Two??Step Labeling of Endogenous Enzymatic Activities by Diels–Alder Ligation

…, BI Florea, GA van der Marel, HS Overkleeft

Index: Willems, Lianne I.; Verdoes, Martijn; Florea, Bogdan I.; Van Der Marel, Gijsbert A.; Overkleeft, Herman S. ChemBioChem, 2010 , vol. 11, # 12 p. 1769 - 1781

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Citation Number: 33

Abstract

Abstract A ligation strategy based on the Diels–Alder [4+ 2] cycloaddition for the two-step activity-based labeling of endogenously expressed enzymes in complex biological samples has been developed. A panel of four diene-derivatized proteasome probes was synthesized, along with a dienophile-functionalized BODIPY (TMR) tag. These probes were applied in a Diels–Alder labeling procedure that enabled us to label active proteasome β-subunits ...