Warhead group

22:23 Jul 22, 2018
This question was closed without grading. Reason: No acceptable answer

English to French translations [PRO]
Science - Chemistry; Chem Sci/Eng / Médicament
English term or phrase: Warhead group
A compound of formula I :
wherein R1 is a warhead group....
Katsou
France
Local time: 21:52


Summary of answers provided
4groupe "tête chercheuse" (warhead)
FX Fraipont


  

Answers


8 hrs   confidence: Answerer confidence 4/5Answerer confidence 4/5
warhead group
groupe "tête chercheuse" (warhead)


Explanation:
"1.3.6 Pourquoi les inhibiteurs covalents sont-ils plus spécifiques qu’on ne le pense ?
Le groupement électrophile mis sur une molécule, bien qu‟appelé parfois war head, ne
doit pas agir comme une « tête chercheuse » ciblant le premier nucléophile venu (Vicik et al., 2006). Au contraire, il est nécessaire que les deux groupes soient à proximité pendant un certain temps et qu‟ils s‟orientent favorablement l‟un par rapport à l‟autre pour que la liaison covalente se forme (Figure 35). Cela revient à dire que le squelette entier du ligand doit contribuer à la première étape de reconnaissance/complémentarité entre le ligand et la
protéine. Dans une seconde étape, le groupement électrophile se lie de manière covalente, voir irréversiblement, à la protéine, via un résidu nucléophile peu conservé au sein de la famille.
Évaluation des Protéines Kinases en tant que Cibles Thérapeutiques ...
http://scd-theses.u-strasbg.fr/2295/01/LEPROULT_Emeline_2011...

"Those skilled in the art will recognize that certain reactive functional groups can be used as "warhead." As used herein, the term "warhead" or "warhead group" means a functional group present on a compound of the present invention, wherein the functional group capable of binding covalently to the amino acid residues present in the binding pocket of the target protein (e.g. cysteine , lysine, histidine or other residues can be covalently modified group), thereby irreversibly inhibiting the protein. It should be appreciated, -LY group (as defined and described herein) to provide for the warhead group covalently and irreversibly inhibited protein."
https://patents.google.com/patent/CN103501610A/en


FX Fraipont
Belgium
Local time: 21:52
Native speaker of: Native in FrenchFrench
PRO pts in category: 391
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