Target identification for biologically active small molecules using chemical biology approaches

@article{Lee2016TargetIF,
  title={Target identification for biologically active small molecules using chemical biology approaches},
  author={Heesu Lee and Jae Wook Lee},
  journal={Archives of Pharmacal Research},
  year={2016},
  volume={39},
  pages={1193-1201}
}
  • Heesu Lee, J. Lee
  • Published 8 July 2016
  • Biology, Medicine
  • Archives of Pharmacal Research
The identification and validation of the targets of biologically active molecules is an important step in the field of chemical biology. While recent advances in proteomic and genomic technology have accelerated this identification process, the discovery of small molecule targets remains the most challenging step. A general method for the identification of these small molecule targets has not yet been established. To overcome the difficulty in target identification, new technology derived from… Expand

Topics from this paper

Target Engagement of Small Molecules: Thermal Profiling Approaches on Different Levels.
TLDR
The CETSA approach requires preknowledge about possible target proteins and can only detect a few proteins at once, but an unbiased approach based on a proteome-wide mass spectrometric analysis (thermal proteome profiling, TPP) allows for the identification of multiple (off)targets without any preknowledge. Expand
Identification and validation nucleolin as a target of curcumol in nasopharyngeal carcinoma cells.
TLDR
The effectiveness of chemical proteomics approaches in natural drugs molecular target identification is demonstrated, revealing that the anti-cancer effects of curcumol in NPC cells are mediated, at least in part, by NCL inhibition. Expand
An in silico Approach for Integrating Phenotypic and Target‐based Approaches in Drug Discovery
TLDR
A new in silico method that can computationally execute target deconvolution considering polypharmacology and can provide keys for understanding the pathway and mechanism from compound to phenotype, thereby promoting drug discovery. Expand
berriak aurkitzeko ( Protein analysis through thermal denaturation for the discovery of new bioactive compounds )
Bioactive compounds are either natural or synthetic chemicals that can affect both the cellular and/or physiological activity in living organisms. Included among these are, for example, drugs thatExpand
Natural Products for Drug Discovery in the 21st Century: Innovations for Novel Drug Discovery
TLDR
This review discusses plant-based natural product drug discovery and how innovative technologies play a role in next-generation drug discovery. Expand
Opportunities and challenges in phenotypic drug discovery: an industry perspective
TLDR
This article focuses on the lessons learned by researchers engaged in PDD in the pharmaceutical industry and considers the impact of 'omics' knowledge in defining a cellular disease phenotype in the era of precision medicine, introducing the concept of a chain of translatability. Expand
In silico systems for predicting chemical-induced side effects using known and potential chemical protein interactions, enabling mechanism estimation.
TLDR
Novel in silico models to predict chemical-induced side effects and estimate the underlying mechanisms with high general versatility by integrating the comprehensive prediction of potential chemical-protein interactions (CPIs) with machine learning are constructed. Expand
Advancement of multi-target drug discoveries and promising applications in the field of Alzheimer's disease.
TLDR
The authors review the recent progress made in the discovery and design processes of selective multi-targeted agents, especially the successful application of multi- target drugs for the treatment of Alzheimer's disease. Expand
The Role of Natural Products as Sources of Therapeutic Agents for Innovative Drug Discovery
  • K. Dzobo
  • Medicine
  • Reference Module in Biomedical Sciences
  • 2021
TLDR
The biosynthesis and screening of natural products during drug discovery as well as methods used in studying natural products are described, offering an opportunity to discover new compounds that can be converted into drugs given their chemical structure diversity. Expand
Cyclin-dependent kinase 12, a novel drug target for visceral leishmaniasis
TLDR
Development of an anti-leishmanial drug-like chemical series based on a pyrazolopyrimidine scaffold is described, and cdc2-related kinase 12 (CRK12) is identified as the probable primary drug target for visceral leishmaniasis. Expand
...
1
2
3
...

References

SHOWING 1-10 OF 63 REFERENCES
Target deconvolution of bioactive small molecules: the heart of chemical biology and drug discovery
TLDR
A systematic approach that involves the combination of multi-omics-based target identification and validation and preclinical target validation is proposed to obtain an integrated view of the mechanisms of action of small molecules. Expand
Affinity-based target identification for bioactive small molecules
Identification of the cellular targets of bioactive small molecules is a crucial step in drug discovery and chemical genetics. Classical affinity purification with small-molecule affinity probesExpand
Target identification for small bioactive molecules: finding the needle in the haystack.
TLDR
Current methods for target identification of small molecules are summarized, primarily for a chemistry audience but also the biological community, for example, the chemist or biologist attempting to identify the target of a given bioactive compound. Expand
Identification of Direct Protein Targets of Small Molecules
TLDR
The DARTS method is reviewed, why it works, and new perspectives for future development in this area are provided. Expand
Target identification of biologically active small molecules via in situ methods.
TLDR
Some of the recent advances in target identification of bioactive molecules (including drugs and natural products) using in situ methods for cell-based proteome profiling of potential on and off targets are summarized. Expand
Target identification of small molecules based on chemical biology approaches.
TLDR
Recent progress in both affinity-based (direct) and phenotypic profiling (indirect) approaches for chemical biology target identification are described and summarized. Expand
Discovery of new small molecules and targets towards angiogenesis via chemical genomics approach.
  • H. Kwon
  • Chemistry, Medicine
  • Current drug targets
  • 2006
TLDR
This work has applied chemical genomics to angiogenesis, a new blood vessel formation, resulting in the identification of new small molecules as well as targets, and its application towards a cellular phenotype, angiogenic, will be demonstrated. Expand
Identification and validation of bioactive small molecule target through phenotypic screening.
TLDR
The combination of phenotypic screening in combination with multi-omics-based target identification and validation will provide an effective approach to discover new bioactive small molecules and their target protein and mechanism identification. Expand
Proteomic methods for drug target discovery.
TLDR
Significant progress has been made in this rapidly advancing field, speeding the clinical validation of drug candidates and the discovery of the novel targets for lead compounds developed using cell-based phenotypic screens. Expand
Target identification and mechanism of action in chemical biology and drug discovery.
TLDR
This work focuses on target-identification and mechanism-of-action studies, which allow small-molecule action to be tested in a more disease-relevant setting at the outset, but require follow-up studies to determine the precise protein target or targets responsible for the observed phenotype. Expand
...
1
2
3
4
5
...