Corpus ID: 23146755

Target validation: A door to drug discovery.

@article{Chen2007TargetVA,
  title={Target validation: A door to drug discovery.},
  author={Xiao-hong Chen and Guo-hua Du},
  journal={Drug discoveries \& therapeutics},
  year={2007},
  volume={1 1},
  pages={
          23-9
        }
}
  • X. Chen, G. Du
  • Published 2007
  • Computer Science, Medicine
  • Drug discoveries & therapeutics
From ancient times to today, drug discovery transitioned from serendipity to rationality over its long history. Proper drug target selection and validation are crucial to the discovery of new drugs. This review discusses the definition of drug targets and proposes several characteristics for drug targets. The limitations of the term 'target' itself are summarized. The drug target validation process is also discussed in detail and pitfalls during this process are outlined. Small active chemical… Expand
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References

SHOWING 1-10 OF 26 REFERENCES
Evaluation and validation of drug targets
TLDR
This work states that based on the knowledge of molecular biology, human genomics and proteomics, it has been predicted that 5000 to 10000 drug targets exist in human and it is important to evaluate and validate the drug targets. Expand
How many drug targets are there?
TLDR
A consensus number of current drug targets for all classes of approved therapeutic drugs is proposed, and an emerging realization of the importance of polypharmacology and also the power of a gene-family-led approach in generating novel and important therapies is highlighted. Expand
High‐Throughput Screening for Lead Discovery
TLDR
The process of bioassay design, screen construction, hit identification, and compound profiling is the basic backbone of the lead discovery process, and is underpinned by a set of large scale, novel technologies that provide a seamless, highly efficient discovery process. Expand
Tools for target identification and validation.
TLDR
Besides being used as an essential step in analyzing high-throughput experiments such as those involving microarrays, bioinformatics can also contribute to the processes of target identification and validation by providing functional information about target candidates and positioning information to biological networks. Expand
Drug Discovery Handbook
This comprehensive, practical guide presents an explanation of the latest techniques and methods in drug discovery, including: • Genomics, proteomics, high-throughput screening, and systems biology •Expand
Drugs, their targets and the nature and number of drug targets
TLDR
This work considers the nature of drug targets, and by classifying known drug substances on the basis of the discussed principles it provides an estimation of the total number of current drug targets. Expand
High-throughput fluorescence polarization method for identifying ligands of LOX-1
TLDR
The established competitive FP-based assay is sensitive, stable, highly reproducible and robust, and suitable for HTS for ligands of the hLOX-1 receptor. Expand
Lectin‐like oxidized low‐density lipoprotein receptor‐1: protein, ligands, expression and pathophysiological significance
TLDR
Identification of LOX‐1 and a definition of its biological role in pathophysiologic states provide deeper insight into the pathogenesis of some cardiovascular diseases especially in atherosclerosis and provide a potential selective therapeutic approach. Expand
Lectin-like oxidized low-density lipoprotein receptor-1, a new promising target for the therapy of atherosclerosis?
TLDR
Identification and regulation of LOX-1 and understanding its signal transduction pathways might improve the insight toward the pathogenesis of atherosclerosis and provide a selective treatment approach. Expand
The expression of recombinant human LOX-1 and identifying its mimic ligands by fluorescence polarization-based high throughput screening.
TLDR
The preliminary results indicated that isolated mimic ligands may act as a function of antagonist and the discovery of human LOX-1 mimic ligand would benefit to further study the function of LOx-1 and identify a novel avenue for prevention and treatment atherosclerosis. Expand
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