The maturation of DNA encoded libraries: opportunities for new users

2020 ◽  
Author(s):  
Daniel Conole ◽  
James H Hunter ◽  
Michael J Waring
Keyword(s):  
Data Analysis ◽  
Cost Effectiveness ◽  
Drug Discovery ◽  
High Throughput ◽  
High Throughput Screening ◽  
New Technology ◽  
Combinatorial Libraries ◽  
Library Design ◽  
First Time ◽  
Screening Technology

DNA-encoded combinatorial libraries (DECLs) represent an exciting new technology for high-throughput screening, significantly increasing its capacity and cost–effectiveness. Historically, DECLs have been the domain of specialized academic groups and industry; however, there has recently been a shift toward more drug discovery academic centers and institutes adopting this technology. Key to this development has been the simplification, characterization and standardization of various DECL subprotocols, such as library design, affinity screening and data analysis of hits. This review examines the feasibility of implementing DECL screening technology as a first-time user, particularly in academia, exploring the some important considerations for this, and outlines some applications of the technology that academia could contribute to the field.

Abstract 4206: Utilizing a Drosophila high throughput screening technology for cancer drug discovery

2010 ◽  
Author(s):  
Elena M. Gracheva ◽  
Eduardo J. Martinez ◽  
Jill Thompson ◽  
Dominick Thompson ◽  
Ross L. Cagan
Keyword(s):  
Drug Discovery ◽  
High Throughput ◽  
High Throughput Screening ◽  
Cancer Drug ◽  
Cancer Drug Discovery ◽  
Screening Technology

High Throughput Screening for Drug Discovery: Continually Transitioning into New Technology

1999 ◽  
Vol 4 (4) ◽  
pp. 183-186 ◽  
Author(s):  
Sandra Fox ◽  
Shauna Farr-Jones ◽  
Mary Alice Yund
Keyword(s):  
Drug Discovery ◽  
Virtual Screening ◽  
High Throughput ◽  
High Throughput Screening ◽  
New Technology ◽  
Microfluidic Chips ◽  
Automated Systems ◽  
Enabling Technologies ◽  
Drug Leads ◽  
Homogeneous Assays

Those working in HTS laboratories, pressured to find increasing numbers of drug leads while containing costs, are seeking larger compound sets, more automated systems to screen them faster, and an integrated set of equipment and consumables. Enabling technologies are continually being developed and suppliers are teaming up to supply integrated equipment and consumable sets. Miniaturization, microfluidic chips, subnanoliter dispensing, fluorescence, homogeneous assays for HTS, and virtual screening are just some of the evolving tools that HTS experts are continually evaluating and incorporating into drug discovery operations.

Upscaling and Automation of Electrophysiology: Toward High Throughput Screening in Ion Channel Drug Discovery

2003 ◽  
Vol 9 (1) ◽  
pp. 49-58
Author(s):  
Margit Asmild ◽  
Nicholas Oswald ◽  
Karen M. Krzywkowski ◽  
Søren Friis ◽  
Rasmus B. Jacobsen ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Ion Channel ◽  
High Throughput ◽  
High Throughput Screening

High-Throughput Affinity Selection Mass Spectrometry Using SAMDI-MS to Identify Small-Molecule Binders of the Human Rhinovirus 3C Protease

2021 ◽  
pp. 247255522110232
Author(s):  
Michael D. Scholle ◽  
Doug McLaughlin ◽  
Zachary A. Gurard-Levin
Keyword(s):  
Mass Spectrometry ◽  
Drug Discovery ◽  
High Throughput ◽  
High Throughput Screening ◽  
Human Rhinovirus ◽  
Binding Potential ◽  
Affinity Selection ◽  
Response Curves ◽  
Desorption Ionization ◽  
Self Assembled

Affinity selection mass spectrometry (ASMS) has emerged as a powerful high-throughput screening tool used in drug discovery to identify novel ligands against therapeutic targets. This report describes the first high-throughput screen using a novel self-assembled monolayer desorption ionization (SAMDI)–ASMS methodology to reveal ligands for the human rhinovirus 3C (HRV3C) protease. The approach combines self-assembled monolayers of alkanethiolates on gold with matrix-assisted laser desorption ionization time-of-flight (MALDI TOF) mass spectrometry (MS), a technique termed SAMDI-ASMS. The primary screen of more than 100,000 compounds in pools of 8 compounds per well was completed in less than 8 h, and informs on the binding potential and selectivity of each compound. Initial hits were confirmed in follow-up SAMDI-ASMS experiments in single-concentration and dose–response curves. The ligands identified by SAMDI-ASMS were further validated using differential scanning fluorimetry (DSF) and in functional protease assays against HRV3C and the related SARS-CoV-2 3CLpro enzyme. SAMDI-ASMS offers key benefits for drug discovery over traditional ASMS approaches, including the high-throughput workflow and readout, minimizing compound misbehavior by using smaller compound pools, and up to a 50-fold reduction in reagent consumption. The flexibility of this novel technology opens avenues for high-throughput ASMS assays of any target, thereby accelerating drug discovery for diverse diseases.

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