The High-Throughput Screening (HTS) Core carries out target- and phenotype-based screens of small- molecule libraries. The HTS core will support the activities of twelve CF-related screening projects, including correctors and potentiators of ?F508-CFTR, and various CF-relevant ion transport and inflammation targets. The instrumentation available for screening includes a fully automated screening platform with liquid handling and two plate readers, and two separate plate readers with stackers. Plate-readers provide fluorescence, polarization, absorbance, and luminescence readout. Functions of the Core include compound storage and handling, assay design and validation, assay execution, and data analysis. Core resources also include HPLC, LC/MS, and NMR instrumentation for compound quality control. The Core also carries out optimization of validated initial `hits' (active compounds) by screening commercially available analogs. Further `hit-to-lead' development is done on individual projects in consultation with the Synthesis Core (Core C). Having operated the HTS Core for the past 9 years, the Core established practical procedures for efficient and cost-effective compound screening, quality control, and hit-to-lead optimization.
The High-Throughput Screening Core carries out target- and phenotype-based screens of small-molecule libraries in order to identify new drug candidates for cystic fibrosis therapy. The functions of the Core include compound storage and handling, assay design and validation, assay execution and data analysis.
|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|
Showing the most recent 10 out of 263 publications