January 2024 HighlightsBy Anonymous / February 4, 2024 Methotrexate-based PROTACs as DHFR-specific chemical probes Anti-tumor immunotherapy using engineered bacterial outer membrane vesicles fused to lysosome-targeting chimeras mediated by transferrin receptorDiscovery and Preclinical Pharmacology of NX-2127, an Orally Bioavailable Degrader of Bruton’s Tyrosine Kinase with Immunomodulatory Activity for the Treatment of Patients with B Cell Malignancies Proteolysis-targeting chimeras with reduced off-targetsSelective CK1α degraders exert antiproliferative activity against a broad range of human cancer cell lines Ubiquitin-Derived Fragment as a Peptide Linker for the Efficient Cleavage of a Target Protein from a DegronDesign, Synthesis, and In Vitro and In Vivo Evaluation of Cereblon Binding Bruton’s Tyrosine Kinase (BTK) Degrader CD79b Targeted Antibody–Drug Conjugates JAK1/JAK2 degraders based on PROTAC for topical treatment of atopic dermatitisDiscovery of a PROTAC degrader for METTL3-METTL14 complex A small molecule VHL molecular glue degrader for cysteine dioxygenase 1From Thalidomide to Rational Molecular Glue Design for Targeted Protein Degradation Discovery of Novel PDEδ Autophagic Degraders: A Case Study of Autophagy-Tethering Compound (ATTEC)Cereblon-Based Bifunctional Degrader of SOS1, BTX-6654, Targets Multiple KRAS Mutations and Inhibits Tumor Growth Development of sulfonyl fluoride chemical probes to advance the discovery of cereblon modulators†Discovery of Potent SOS1 PROTACs with Effective Antitumor Activities against NCI-H358 Tumor Cells In Vitro/In Vivo Design, Synthesis, and Biological Evaluation of Potent and Selective PROTAC Degraders of Oncogenic KRASG12DPROTACs Targeting BRM (SMARCA2) Afford Selective In Vivo Degradation over BRG1 (SMARCA4) and Are Active in BRG1 Mutant Xenograft Tumor Models Development of a GC-376 Based Peptidomimetic PROTAC as a Degrader of 3-Chymotrypsin-like Protease of SARS-CoV-2Design and Evaluation of PROTACs Targeting Acyl Protein Thioesterase 1 Journey of Von Hippel-Lindau (VHL) E3 ligase in PROTACs design: From VHL ligands to VHL-based degradersDiscovery of the cereblon-recruiting tubulin PROTACs effective in overcoming Taxol resistance in vitro and in vivo Design, synthesis, and evaluation of VHL-based EZH2 degraders for breast cancerDegradation by Design: New Cyclin K Degraders from Old CDK Inhibitors DCAF1-based PROTACs with activity against clinically validated targets overcoming intrinsic- and acquired-degrader resistanceCo-opting the E3 ligase KLHDC2 for targeted protein degradation by small molecules Proteolysis-targeting chimeras with reduced off-targets
