The development of small-molecule modulators for ClpP protease activity

2017 ◽  
Vol 13 (1) ◽  
pp. 23-31 ◽  
Author(s):  
Fei Ye ◽  
Jiahui Li ◽  
Cai-Guang Yang
Keyword(s):  
Antibacterial Activity ◽  
Small Molecule ◽  
Protease Activity ◽  
Small Molecule Modulators

Deregulating ClpP activity either through inhibition or overactivation could lead to antibacterial activity.

scholarly journals Small-molecule modulators of inward rectifier K+channels: recent advances and future possibilities

2010 ◽  
Vol 2 (5) ◽  
pp. 757-774 ◽  
Author(s):  
Gautam Bhave ◽  
Daniel Lonergan ◽  
Brian A Chauder ◽  
Jerod S Denton
Keyword(s):  
Small Molecule ◽  
Inward Rectifier ◽  
K Channels ◽  
Recent Advances ◽  
Small Molecule Modulators

Polyamines: Naturally occurring small molecule modulators of electrostatic protein–protein interactions

2010 ◽  
Vol 104 (2) ◽  
pp. 118-125 ◽  
Author(s):  
Anja Berwanger ◽  
Susanne Eyrisch ◽  
Inge Schuster ◽  
Volkhard Helms ◽  
Rita Bernhardt
Keyword(s):  
Small Molecule ◽  
Protein Interactions ◽  
Protein Protein Interactions ◽  
Naturally Occurring ◽  
Small Molecule Modulators

scholarly journals Fluorescent Probes with Unnatural Amino Acids to Monitor Proteasome Activity in Real-Time

2020 ◽  
Author(s):  
Breanna L. Zerfas ◽  
Rachel A. Coleman ◽  
Andres Salazar Chaparro ◽  
Nathaniel J. Macatangay ◽  
Darci Trader
Keyword(s):  
Amino Acids ◽  
Small Molecule ◽  
Fluorescent Probes ◽  
Unnatural Amino Acids ◽  
Cell Types ◽  
Proteasome Activity ◽  
Live Cells ◽  
Fluorescent Substrate ◽  
The Individual ◽  
Small Molecule Modulators

<div> <div> <div> <p>The proteasome is an essential protein complex that, when dysregulated, can result in various diseases in eukaryotic cells. As such, understanding the enzymatic activity of the proteasome and what can alter it is crucial to elucidating its roles in these diseases. This can be done effectively by using activity-based fluorescent substrate probes, of which there are many commercially available that target the individual protease-like subunits in the 20S CP of the proteasome. Unfortunately, these probes have not displayed appropriate characteristics for their use in live cell-based assays. In the work presented here, we have developed a set of probes which have shown improved fluorescence properties and selectivity towards the proteasome compared to other cellular proteases. By including unnatural amino acids, we have found probes which can be utilized in various applications, including monitoring the effects of small molecule stimulators of the proteasome in live cells and comparing the relative proteasome activity across different cancer cell types. In future studies, we expect the fluorescent probes presented here will serve as tools to support the discovery and characterization of small molecule modulators of proteasome activity. </p> </div> </div> </div>

scholarly journals Detection of Small-Molecule Modulators of Actin-Myosin Structure and Function using High-Throughput Time-Resolved FRET

2017 ◽  
Vol 112 (3) ◽  
pp. 237a
Author(s):  
Piyali Guhathakurta ◽  
Ewa Prochniewicz ◽  
Kurt C. Peterson ◽  
Benjamin D. Grant ◽  
Gregory D. Gillispie ◽  
...  
Keyword(s):  
Small Molecule ◽  
High Throughput ◽  
Structure And Function ◽  
Throughput Time ◽  
Time Resolved ◽  
Small Molecule Modulators ◽  
And Function
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