The high-throughput screening core will continue to carry out screening of small-molecule libraries against defined targets or phenotypes. Resources of the core at present include more than 250,000 drug-like compounds and smaller collections of purified natural compounds and approved/investigational drugs, and automated instrumentation for high-throughput screening utilizing optical (fluorescence, absorbance, luminescence) assays. Functions of the core include compound storage and handling, assay design and validation, assay execution, and data analysis. Initial optimization of validated 'hits' (compounds with activity against defined targets or phenotypes) is done by screening of commercially purchased compound analogs. Further 'hit-to-lead' development is done in individual projects in consultation with the core. The core has been utilized extensively during the current project with successful identification and characterization of novel modulators of ion transporters and infection. The core will be heavily utilized by 28 ongoing and new CF related projects.

Agency
National Institute of Health (NIH)
Institute
National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)
Type
Center Core Grants (P30)
Project #
5P30DK072517-08
Application #
8564917
Study Section
Special Emphasis Panel (ZDK1-GRB-W (M2))
Project Start
2012-06-01
Project End
2015-05-31
Budget Start
2012-06-01
Budget End
2013-05-31
Support Year
8
Fiscal Year
2012
Total Cost
$160,692
Indirect Cost
$48,921
Name
University of California San Francisco
Department
Type
DUNS #
094878337
City
San Francisco
State
CA
Country
United States
Zip Code
94143
Yao, Xiaoming; Verkman, Alan S (2017) Complement regulator CD59 prevents peripheral organ injury in rats made seropositive for neuromyelitis optica immunoglobulin G. Acta Neuropathol Commun 5:57
Cil, Onur; Phuan, Puay-Wah; Gillespie, Anne Marie et al. (2017) Benzopyrimido-pyrrolo-oxazine-dione CFTR inhibitor (R)-BPO-27 for antisecretory therapy of diarrheas caused by bacterial enterotoxins. FASEB J 31:751-760
Truong, Eric C; Phuan, Puay W; Reggi, Amanda L et al. (2017) Substituted 2-Acylaminocycloalkylthiophene-3-carboxylic Acid Arylamides as Inhibitors of the Calcium-Activated Chloride Channel Transmembrane Protein 16A (TMEM16A). J Med Chem 60:4626-4635
Son, Jung-Ho; Zhu, Jie S; Phuan, Puay-Wah et al. (2017) High-Potency Phenylquinoxalinone Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Activators. J Med Chem 60:2401-2410
Tradtrantip, Lukmanee; Jin, Bjung-Ju; Yao, Xiaoming et al. (2017) Aquaporin-Targeted Therapeutics: State-of-the-Field. Adv Exp Med Biol 969:239-250
Felix, Christian M; Lee, Sujin; Levin, Marc H et al. (2017) Pro-Secretory Activity and Pharmacology in Rabbits of an Aminophenyl-1,3,5-Triazine CFTR Activator for Dry Eye Disorders. Invest Ophthalmol Vis Sci 58:4506-4513
Lee, Sujin; Phuan, Puay-Wah; Felix, Christian M et al. (2017) Nanomolar-Potency Aminophenyl-1,3,5-triazine Activators of the Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Chloride Channel for Prosecretory Therapy of Dry Eye Diseases. J Med Chem 60:1210-1218
Verkman, Alan S; Tradtrantip, Lukmanee; Smith, Alex J et al. (2017) Aquaporin Water Channels and Hydrocephalus. Pediatr Neurosurg 52:409-416
Haggie, Peter M; Phuan, Puay-Wah; Tan, Joseph-Anthony et al. (2017) Correctors and Potentiators Rescue Function of the Truncated W1282X-Cystic Fibrosis Transmembrane Regulator (CFTR) Translation Product. J Biol Chem 292:771-785
Cil, Onur; Phuan, Puay-Wah; Son, Jung-Ho et al. (2017) Phenylquinoxalinone CFTR activator as potential prosecretory therapy for constipation. Transl Res 182:14-26.e4

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