Gluetacs Therapeutics constructed a novel class of sulfur-containing CRBN ligands with high affinity based on its proprietary GlueTacs® platform

Release Time:2026-10-22
Publisher:SHANGHAITECH UNIVERSITY

Gluetacs Therapeutics constructed a novel class of sulfur-containing CRBN ligands with high affinity based on its proprietary GlueTacs® platform, and based on these ligands, the R&D team adopted a "one fish, two dishes" approach to create two types of degraders. The first is the molecular glue GT-02624: it selectively degrades GSPT1, has no effect on classic substrates such as IKZF1/3, ZFP91, CK1α, and SALL4, and has good metabolic and pharmacokinetic profiles; the second is the PROTAC GT-01956: it targets and degrades BRD2/4 at picomolar concentrations and exhibits excellent antiproliferative activity in both hematologic and solid tumor cell lines. The significance of this research goes beyond the design and development of degraders with two different mechanisms; it also provides a platform-based design approach. The related results were published online in the internationally renowned journal RSC Medicinal Chemistry under the title "Rational design and synthesis of a novel cereblon ligand class enabling selective molecular glue and potent PROTAC."