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Dynamic Compound-Dependent Acoustic Transfer to Investigate Inhibitor Reversibility.
Nothstein, Jennifer; MacColl, Elisabeth; Zuck, Paul; Cassaday, Jason; Uebele, Victor N; Hermes, Jeffrey D; Homsher, Michelle F.
Afiliación
  • Nothstein J; 1 Screening and Protein Sciences, Merck Research Laboratories, North Wales, PA, USA.
  • MacColl E; 2 Hamilton College, Clinton, NY, USA.
  • Zuck P; 1 Screening and Protein Sciences, Merck Research Laboratories, North Wales, PA, USA.
  • Cassaday J; 1 Screening and Protein Sciences, Merck Research Laboratories, North Wales, PA, USA.
  • Uebele VN; 1 Screening and Protein Sciences, Merck Research Laboratories, North Wales, PA, USA.
  • Hermes JD; 1 Screening and Protein Sciences, Merck Research Laboratories, North Wales, PA, USA.
  • Homsher MF; 1 Screening and Protein Sciences, Merck Research Laboratories, North Wales, PA, USA.
SLAS Technol ; 22(5): 485-492, 2017 10.
Article en En | MEDLINE | ID: mdl-28027447
Automated mechanism of action studies are introducing the need for tailored compound delivery, which can be challenging for standard compound management procedures. Jump dilution assays investigating inhibitor reversibility require compound delivery at specific volumes to assay specific concentrations of 10 × IC50 for each inhibitor. Creating custom-made source plates with unique compound concentrations to dispense a uniform single volume can be prohibitively slow. A broadly applicable tool that enables on-the fly dispensing of variable amounts of stock concentrations was developed using the Acoustic Transfer System (ATS). The Dynamic Transfer Modification Program (DTMP) is an integrated LabVIEW program used to automate customized volume transfers from each well based on compound identity within a given source plate. A jump dilution investigating the time-dependent inhibition of the enzyme dipeptidyl peptidase-4 (DPP4) with multiple inhibitors is described here to demonstrate the delivery of specific volumes of various compounds in a high-throughput manner. The ability to automate this process allows for the characterization of inhibitor reversibility earlier in the drug discovery process, resulting in better informed lead candidate selection.
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Texto completo: 1 Base de datos: MEDLINE Asunto principal: Acústica / Técnicas de Dilución del Indicador / Dipeptidil Peptidasa 4 / Inhibidores de la Dipeptidil-Peptidasa IV / Descubrimiento de Drogas Idioma: En Revista: SLAS Technol Año: 2017 Tipo del documento: Article

Texto completo: 1 Base de datos: MEDLINE Asunto principal: Acústica / Técnicas de Dilución del Indicador / Dipeptidil Peptidasa 4 / Inhibidores de la Dipeptidil-Peptidasa IV / Descubrimiento de Drogas Idioma: En Revista: SLAS Technol Año: 2017 Tipo del documento: Article