A Peptide Stapling Strategy with Built‐In Fluorescence by Direct Late‐Stage C(sp 2 )−H Olefination of Tryptophan

2020 ◽  
Vol 26 (68) ◽  
pp. 16122-16128 ◽  
Author(s):  
Jiang Liu ◽  
Xin Liu ◽  
Fangfang Zhang ◽  
Jiaojiao Qu ◽  
Hongyan Sun ◽  
...  
Keyword(s):  
2022 ◽  
Vol 18 ◽  
pp. 1-12
Author(s):  
Hendrik Gruß ◽  
Rebecca C Feiner ◽  
Ridhiwan Mseya ◽  
David C Schröder ◽  
Michał Jewgiński ◽  
...  

The development of peptide stapling techniques to stabilise α-helical secondary structure motifs of peptides led to the design of modulators of protein–protein interactions, which had been considered undruggable for a long time. We disclose a novel approach towards peptide stapling utilising macrocyclisation by late-stage Suzuki–Miyaura cross-coupling of bromotryptophan-containing peptides of the catenin-binding domain of axin. Optimisation of the linker length in order to find a compromise between both sufficient linker rigidity and flexibility resulted in a peptide with an increased α-helicity and enhanced binding affinity to its native binding partner β-catenin. An increased proteolytic stability against proteinase K has been demonstrated.


2007 ◽  
Vol 45 (05) ◽  
Author(s):  
F Sipos ◽  
S Spisák ◽  
T Krenács ◽  
O Galamb ◽  
B Galamb ◽  
...  

2020 ◽  
Vol 17 (5) ◽  
pp. 34-47
Author(s):  
V. M. Polyakov ◽  
Z. S. Agalarov

The article offers a method for assessing the environmental risk in the territories adjacent to the planning zone of emergency protection measures around the NPP. The method is based on simulation modeling of territory pollution, which is formed at the late stage of a radiation accident and zoning of territories by risk, taking into account the characteristics of the population’s life in a potentially dangerous territory. A vector criterion of environmental risk is proposed that allows zoning these territories according to the degree of danger to the population.


Author(s):  
I Leal ◽  
K Bohn ◽  
SJ Hawkins ◽  
SR Jenkins ◽  
AAV Flores ◽  
...  
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