Soluble templates for drug design: the acetylcholine binding proteins and freeze-frame, click chemistry for in situ synthesis of nicotinic ligands

SciVee ◽  
2008 ◽  
2012 ◽  
Vol 5 (3) ◽  
pp. 119-123 ◽  
Author(s):  
María Garrido ◽  
José Luis Abad ◽  
Alicia Alonso ◽  
Félix M. Goñi ◽  
Antonio Delgado ◽  
...  

2013 ◽  
Vol 104 (2) ◽  
pp. 373a
Author(s):  
L. Ruth Montes ◽  
Maria Garrido ◽  
Jose Luis Abad ◽  
Antonio Delgado ◽  
Felix M. Goni ◽  
...  

2022 ◽  
Author(s):  
K. M. Kacprzak ◽  
I. Skiera ◽  
J. Rutkowski

AbstractProclaimed by Sharpless in 2001, the manifesto of click chemistry philosophy shifted the focus from target-oriented to drug-like-oriented synthesis, and has enormously accelerated the drug-discovery process over the last two decades. Copper(I)-catalyzed and metal-free versions of the Huisgen 1,3-dipolar cycloaddition of azides and alkynes have become the reference click chemistry synthetic tools. These processes are adaptable to various drug-design modes such as kinetic target guided synthesis (in situ click chemistry assembling; KTGS), combinatorial chemistry/high-throughput-screening approaches, or structure-based rational projecting. Moreover, the facile click chemistry derivatization of natural or synthetic products, linking molecules or improving the stability of leads by installation of 1,2,3-triazoles, is another important stream of bioactivities. This review is intended to provide a general overview of click-chemistry-powered drug design, with dozens of successful examples resulting in the discovery of nanomolar-active 1,2,3-triazoles in every stage of drug development.


2008 ◽  
Vol 49 (33) ◽  
pp. 4824-4827 ◽  
Author(s):  
Ralf Schirrmacher ◽  
Younes Lakhrissi ◽  
Dean Jolly ◽  
Julian Goodstein ◽  
Philippe Lucas ◽  
...  

2013 ◽  
Vol 30 (6) ◽  
pp. 667
Author(s):  
Zhenzhen WANG ◽  
Fangfang LI ◽  
Han GUO ◽  
Jiuju FENG ◽  
Aijun WANG

2017 ◽  
Vol 101 (3) ◽  
pp. 1371-1380 ◽  
Author(s):  
Tao Li ◽  
Yulei Zhang ◽  
Jia Sun ◽  
Jincui Ren ◽  
Pengfei Zhang ◽  
...  

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