Design and Evolution: Molecular Sleuthing Reveals Drug Selectivity

2015 ◽  
Author(s):  
Angela K. Eggleston
Keyword(s):  
Drug Selectivity

Antagonist drug selectivity for radioligand binding sites on voltage-gated and receptor-gated Ca2+ channels

1989 ◽  
Vol 105 (1-2) ◽  
pp. 227-232 ◽  
Author(s):  
Drusilla B. Jaffe ◽  
Shelley S. Marks ◽  
David A. Greenberg
Keyword(s):  
Binding Sites ◽  
Radioligand Binding ◽  
Voltage Gated ◽  
Drug Selectivity ◽  
Ca2 Channels

Cryo-EM catalyzes the exploration of drug selectivity: The CDK7 inhibitor example

2021 ◽  
Vol 120 (8) ◽  
pp. 1304-1305
Author(s):  
Montserrat Samsó
Keyword(s):  
Drug Selectivity

Angiogenesis Inhibitors. Drug Selectivity and Target Specificity

2007 ◽  
Vol 13 (27) ◽  
pp. 2795-2809 ◽  
Author(s):  
Georgios Kesisis ◽  
Henk Broxterman ◽  
Giuseppe Giaccone
Keyword(s):  
Angiogenesis Inhibitors ◽  
Target Specificity ◽  
Drug Selectivity

scholarly journals Problems of drug selectivity and dose - pharmacology

2005 ◽  
Vol 569 (2) ◽  
pp. 711-711 ◽  
Author(s):  
Andrew Ramage
Keyword(s):  
Drug Selectivity

scholarly journals Structural basis of nucleoside and nucleoside drug selectivity by concentrative nucleoside transporters

eLife ◽  
2014 ◽  
Vol 3 ◽  
Author(s):  
Zachary Lee Johnson ◽  
Jun-Ho Lee ◽  
Kiyoun Lee ◽  
Minhee Lee ◽  
Do-Yeon Kwon ◽  
...  
Keyword(s):  
Antiviral Agents ◽  
Nucleoside Transporters ◽  
Structural Basis ◽  
Biological Processes ◽  
Functional Information ◽  
Binding Studies ◽  
X Ray ◽  
Equilibrium Binding ◽  
Drug Selectivity ◽  
Proof Of Principle

Concentrative nucleoside transporters (CNTs) are responsible for cellular entry of nucleosides, which serve as precursors to nucleic acids and act as signaling molecules. CNTs also play a crucial role in the uptake of nucleoside-derived drugs, including anticancer and antiviral agents. Understanding how CNTs recognize and import their substrates could not only lead to a better understanding of nucleoside-related biological processes but also the design of nucleoside-derived drugs that can better reach their targets. Here, we present a combination of X-ray crystallographic and equilibrium-binding studies probing the molecular origins of nucleoside and nucleoside drug selectivity of a CNT from Vibrio cholerae. We then used this information in chemically modifying an anticancer drug so that it is better transported by and selective for a single human CNT subtype. This work provides proof of principle for utilizing transporter structural and functional information for the design of compounds that enter cells more efficiently and selectively.

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