Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL.
about
Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibitionInduced protein degradation: an emerging drug discovery paradigm.In Vivo Knockdown of Pathogenic Proteins via Specific and Nongenetic Inhibitor of Apoptosis Protein (IAP)-dependent Protein Erasers (SNIPERs).Structural basis of PROTAC cooperative recognition for selective protein degradationChemical approaches to targeted protein degradation through modulation of the ubiquitin-proteasome pathwayThe chimeric ubiquitin ligase SH2-U-box inhibits the growth of imatinib-sensitive and resistant CML by targeting the native and T315I-mutant BCR-ABLNew Modalities for Challenging Targets in Drug Discovery.Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds.Synthetic Biology-The Synthesis of Biology.Cereblon and its downstream substrates as molecular targets of immunomodulatory drugs.The molecular mechanism of thalidomide analogs in hematologic malignancies.Targeted Protein Degradation by Small Molecules.Waste disposal-An attractive strategy for cancer therapy.Targeted protein knockdown using small molecule degraders.Targeted Protein Degradation: from Chemical Biology to Drug Discovery.Protein Degradation by In-Cell Self-Assembly of Proteolysis Targeting Chimeras.Development of protein degradation inducers of oncogenic BCR-ABL protein by conjugation of ABL kinase inhibitors and IAP ligands.Homo-PROTACs: bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation.Targeting the Allosteric Site of Oncoprotein BCR-ABL as an Alternative Strategy for Effective Target Protein Degradation.Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766).Group-Based Optimization of Potent and Cell-Active Inhibitors of the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase: Structure-Activity Relationships Leading to the Chemical Probe (2S,4R)-1-((S)-2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-Targeting oncoproteins for degradation by small molecules in myeloid leukemia.Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead.The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study.Molecular recognition of ternary complexes: a new dimension in the structure-guided design of chemical degraders.Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation.Degradation of the BAF Complex Factor BRD9 by Heterobifunctional Ligands.Chemically induced degradation of CDK9 by a proteolysis targeting chimera (PROTAC).Design, Synthesis, and Characterization of Brequinar Conjugates as Probes to Study DHODH Inhibition.Derivatization of inhibitor of apoptosis protein (IAP) ligands yields improved inducers of estrogen receptor α degradation.Small Molecule Modulators of RING-Type E3 Ligases: MDM and Cullin Families as Targets.Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugsPharmacological difference between degrader and inhibitor against oncogenic BCR-ABL kinase
P2860
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P2860
Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL.
description
2015 nî lūn-bûn
@nan
2015年の論文
@ja
2015年論文
@yue
2015年論文
@zh-hant
2015年論文
@zh-hk
2015年論文
@zh-mo
2015年論文
@zh-tw
2015年论文
@wuu
2015年论文
@zh
2015年论文
@zh-cn
name
Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL.
@en
type
label
Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL.
@en
prefLabel
Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL.
@en
P2093
P2860
P356
P1476
Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL
@en
P2093
Ashton C Lai
Craig M Crews
Jemilat Salami
John Hines
Momar Toure
Saul Jaime-Figueroa
P2860
P304
P356
10.1002/ANIE.201507634
P407
P577
2015-11-23T00:00:00Z