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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- Hypoxia-activated PROTAC for dual inhibition of FAK and EGFR enables synergistic mechano-chemical cancer therapyKeli An, Y F Li, Chunyu Cao, M Wang, Xiaohui Jia, Guorui Jin, Bo Cheng, Yuanbo Jia, Lei Wang, Guo H et al. · 2026 · Neoplasia
- Recent Advances of RNA m6A Modifications in Cancer Immunoediting and ImmunotherapyShoubao Ma, Tasha Barr, Jianhua Yu · 2023 · Cancer treatment and research
- PROteolysis TArgetting Chimeras (PROTACs) Strategy Applied to Kinases: Recent AdvancesAnthony Feral, Guillaume Laconde, Muriel Amblard, Nicolas Masurier · 2020 · Advanced Therapeutics
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- 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 cancerAlix Le Marois, Sasha Bailey, Steven Hooper, Sunil Kumar, Hugh Sparks, Yuriy Alexandrov, Deborah R. Caswell, Fabian Fröhlich, Karin Schlegelmilch, Karishma Valand et al. · 2024 · bioRxiv (Cold Spring Harbor Laboratory)
- Predicting PROTAC-targeted Degradation and Designing Androgen Receptor Degraders with AiPROTACLi Zhang, Renhong Sun, Xia Li, Chaowei Ren, Yahui Long, Wenjuan Tan, Xiaolong Wang, Ke Zou, Xiaobao Yang, Min Wu et al. · 2025 · bioRxiv (Cold Spring Harbor Laboratory)
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- Discovery of a macrocyclic FAK inhibitor GZD-257 for treatment of glioblastomaTing Wu, Yaqing Zuo, Kehui Chen, Ying Xu, Daili Wu, Yi Le, Li Liu, Longjia Yan · 2025 · Bioorganic & Medicinal Chemistry Letters
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- Development of CDK12 as a Cancer Therapeutic Target and Related InhibitorsBiqing Chen, Jiaqi Liu · 2024 · Current Cancer Drug Targets
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- Targeting the WNT/β-Catenin Pathway in Hematological Malignancies: From Molecular Pathogenesis to Emerging Therapeutic StrategiesAli Keyhani, Hamed Haddad Kashani, Khadijeh Dizaji Asl, Zeinab Mazloumi, Faride kaikavoosnejad, Sahar Sadat Moosavi, Milad Verdi, Ali Rafat, Reza Nejati · 2026 · Biomolecules
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- Kinases/Phosphatases | FAK FamilySteven K. Hanks, Sarah C. Stainbrook · 2021 · Elsevier eBooks
- A Structural and Biophysical Perspective of Degrader Activity Through Ternary Complex FormationMorgan S. Gadd, Marine C. Aublette · 2022 · Wiley eBooks
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- PROTACS- targeted protein degradation as a path to precision cancer therapeuticsHannah R Gatley, Paul B. Fisher, Swadesh Kumar Das · 2025 · Advances in cancer research
- Establishing selectivity of FAK-paxillin PPI inhibitor using pulldown proteomics and a focal adhesion protein selectivity panelHunter O'Brien, Brock Hay, Huzaifah Sheikh, Liam McCreary, Krishna Parsawar, Timothy A. Marlowe · 2025 · Biochemistry and Biophysics Reports
- Chemical synthesis of novel aminopyrimidin-4-yl-1H-pyrazole derivatives as spleen tyrosine kinase (SYK) inhibitorsK. V. Rajasheker, M. S. Pallavi, Pallavi Singh, Victor Stupin, Ekaterina Vladimirovna Silina, Kavitharaj Varadaraju, Mohammad Yahya Alfaifi, Ali Abdullah Shati, Serag Eldin I. Elbehairi, Chandan Shivamallu et al. · 2026 · Scientific Reports
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- BindingDB Entry 50017954: PROTACs to address the challenges facing small molecule inhibitors.BindingDB · 2023 · UC San Diego
- BindingDB Entry 50022745: Targeting focal adhesion kinase (FAK) in cancer therapy: A recent update on inhibitors and PROTAC degraders.BindingDB · 2026 · UC San Diego
- BindingDB Entry 50014967: Amide-to-Ester Substitution as a Strategy for Optimizing PROTAC Permeability and Cellular Activity.BindingDB · 2023 · UC San Diego
- BindingDB Entry 50018749: PROTAC: A promising technology for cancer treatment.BindingDB · 2024 · UC San Diego
- BindingDB Entry 50019525: PROTACS: A technology with a gold rush-like atmosphere.BindingDB · 2024 · UC San Diego
- BindingDB Entry 50018545: Blocking Non-enzymatic Functions by PROTAC-Mediated Targeted Protein Degradation.BindingDB · 2024 · UC San Diego
- BindingDB Entry 50007767: Small molecule PROTACs in targeted therapy: An emerging strategy to induce protein degradation.BindingDB · 2021 · UC San Diego
- 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
- BindingDB Entry 50021665: The application of PROTAC in HDAC.BindingDB · 2025 · UC San Diego
- BindingDB Entry 50010796: Discovery of Novel PDEδ Degraders for the Treatment of KRAS Mutant Colorectal Cancer.BindingDB · 2021 · UC San Diego
- BindingDB Entry 50018566: Development and Utility of a PAK1-Selective Degrader.BindingDB · 2024 · UC San Diego
- BindingDB Entry 50022994: Discovery of Novel PROTAC-Based HPK1 Degraders with High Potency and Selectivity for Cancer Immunotherapy.BindingDB · 2026 · UC San Diego
- BindingDB Entry 50016839: VHL-based PROTACs as potential therapeutic agents: Recent progress and perspectives.BindingDB · 2023 · UC San Diego
- BindingDB Entry 50014922: Discovery of a Brigatinib Degrader SIAIS164018 with Destroying Metastasis-Related Oncoproteins and a Reshuffling Kinome Profile.BindingDB · 2023 · UC San Diego
- BindingDB Entry 50022651: Development of novel focal adhesion kinase (FAK) inhibitors for targeting cancer: Structural insights and therapeutic potential.BindingDB · 2026 · UC San Diego