Functional Linkers Support Targeting of Multivalent Tweezers to Taspase1.

Taspase 1 is a unique protease not only pivotal for embryonic development but also implicated in leukemias and solid tumors. As such, this enzyme is a promising while still challenging therapeutic target, and with its protein structure featuring a flexible loop preceding the active site a versatile model system for drug development. Supramolecular ligands provide a promising complementary approach to traditional small-molecule inhibitors.

Arylazopyrazoles for Conjugation by CuAAC Click Chemistry.

Molecular photoswitches are increasingly being implemented in bioactive compounds and responsive materials. For this purpose, photoswitches must be coupled to a wide variety of substrates and scaffolds. We present a library of "clickable" arylazopyrazoles (AAPs), which can be conjugated by Cu-catalyzed alkyne azide cycloaddition (CuAAC).