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

Cromm, Philipp M., Samarasinghe, Kusal T. G., Hines, John, Crews, Craig M.·2018·Journal of the American Chemical Society

Cited by (311)

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  38. Targeting STK33: From Inhibition to Degradation
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  39. Target Protein Localisation and Its Impact on PROTAC-Mediated Degradation
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  40. Imaging of MAP kinase dynamics reveals endocytic regulation of pulsatile signalling and network re-wiring in response to targeted therapy in EGFR-mutant non-small cell lung cancer
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  41. Predicting PROTAC-targeted Degradation and Designing Androgen Receptor Degraders with AiPROTAC
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  42. Destruction of DNA-binding proteins by programmable O’PROTAC: Oligonucleotide-based PROTAC
    Shao, Jingwei, Yan, Yuqian, Ding, Donglin, Wang, Dejie, He, Yundong, Pan, Yunqian, Yan, Wei, Kharbanda, Anupreet, Li, Hong-yu, Huang, Haojie · 2021
  43. Discovery of a macrocyclic FAK inhibitor GZD-257 for treatment of glioblastoma
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  44. Design and Synthesis of Novel Candidate CK1δ Proteolysis Targeting Chimeras (PROTACs)
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  45. Targeting focal adhesion kinase (FAK) in non-small cell lung cancer (NSCLC): Molecular mechanisms and combination therapeutic strategies
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  46. Targeting Activin Receptor-like Kinase 2 Using Heterobifunctional Protein Degraders
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  48. Development of CDK12 as a Cancer Therapeutic Target and Related Inhibitors
    Biqing Chen, Jiaqi Liu · 2024 · Current Cancer Drug Targets
  49. Future of Trends in the Design and Development of PROTAC
    Popat Kumbhar, Kaustubh Ajit Kolekar, Vikas Kamble, Chukwuebuka Emmanuel Umeyor, John Disouza, Vandana Bharat Patravale · 2024 · Springer eBooks
  50. Targeted Protein Degradation by Proteolysis Targeting Chimeras
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  86. BindingDB Entry 50017954: PROTACs to address the challenges facing small molecule inhibitors.
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  87. BindingDB Entry 50022745: Targeting focal adhesion kinase (FAK) in cancer therapy: A recent update on inhibitors and PROTAC degraders.
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  88. BindingDB Entry 50014967: Amide-to-Ester Substitution as a Strategy for Optimizing PROTAC Permeability and Cellular Activity.
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  89. BindingDB Entry 50018749: PROTAC: A promising technology for cancer treatment.
    BindingDB · 2024 · UC San Diego
  90. BindingDB Entry 50019525: PROTACS: A technology with a gold rush-like atmosphere.
    BindingDB · 2024 · UC San Diego
  91. BindingDB Entry 50018545: Blocking Non-enzymatic Functions by PROTAC-Mediated Targeted Protein Degradation.
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  92. BindingDB Entry 50007767: Small molecule PROTACs in targeted therapy: An emerging strategy to induce protein degradation.
    BindingDB · 2021 · UC San Diego
  93. BindingDB Entry 50015218: Noncovalent CDK12/13 dual inhibitors-based PROTACs degrade CDK12-Cyclin K complex and induce synthetic lethality with PARP inhibitor.
    BindingDB · 2023 · UC San Diego
  94. BindingDB Entry 50021665: The application of PROTAC in HDAC.
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  95. BindingDB Entry 50010796: Discovery of Novel PDEδ Degraders for the Treatment of KRAS Mutant Colorectal Cancer.
    BindingDB · 2021 · UC San Diego
  96. BindingDB Entry 50018566: Development and Utility of a PAK1-Selective Degrader.
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  97. BindingDB Entry 50022994: Discovery of Novel PROTAC-Based HPK1 Degraders with High Potency and Selectivity for Cancer Immunotherapy.
    BindingDB · 2026 · UC San Diego
  98. BindingDB Entry 50016839: VHL-based PROTACs as potential therapeutic agents: Recent progress and perspectives.
    BindingDB · 2023 · UC San Diego
  99. BindingDB Entry 50014922: Discovery of a Brigatinib Degrader SIAIS164018 with Destroying Metastasis-Related Oncoproteins and a Reshuffling Kinome Profile.
    BindingDB · 2023 · UC San Diego
  100. BindingDB Entry 50022651: Development of novel focal adhesion kinase (FAK) inhibitors for targeting cancer: Structural insights and therapeutic potential.
    BindingDB · 2026 · UC San Diego