lead evolution
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2020 ◽  
Vol 7 ◽  
Author(s):  
Anthony Martino ◽  
Olivier Darbin ◽  
Kelsey Templeton ◽  
Daniel Dees ◽  
Markus Lammle ◽  
...  

2019 ◽  
Vol 20 (13) ◽  
pp. 3230 ◽  
Author(s):  
Gilbert Nshogoza ◽  
Yaqian Liu ◽  
Jia Gao ◽  
Mingqing Liu ◽  
Sayed Ala Moududee ◽  
...  

The TDP-43 is originally a nuclear protein but translocates to the cytoplasm in the pathological condition. TDP-43, as an RNA-binding protein, consists of two RNA Recognition Motifs (RRM1 and RRM2). RRMs are known to involve both protein-nucleotide and protein-protein interactions and mediate the formation of stress granules. Thus, they assist the entire TDP-43 protein with participating in neurodegenerative and cancer diseases. Consequently, they are potential therapeutic targets. Protein-observed and ligand-observed nuclear magnetic resonance (NMR) spectroscopy were used to uncover the small molecule inhibitors against the tandem RRM of TDP-43. We identified three hits weakly binding the tandem RRMs using the ligand-observed NMR fragment-based screening. The binding topology of these hits is then depicted by chemical shift perturbations (CSP) of the 15N-labeled tandem RRM and RRM2, respectively, and modeled by the CSP-guided High Ambiguity Driven biomolecular DOCKing (HADDOCK). These hits mainly bind to the RRM2 domain, which suggests the druggability of the RRM2 domain of TDP-43. These hits also facilitate further studies regarding the hit-to-lead evolution against the TDP-43 RRM domain.


2012 ◽  
Vol 22 (14) ◽  
pp. 4660-4664 ◽  
Author(s):  
Julien Pothier ◽  
Markus A. Riederer ◽  
Oliver Peter ◽  
Xavier Leroy ◽  
Anja Valdenaire ◽  
...  

2007 ◽  
Vol 2 (5) ◽  
pp. 707-723 ◽  
Author(s):  
Ákos Papp ◽  
Tamás Szommer ◽  
László Barna ◽  
Gergely Gyimesi ◽  
Péter Ferdinandy ◽  
...  

2006 ◽  
Vol 16 (5) ◽  
pp. 1371-1379 ◽  
Author(s):  
Kazuto Yamazaki ◽  
Naoto Kusunose ◽  
Katsuya Fujita ◽  
Hideshi Sato ◽  
Shigehiro Asano ◽  
...  

2002 ◽  
Vol 45 (12) ◽  
pp. 2494-2500 ◽  
Author(s):  
Jayashree Srinivasan ◽  
Angelo Castellino ◽  
Erin K. Bradley ◽  
John E. Eksterowicz ◽  
Peter D. J. Grootenhuis ◽  
...  

2002 ◽  
Vol 186 (3-4) ◽  
pp. 183-197 ◽  
Author(s):  
Friedrich Lucassen ◽  
Russell Harmon ◽  
Gerhard Franz ◽  
Rolf L. Romer ◽  
Raul Becchio ◽  
...  
Keyword(s):  

2002 ◽  
Vol 2 ◽  
pp. 86-94 ◽  
Author(s):  
Yukio Tada ◽  
Ichiro Yamawaki ◽  
Shuichi Ueda ◽  
Hiroshi Matsumoto ◽  
Naosuke Matsuura ◽  
...  
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