Bioneer’s unique Drug Target & Toxicity Identification Services



Drug Target Validation in Human Cells
SAMiRNA in vivo Drug Target Validation

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Features & Benefits of GPScreen™ Services

  • World's unique & innovative technology
  • Identify any classes of drug targets in genome through genome-wide screening
  • Live cell-based screening
  • High throughput screening
  • Rapid; average 20 days for genome-wide screening
  • Accurate, precise & cost-effective
  • Drug target validation services available in human cells (optional !)
  • Applicable to drug repositioning, natural drug target discovery, toxicity profiling

Ⅰ. Introduction

Precise Drug Target Identification is a first step for improving efficacy, tracing and avoiding side-effects as well as understanding the mode-of-actions of drug candidates. However, until now, effective systematic approaches for the precise drug target identification at genome levels have not been commercially available. Using S. pombe genome-wide heterozygous deletion mutant library, Bioneer has developed a high-throughput genome-wide drug target screening service system (GPScreen™) and made it commercially available for your drug discovery needs. GPScreen™ screening service covers a broad spectrum of drug candidates in whole disease areas from cancers & metabolic diseases to neglected & rare diseases and, therefore, will provide the total solutions for an efficient drug discovery through providing clear-cut answers to problems such as drug-target(s) and toxicity as well as mode-of-actions of drug candidates.

KOG Analysis of S.pombe Genome

“Bioneer’s GPScreen™ using S. pombe genome-wide heterozygous deletion mutant library
has enabled genome-wide screening for drug target identification”

GPScreen™ is based on Bioneer’s unique S. pombe genome-wide deletion mutant library, which was developed by Bioneer and the Korea Research Institute of Bioscience & Biotechnology (KRIBB) in collaboration with Dr. Paul Nurse of Cancer Research Center UK (Nat. Biotech, 28, 617–623 (2010)). It can be used for genetic and chemical screening such as drug target identification, gene expression profiling and synthetic lethal profiling.

This mutant library comprised of a total of 4,840 heterozygous diploid deletion mutants representing 98.5% genome coverage and one copy of a specific gene in each mutant was deleted by homologous recombination. GPScreen™ exclusively offers S. pombe deletion mutant library as a powerful tool for large-scale genetic functional analysis, identification and verification research of drug targets and for integrated systems research of cell function.

Ⅱ. Principle of GPScreen

"Drug-induced Haploinsufficiency (DIH)" is a situation in which a strain with a heterozygous gene deletion (producing target proteins to about half of normal levels), result in cells sensitive to a specific drug. DIH occurs when a drug or drug candidate acts on a mutant strain in which the level of target gene protein is lowered from normal to half level, and is considered to be a valuable tool for drug target identification. Previously, a number of reports have provided identifications of drug targets using DIH in budding yeast S. cerevisiae (Baetz K et al., 2004; Lum et al., 2004). However, fission yeast S. pombe is considered a better model of mammalian cells since its cell cycle regulation is closer to that of mammalian cells than that of S. cerevisiae

GPScreen™ utilizes DIH in the fission yeast S. pombe genome-wide heterozygous deletion mutant library to identify the drug target(s).


• Baetz K et al. Yeast genome-wide drug-induced haploinsufficiency screen to determine drug mode of action. PNAS. 2004
  [More information]

• Lum PY et al. Discovering modes of action for therapeutic compounds using a genome-wide screen of yeast heterozygotes.
  Cell. 2004
   [More information]

Ⅲ. Performance of GPScreen

GPScreen™ is a best-in class genome-wide drug target identification system that is exclusively offered by Bioneer Inc. It allows for the clear-cut identification of molecular targets of drugs/ drug candidates (A representative is below). Figure 1. Drug Target Identification using GPScreen™.
In the presence of cytochalasin A (Fig. 1A), a heterozygous deletion mutant of act1 shows decreased growth as a result of a decrease in “functional” Act1 protein. act1 was the only gene in the genome-wide screen to show this effect, demonstrating that act1 is a target of cytochalasin A (Fig. 1B).

Ⅳ. Applications of GPScreen

 Toxicity profiling and Drug Prioritization
 Drug Repositioning and Enhancement
 Natural Drug Target Discovery
 Chemogenomic profiling

Toxicity profiling using GPScreen™ at early stage of drug development would accommodate 'Drug Prioritization' among drug candidates very efficiently, thereby reducing time and money dramatically in the later stage of drug discovery.

V. Flow chart of GPScreen™ Service