chemical genetics
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Author(s):  
Yasushi Takemoto ◽  
Shin Kadota ◽  
Itsunari Minami ◽  
Shinya Otsuka ◽  
Satoshi Okuda ◽  
...  

2021 ◽  
Author(s):  
Yasushi Takemoto ◽  
Shin Kadota ◽  
Itsunari Minami ◽  
Shinya Otsuka ◽  
Satoshi Okuda ◽  
...  

2021 ◽  
Vol 95 (15) ◽  
Author(s):  
Kin Kui Lai ◽  
Nam Nam Cheung ◽  
Fang Yang ◽  
Jun Dai ◽  
Li Liu ◽  
...  

2021 ◽  
Vol 10 (2) ◽  
Author(s):  
Phelps Tin ◽  
Sam Kunes

SARS-CoV2 continues to affect the lives of the majority of the world, and although vaccines are beginning to become available, much of the world will still be unable to obtain them. Furthermore, some studies have suggested that there may have to be annual vaccines and as strains of the virus continue to increase, it is essential for us to move to the next stage of research and attempt to better understand the virus. By utilizing a chemical genetics approach where numerous ligands of distinct chemical libraries are screened through high-throughput screening, we may be able to form an ordered viral cycle of metabolic events that could help identify drug targets more efficiently and coordinate drug use to improve efficacy. A modified version of the virus (to decrease its ability of infection) along with the URA3 protein is then inserted into yeast cells (Saccharomyces cerevisiae) and screened. A simple assay involving the addition of 5’- fluoroorotic acid helps to determine ligand interference and after identifying the compounds, we can order their action into specific steps in the lifecycle and order the events of the life cycle.


Antibiotics ◽  
2021 ◽  
Vol 10 (5) ◽  
pp. 565
Author(s):  
Bernardo Ribeiro da Cunha ◽  
Paulo Zoio ◽  
Luís P. Fonseca ◽  
Cecília R. C. Calado

There are two main strategies for antibiotic discovery: target-based and phenotypic screening. The latter has been much more successful in delivering first-in-class antibiotics, despite the major bottleneck of delayed Mechanism-of-Action (MOA) identification. Although finding new antimicrobial compounds is a very challenging task, identifying their MOA has proven equally challenging. MOA identification is important because it is a great facilitator of lead optimization and improves the chances of commercialization. Moreover, the ability to rapidly detect MOA could enable a shift from an activity-based discovery paradigm towards a mechanism-based approach. This would allow to probe the grey chemical matter, an underexplored source of structural novelty. In this study we review techniques with throughput suitable to screen large libraries and sufficient sensitivity to distinguish MOA. In particular, the techniques used in chemical genetics (e.g., based on overexpression and knockout/knockdown collections), promoter-reporter libraries, transcriptomics (e.g., using microarrays and RNA sequencing), proteomics (e.g., either gel-based or gel-free techniques), metabolomics (e.g., resourcing to nuclear magnetic resonance or mass spectrometry techniques), bacterial cytological profiling, and vibrational spectroscopy (e.g., Fourier-transform infrared or Raman scattering spectroscopy) were discussed. Ultimately, new and reinvigorated phenotypic assays bring renewed hope in the discovery of a new generation of antibiotics.


2021 ◽  
Vol 8 ◽  
Author(s):  
Matylda Anna Izert ◽  
Maria Magdalena Klimecka ◽  
Maria Wiktoria Górna

A repertoire of proteolysis-targeting signals known as degrons is a necessary component of protein homeostasis in every living cell. In bacteria, degrons can be used in place of chemical genetics approaches to interrogate and control protein function. Here, we provide a comprehensive review of synthetic applications of degrons in targeted proteolysis in bacteria. We describe recent advances ranging from large screens employing tunable degradation systems and orthogonal degrons, to sophisticated tools and sensors for imaging. Based on the success of proteolysis-targeting chimeras as an emerging paradigm in cancer drug discovery, we discuss perspectives on using bacterial degraders for studying protein function and as novel antimicrobials.


Author(s):  
Tommaso Cupido ◽  
Natalie H. Jones ◽  
Michael J. Grasso ◽  
Rudolf Pisa ◽  
Tarun M. Kapoor
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