Protein Targeting with Small Molecules. Chemical Biology Techniques and Applications. Edited by Hiroyuki Osada.

2010 ◽  
Vol 49 (14) ◽  
pp. 2472-2472 ◽  
Author(s):  
Herbert Waldmann
Keyword(s):  
Small Molecules ◽  
Chemical Biology ◽  
Protein Targeting

scholarly journals Small molecules with big roles in microRNA chemical biology and microRNA-targeted therapeutics

RNA Biology ◽  
2019 ◽  
Vol 16 (6) ◽  
pp. 707-718 ◽  
Author(s):  
Rengen Fan ◽  
Chaocheng Xiao ◽  
Xinqiang Wan ◽  
Wenzhang Cha ◽  
Yufeng Miao ◽  
...  
Keyword(s):  
Small Molecules ◽  
Chemical Biology ◽  
Targeted Therapeutics

Target engagement approaches for pharmacological evaluation in animal models

2019 ◽  
Vol 55 (63) ◽  
pp. 9241-9250 ◽  
Author(s):  
James E. Kath ◽  
Aleksandra Baranczak
Keyword(s):  
Animal Models ◽  
Small Molecules ◽  
Chemical Biology ◽  
Target Engagement ◽  
Pharmacological Evaluation

We highlight recent applications of chemical biology approaches to measure target engagement of small molecules in animal models to support the nomination of clinical candidates.

scholarly journals From Phenotypic Hit to Chemical Probe: Chemical Biology Approaches to Elucidate Small Molecule Action in Complex Biological Systems

Molecules ◽  
2020 ◽  
Vol 25 (23) ◽  
pp. 5702
Author(s):  
Quentin T. L. Pasquer ◽  
Ioannis A. Tsakoumagkos ◽  
Sascha Hoogendoorn
Keyword(s):  
Small Molecules ◽  
Chemical Biology ◽  
Target Identification ◽  
Biologically Active ◽  
Phenotypic Screening ◽  
Biological Processes ◽  
Chemical Probes ◽  
Target Deconvolution ◽  
Cellular Target ◽  
Screening Approaches

Biologically active small molecules have a central role in drug development, and as chemical probes and tool compounds to perturb and elucidate biological processes. Small molecules can be rationally designed for a given target, or a library of molecules can be screened against a target or phenotype of interest. Especially in the case of phenotypic screening approaches, a major challenge is to translate the compound-induced phenotype into a well-defined cellular target and mode of action of the hit compound. There is no “one size fits all” approach, and recent years have seen an increase in available target deconvolution strategies, rooted in organic chemistry, proteomics, and genetics. This review provides an overview of advances in target identification and mechanism of action studies, describes the strengths and weaknesses of the different approaches, and illustrates the need for chemical biologists to integrate and expand the existing tools to increase the probability of evolving screen hits to robust chemical probes.

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