Abstract

UNIT 2. HIGH-THROUGHPUT SCREENINGThe HTS Unit has extensive expertise in performing biochemical and cell-based assays and exceeded itscommitment to the MLSCN, thus far uploading >3.4 million data points into PubChem from 36 screeningcampaigns using the NIH library, plus another 3 screening campaigns using Burnham's in-house library, whenthe NIH library failed to yield tractable hits (total 39). We describe progress to date and plans to perform aminimum of 25 screens per year using the NIH library of 300K-500K compounds during the MLPCN Phase.

  Funding Agency

Agency
National Institute of Health (NIH)
Institute
National Human Genome Research Institute (NHGRI)
Type
Specialized Center--Cooperative Agreements (U54)
Project #
1U54HG005033-01
Application #
7695867
Study Section
Special Emphasis Panel (ZRG1-IFCN-K (52))
Project Start
2008-09-01
Project End
2014-05-31
Budget Start
2008-09-01
Budget End
2009-05-31
Support Year
1
Fiscal Year
2008
Total Cost
$1,943,915
Indirect Cost

  Institution

Name
Sanford-Burnham Medical Research Institute
Department
Type
DUNS #
020520466
City
La Jolla
State
CA
Country
United States
Zip Code
92037

  Publications

Lv, Zongyang; Yuan, Lingmin; Atkison, James H et al. (2018) Molecular mechanism of a covalent allosteric inhibitor of SUMO E1 activating enzyme. Nat Commun 9:5145
Pinkerton, Anthony B; Sergienko, Eduard; Bravo, Yalda et al. (2018) Discovery of 5-((5-chloro-2-methoxyphenyl)sulfonamido)nicotinamide (SBI-425), a potent and orally bioavailable tissue-nonspecific alkaline phosphatase (TNAP) inhibitor. Bioorg Med Chem Lett 28:31-34
Pagano, Nicholas; Teriete, Peter; Mattmann, Margrith E et al. (2017) An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors. Bioorg Med Chem 25:6248-6265
Oellrich, Anika; Collier, Nigel; Groza, Tudor et al. (2016) The digital revolution in phenotyping. Brief Bioinform 17:819-30
Ma, Chen-Ting; Sergienko, Eduard A (2016) Time-Resolved Fluorescence Assays. Methods Mol Biol 1439:131-42
Roy, Sudeshna; Šileikyt?, Justina; Neuenswander, Benjamin et al. (2016) N-Phenylbenzamides as Potent Inhibitors of the Mitochondrial Permeability Transition Pore. ChemMedChem 11:283-8
Barak, Larry S; Bai, Yushi; Peterson, Sean et al. (2016) ML314: A Biased Neurotensin Receptor Ligand for Methamphetamine Abuse. ACS Chem Biol 11:1880-90
Schreiber, Stuart L; Kotz, Joanne D; Li, Min et al. (2015) Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes. Cell 161:1252-65
Tautz, Lutz; Senis, Yotis A; Oury, Cécile et al. (2015) Perspective: Tyrosine phosphatases as novel targets for antiplatelet therapy. Bioorg Med Chem 23:2786-97
Alontaga, Aileen Y; Li, Yifei; Chen, Chih-Hong et al. (2015) Design of high-throughput screening assays and identification of a SUMO1-specific small molecule chemotype targeting the SUMO-interacting motif-binding surface. ACS Comb Sci 17:239-46

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