Solution conformations of bradykinin antagonists modified with CαCα cyclized nonaromatic residues

2008 ◽  
Vol 14 (7) ◽  
pp. 819-829 ◽  
Author(s):  
Emilia Sikorska ◽  
Sylwia Rodziewicz‐MotowidŁo
2020 ◽  
Vol 22 (1) ◽  
pp. 257
Author(s):  
Patricia Gomez-Gutierrez ◽  
Juan J. Perez

Covid-19 urges a deeper understanding of the underlying molecular mechanisms involved in illness progression to provide a prompt therapeutical response with an adequate use of available drugs, including drug repurposing. Recently, it was suggested that a dysregulated bradykinin signaling can trigger the cytokine storm observed in patients with severe Covid-19. In the scope of a drug repurposing campaign undertaken to identify bradykinin antagonists, raloxifene was identified as prospective compound in a virtual screening process. The pharmacodynamics profile of raloxifene towards bradykinin receptors is reported in the present work, showing a weak selective partial agonist profile at the B2 receptor. In view of this new profile, its possible use as a therapeutical agent for the treatment of severe Covid-19 is discussed.


Biochemistry ◽  
2017 ◽  
Vol 56 (21) ◽  
pp. 2701-2714 ◽  
Author(s):  
Drew R. Tietz ◽  
Larissa M. Podust ◽  
David H. Sherman ◽  
Thomas C. Pochapsky

2003 ◽  
Vol 75 (6) ◽  
pp. 1325-1330 ◽  
Author(s):  
Dunmin Mao ◽  
Kodali Ravindra Babu ◽  
Yu-Luan Chen ◽  
D. J. Douglas

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