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

PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer

Kanak Raina, Jing Lü, Yimin Qian, +11

Proceedings of the National Academy of Sciences

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

Ras CAAX Peptidomimetic FTI-277 Selectively Blocks Oncogenic Ras Signaling by Inducing Cytoplasmic Accumulation of Inactive Ras-Raf Complexes

Edwina C. Lerner, Yimin Qian, Michelle A. Blaskovich, +7

Journal of Biological Chemistry

Molecular BiologyCancer BiologyTumor BiologyMolecular PharmacologySignaling Pathway +15

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

Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1

Andrew P. Crew, Kanak Raina, Hanqing Dong, +12

Journal of Medicinal Chemistry

Inhibition of the prenylation of K-Ras, but not H- or N-Ras, is highly resistant to CAAX peptidomimetics and requires both a farnesyltransferase and a geranylgeranyltransferase I inhibitor in human tumor cell lines

Edwina C. Lerner, Tingting Zhang, David B. Knowles, +3

Oncogene

Caax PeptidomimeticsMedicineAnti-cancer AgentTumor SuppressorPharmacology +3

Both farnesyltransferase and geranylgeranyltransferase I inhibitors are required for inhibition of oncogenic K-Ras prenylation but each alone is sufficient to suppress human tumor growth in nude mouse xenografts

Jiazhi Sun, Yimin Qian, Andrew D. Hamilton, +1

Oncogene

Oncogenic K-ras PrenylationOncogenic AgentMedicineHuman Tumor GrowthNude Mouse Xenografts +6

Ras CAAX peptidomimetic FTI 276 selectively blocks tumor growth in nude mice of a human lung carcinoma with K-Ras mutation and p53 deletion.

Jiazhi Sun, Yimin Qian, Andrew D. Hamilton, +1

PubMed

PathologyCancer BiologyBlocks Tumor GrowthRas ProcessingTumor Biology +15

Antitumor efficacy of a novel class of non-thiol-containing peptidomimetic inhibitors of farnesyltransferase and geranylgeranyltransferase I: combination therapy with the cytotoxic agents cisplatin, Taxol, and gemcitabine.

Jiazhi Sun, Michelle A. Blaskovich, David B. Knowles, +5

PubMed

Antitumor EfficacyPharmacotherapyInhibits Tumor GrowthTumor BiologyNon-thiol-containing Peptidomimetic Inhibitors +15