Solid-Phase Synthesis of PROTACs and SNIPERs on Backbone Amide Linked (BAL) Resin.

Developing straightforward but flexible approaches to PROTAC synthesis that can incorporate the structural elements of emerging designs can improve the quality and efficiency of PROTAC development. Solid-phase approaches could offer many advantages over conventional PROTAC synthesis if diverse chemistries and topographies can be incorporated. We have exploited the backbone-amide-linked (BAL) resin to employ an array of solid-phase organic reactions, providing access to VHL- and IAP-targeting degraders using the BRD4-targeting JQ1 conjugates as examples.

The effects of exosite occupancy on the substrate specificity of thrombin.

Thrombin (EC 3.4.4.