Abstract

UNIT 2. HIGH-THROUGHPUT SCREENING The HTS Unit has extensive expertise in performing biochemical and cell-based assays and exceeded its commitment to the MLSCN, thus far uploading >3.4 million data points into PubChem from 36 screening campaigns using the NIH library, plus another 3 screening campaigns using Burnham's in-house library, when the NIH library failed to yield tractable hits (total 39). We describe progress to date and plans to perform a minimum 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 #
5U54HG005033-05
Application #
8379687
Study Section
Special Emphasis Panel (ZRG1-IFCN-K)
Project Start
Project End
2014-05-31
Budget Start
2012-06-01
Budget End
2013-05-31
Support Year
5
Fiscal Year
2012
Total Cost
$638,236
Indirect Cost
$304,081

  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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