Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

Jing Lü, Yimin Qian, Martha Altieri, +8

Chemistry & Biology

Natural SciencesMolecular BiologyDna ReplicationEfficiently Target Brd4Genome Engineering +1

Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead

Daniel P. Bondeson, Blake E. Smith, George M. Burslem, +7

Cell chemical biology

Protac DesignSelective DegradationBiomolecular EngineeringPromiscuous Warhead

The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study

George M. Burslem, Blake E. Smith, Ashton C. Lai, +10

Cell chemical biology

Protein ChemistryProtein FunctionBiochemistryProtein FoldingNatural Sciences +12

Modular PROTAC Design for the Degradation of Oncogenic BCR‐ABL

Ashton C. Lai, Momar Toure, Doris Hellerschmied, +5

Angewandte Chemie International Edition

HaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion Proteins

Dennis L. Buckley, Kanak Raina, Nicole Darricarrère, +6

ACS Chemical Biology

Protein AssemblyMolecular BiologyChemical BiologyHalotag7 Fusion ProteinsProtein Synthesis +16

MDM2-Recruiting PROTAC Offers Superior, Synergistic Antiproliferative Activity via Simultaneous Degradation of BRD4 and Stabilization of p53

John Hines, Schan Lartigue, Hanqing Dong, +2

Cancer Research

Addressing Kinase-Independent Functions of Fak via PROTAC-Mediated Degradation

Philipp M. Cromm, Kusal T. G. Samarasinghe, John Hines, +1

Journal of the American Chemical Society

Enzymatic InhibitionSignaling PathwayReceptor Tyrosine KinaseAutophagyKinase-independent Functions +16

Small‐Molecule‐Mediated Degradation of the Androgen Receptor through Hydrophobic Tagging

Jeffrey L. Gustafson, Taavi K. Neklesa, Carly S. Cox, +9

Angewandte Chemie International Edition

Posttranslational protein knockdown coupled to receptor tyrosine kinase activation with phosphoPROTACs

John Hines, Jonathan D. Gough, Timothy W. Corson, +1

Proceedings of the National Academy of Sciences

Molecular RegulationMolecular BiologySignaling PathwayReceptor Tyrosine KinasePosttranslational Protein Knockdown +20

Enhancing Antiproliferative Activity and Selectivity of a FLT-3 Inhibitor by Proteolysis Targeting Chimera Conversion

George M. Burslem, Jayoung Song, Xin Chen, +2

Journal of the American Chemical Society

Chemical BiologyPharmaceutical ChemistryTumor BiologyMedicinal ChemistryReceptor Tyrosine Kinase +17