Phthalimide conjugation as a strategy for in vivo target protein degradation

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Items 101–200 of 1,004

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5. Discovery of ERD-308 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Estrogen Receptor (ER)
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7. Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression
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19. Structure‐Based Design of a Macrocyclic PROTAC
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20. Homolog-Selective Degradation as a Strategy to Probe the Function of CDK6 in AML
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21. Targeting Epigenetics in Cancer
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22. Unraveling the Role of Linker Design in Proteolysis Targeting Chimeras
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23. Alternative approaches to target Myc for cancer treatment
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24. Specific Knockdown of Endogenous Tau Protein by Peptide-Directed Ubiquitin-Proteasome Degradation
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25. PROteolysis TArgeting Chimeras (PROTACs) as emerging anticancer therapeutics
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26. Homo-PROTACs: bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation
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27. The Expanding World of N-MYC–Driven Tumors
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28. Discovery of CRBN E3 Ligase Modulator CC-92480 for the Treatment of Relapsed and Refractory Multiple Myeloma
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29. Molecular recognition of ternary complexes: a new dimension in the structure-guided design of chemical degraders
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30. In Vivo Knockdown of Pathogenic Proteins via Specific and Nongenetic Inhibitor of Apoptosis Protein (IAP)-dependent Protein Erasers (SNIPERs)
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31. Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity
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32. Bromodomains: Structure, function and pharmacology of inhibition
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33. Extended pharmacodynamic responses observed upon PROTAC-mediated degradation of RIPK2
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34. Recent Developments in PROTAC‐Mediated Protein Degradation: From Bench to Clinic
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35. Chemical probes and drug leads from advances in synthetic planning and methodology
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36. Bispecific Aptamer Chimeras Enable Targeted Protein Degradation on Cell Membranes
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37. Proteolysis-Targeting Chimeras: Induced Protein Degradation as a Therapeutic Strategy
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38. Optical Control of Small Molecule-Induced Protein Degradation
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39. PROTACs: An Emerging Targeting Technique for Protein Degradation in Drug Discovery
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40. Bromodomain and extraterminal (BET) proteins: biological functions, diseases and targeted therapy
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41. 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
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42. Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands
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43. Discovery of a Covalent FEM1B Recruiter for Targeted Protein Degradation Applications
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44. Chemically induced degradation of CDK9 by a proteolysis targeting chimera (PROTAC)
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45. PROTAC-DB: an online database of PROTACs
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46. Prospective discovery of small molecule enhancers of an E3 ligase-substrate interaction
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47. The novel mechanism of lenalidomide activity
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48. A “Click Chemistry Platform” for the Rapid Synthesis of Bispecific Molecules for Inducing Protein Degradation
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49. Discovery of a molecular glue promoting CDK12-DDB1 interaction to trigger cyclin K degradation
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50. Small Molecule Targeted Recruitment of a Nuclease to RNA
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51. Potent and Preferential Degradation of CDK6 via Proteolysis Targeting Chimera Degraders
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52. Chemically Induced Degradation of the Oncogenic Transcription Factor BCL6
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53. Targeted Protein Degradation by Small Molecules
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54. Choose and Use Your Chemical Probe Wisely to Explore Cancer Biology
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55. Time-resolved protein activation by proximal decaging in living systems
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56. Synthetic Lethal and Resistance Interactions with BET Bromodomain Inhibitors in Triple-Negative Breast Cancer
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57. Emerging New Concepts of Degrader Technologies
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58. Antibody Conjugation of a Chimeric BET Degrader Enables <i>in vivo</i> Activity
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59. Prey for the Proteasome: Targeted Protein Degradation—A Medicinal Chemist's Perspective
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63. <i>In Silico</i> Modeling of PROTAC-Mediated Ternary Complexes: Validation and Application
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64. DCAF11 Supports Targeted Protein Degradation by Electrophilic Proteolysis-Targeting Chimeras
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68. Elucidating the cellular determinants of targeted membrane protein degradation by lysosome-targeting chimeras
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69. Targeted Degradation of BET Proteins in Triple-Negative Breast Cancer
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70. Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors
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71. Discovering and understanding oncogenic gene fusions through data intensive computational approaches
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73. Radiotherapy-Triggered Proteolysis Targeting Chimera Prodrug Activation in Tumors
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74. Simple Structural Modifications Converting a Bona fide MDM2 PROTAC Degrader into a Molecular Glue Molecule: A Cautionary Tale in the Design of PROTAC Degraders
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75. Development of the first small molecule histone deacetylase 6 (HDAC6) degraders
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76. Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK)
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81. Induction of apoptosis in MDA-MB-231 breast cancer cells by a PARP1-targeting PROTAC small molecule
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82. pSILAC mass spectrometry reveals ZFP91 as IMiD-dependent substrate of the CRL4CRBN ubiquitin ligase
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84. Recent developments in epigenetic cancer therapeutics: clinical advancement and emerging trends
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85. Targeted degradation of transcription factors by TRAFTACs: TRAnscription Factor TArgeting Chimeras
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88. Harnessing the Power of Proteolysis for Targeted Protein Inactivation
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89. Development of Multifunctional Histone Deacetylase 6 Degraders with Potent Antimyeloma Activity
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91. Visualizing biologically active small molecules in cells using click chemistry
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92. Expedited mapping of the ligandable proteome using fully functionalized enantiomeric probe pairs
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95. Enhancing Antiproliferative Activity and Selectivity of a FLT-3 Inhibitor by Proteolysis Targeting Chimera Conversion
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96. PROTAC-mediated degradation reveals a non-catalytic function of AURORA-A kinase
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97. E3 ligase ligand chemistries: from building blocks to protein degraders
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98. Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy
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99. EP300 Selectively Controls the Enhancer Landscape of MYCN -Amplified Neuroblastoma
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