| Title : Identification of selective covalent inhibitors of platelet activating factor acetylhydrolase 1B2 from the screening of an oxadiazolone-capped peptoid-azapeptoid hybrid library - Sarma_2016_Bioorg.Med.Chem_24_3953 |
| Author(s) : Sarma BK , Liu X , Kodadek T |
| Ref : Bioorganic & Medicinal Chemistry , 24 :3953 , 2016 |
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Abstract :
A potent and selective inhibitor of platelet-activating factor acetylhydrolase 1B2 (PAFAH1B2) is described. The compound was derived by improvement of a modest affinity primary hit isolated from the screening of a bead-displayed peptoid-azapeptoid hybrid library tethered to an oxadiazolone 'warhead'. The oxadiazolone moiety of the inhibitors was found to react covalently with the active site serine residue of PAFAH1B2. This screening strategy may be useful for the identification of many selective, covalent inhibitors of serine hydrolases. |
| PubMedSearch : Sarma_2016_Bioorg.Med.Chem_24_3953 |
| PubMedID: 27160052 |
Sarma BK, Liu X, Kodadek T (2016)
Identification of selective covalent inhibitors of platelet activating factor acetylhydrolase 1B2 from the screening of an oxadiazolone-capped peptoid-azapeptoid hybrid library
Bioorganic & Medicinal Chemistry
24 :3953
Sarma BK, Liu X, Kodadek T (2016)
Bioorganic & Medicinal Chemistry
24 :3953