660843-23-2Relevant academic research and scientific papers
ANTIBODY DRUG CONJUGATES OF KINESIN SPINDEL PROTEIN (KSP) INHIBITORS WITH ANTIB7H3-ANTIBODIES
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Paragraph 0959-0961, (2020/05/29)
The present application relates to novel binder drug conjugates (ADCs), to active metabolites of these ADCs, to processes for preparing these ADCs, to the use of these ADCs for the treatment and/or prophylaxis of diseases and to the use of these ADCs for preparing medicaments for treatment and/or prophylaxis of diseases, in particular hyperproliferative and/or angiogenic disorders such as, for example, cancer diseases. Such treatments can be effected as monotherapy or else in combination with other medicaments or further therapeutic measures.
Two-step labeling of endogenous enzymatic activities by Diels-Alder ligation
Willems, Lianne I.,Verdoes, Martijn,Florea, Bogdan I.,Van Der Marel, Gijsbert A.,Overkleeft, Herman S.
experimental part, p. 1769 - 1781 (2011/04/18)
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 selectively in cellular extracts and in living cells. We were also able to label the activity of cysteine proteases in cell extracts by utilizing a diene-derivatized cathepsin probe. Importantly, the Diels-Alder strategy described here is fully orthogonal with respect to the Staudinger-Bertozzi ligation, as demonstrated by the independent labeling of different proteolytic activities by the two methods in a single experiment.
Synthesis and characterization of coumarin-based europium complexes and luminescence measurements in aqueous media
Feau, Clementine,Klein, Emmanuel,Dosche, Carsten,Kerth, Paul,Lebeau, Luc
experimental part, p. 5259 - 5270 (2010/04/04)
A series of new ligands suitable for the formation of luminescent lanthanide complexes in water is described. The chelates are designed for analyte labeling and play the role of fluorescent donor in homogeneous time-resolved fluorescence assays using LEDs
