoonus-Gerritsma; R G van Someren; J Draaijer; A E P Adang; C M Timmers; R G J M Hanssen; C A A van Boeckel
Journal:  Chembiochem       Date:  2002-10-04       Impact factor: 3.164

2.  Three classes of glucocerebrosidase inhibitors identified by quantitative high-throughput screening are chaperone leads for Gaucher disease.

Authors:  Wei Zheng; Janak Padia; Daniel J Urban; Ajit Jadhav; Ozlem Goker-Alpan; Anton Simeonov; Ehud Goldin; Douglas Auld; Mary E LaMarca; James Inglese; Christopher P Austin; Ellen Sidransky
Journal:  Proc Natl Acad Sci U S A       Date:  2007-08-01       Impact factor: 11.205

3.  A high-throughput screen for aggregation-based inhibition in a large compound library.

Authors:  Brian Y Feng; Anton Simeonov; Ajit Jadhav; Kerim Babaoglu; James Inglese; Brian K Shoichet; Christopher P Austin
Journal:  J Med Chem       Date:  2007-04-21       Impact factor: 7.446

4.  Toxicology. Transforming environmental health protection.

Authors:  Francis S Collins; George M Gray; John R Bucher
Journal:  Science       Date:  2008-02-15       Impact factor: 47.728

5.  Compound Management for Quantitative High-Throughput Screening.

Authors:  Adam Yasgar; Paul Shinn; Ajit Jadhav; Douglas Auld; Sam Michael; Wei Zheng; Christopher P Austin; James Inglese; Anton Simeonov
Journal:  JALA Charlottesv Va       Date:  2008-04

6.  Evaluation of small-molecule modulators of the luteinizing hormone/choriogonadotropin and thyroid stimulating hormone receptors: structure-activity relationships and selective binding patterns.

Authors:  Susanna Moore; Holger Jaeschke; Gunnar Kleinau; Susanne Neumann; Stefano Costanzi; Jian-kang Jiang; John Childress; Bruce M Raaka; Anny Colson; Ralf Paschke; Gerd Krause; Craig J Thomas; Marvin C Gershengorn
Journal:  J Med Chem       Date:  2006-06-29       Impact factor: 7.446

7.  Mechanism of action of novel NO-releasing furoxan derivatives of aspirin in human platelets.

Authors:  Catriona M Turnbull; Clara Cena; Roberta Fruttero; Alberto Gasco; Adriano G Rossi; Ian L Megson
Journal:  Br J Pharmacol       Date:  2006-05-15       Impact factor: 8.739

8.  A 1,536-well-based kinetic HTS assay for inhibitors of Schistosoma mansoni thioredoxin glutathione reductase.

Authors:  Wendy A Lea; Ajit Jadhav; Ganesha Rai; Ahmed A Sayed; Cynthia L Cass; James Inglese; David L Williams; Christopher P Austin; Anton Simeonov
Journal:  Assay Drug Dev Technol       Date:  2008-08       Impact factor: 1.738

9.  A low molecular weight agonist signals by binding to the transmembrane domain of thyroid-stimulating hormone receptor (TSHR) and luteinizing hormone/chorionic gonadotropin receptor (LHCGR).

Authors:  Holger Jäschke; Susanne Neumann; Susanna Moore; Craig J Thomas; Anny-Odile Colson; Stefano Costanzi; Gunnar Kleinau; Jian-Kang Jiang; Ralf Paschke; Bruce M Raaka; Gerd Krause; Marvin C Gershengorn
Journal:  J Biol Chem       Date:  2006-02-16       Impact factor: 5.157

10.  A specific mechanism for nonspecific activation in reporter-gene assays.

Authors:  Douglas S Auld; Natasha Thorne; Dac-Trung Nguyen; James Inglese
Journal:  ACS Chem Biol       Date:  2008-07-01       Impact factor: 5.100

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  8 in total

1.  Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2).

Authors:  Roberta Pireddu; Kara D Forinash; Nan N Sun; Mathew P Martin; Shen-Shu Sung; Brian Alexander; Jin-Yi Zhu; Wayne C Guida; Ernst Schönbrunn; Saïd M Sebti; Nicholas J Lawrence
Journal:  Medchemcomm       Date:  2012-01-27       Impact factor: 3.597

Review 2.  The future of toxicity testing: a focus on in vitro methods using a quantitative high-throughput screening platform.

Authors:  Sunita J Shukla; Ruili Huang; Christopher P Austin; Menghang Xia
Journal:  Drug Discov Today       Date:  2010-08-11       Impact factor: 7.851

Review 3.  Paradigm shift in toxicity testing and modeling.

Authors:  Hongmao Sun; Menghang Xia; Christopher P Austin; Ruili Huang
Journal:  AAPS J       Date:  2012-04-20       Impact factor: 4.009

4.  The NCGC pharmaceutical collection: a comprehensive resource of clinically approved drugs enabling repurposing and chemical genomics.

Authors:  Ruili Huang; Noel Southall; Yuhong Wang; Adam Yasgar; Paul Shinn; Ajit Jadhav; Dac-Trung Nguyen; Christopher P Austin
Journal:  Sci Transl Med       Date:  2011-04-27       Impact factor: 17.956

5.  Intersection of toxicogenomics and high throughput screening in the Tox21 program: an NIEHS perspective.

Authors:  B Alex Merrick; Richard S Paules; Raymond R Tice
Journal:  Int J Biotechnol       Date:  2015

Review 6.  From QSAR to QSIIR: searching for enhanced computational toxicology models.

Authors:  Hao Zhu
Journal:  Methods Mol Biol       Date:  2013

7.  Supporting read-across using biological data.

Authors:  Hao Zhu; Mounir Bouhifd; Elizabeth Donley; Laura Egnash; Nicole Kleinstreuer; E Dinant Kroese; Zhichao Liu; Thomas Luechtefeld; Jessica Palmer; David Pamies; Jie Shen; Volker Strauss; Shengde Wu; Thomas Hartung
Journal:  ALTEX       Date:  2016-02-11       Impact factor: 6.043

8.  Isotonic Regression Based-Method in Quantitative High-Throughput Screenings for Genotoxicity.

Authors:  Yosuke Fujii; Takeo Narita; Raymond Richard Tice; Shunich Takeda; Ryo Yamada
Journal:  Dose Response       Date:  2015-05-04       Impact factor: 2.658

  8 in total

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