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New Insights on Fak and Fak Inhibitors
Current Medicinal Chemistry, 2021Background: Focal adhesion kinase (Fak) is a cytoplasmic protein tyrosine kinase overexpressed and activated in different solid cancers; it has shown an important role in metastasis formation, cell migration, invasion and angiogenesis and consequently it has been proposed as a potential target in cancer therapy, particularly in a metastatic phase. In
C. Brullo, B. Tasso
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Cell Biology International, 2003
Recent data suggest a novel and significant role for the protein tyrosine kinase Pyk2/CAK /RAFTK in cytoskeletal remodeling, proliferation and motility of adherent cells, such as epithelial cells and fibroblasts, possibly putting this kinase in direct competition with its close cousin, the focal adhesion kinase, FAK. Within a three-month period in late
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Recent data suggest a novel and significant role for the protein tyrosine kinase Pyk2/CAK /RAFTK in cytoskeletal remodeling, proliferation and motility of adherent cells, such as epithelial cells and fibroblasts, possibly putting this kinase in direct competition with its close cousin, the focal adhesion kinase, FAK. Within a three-month period in late
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Educational Issues In Fak Fak, West Papua Province
2018Proceedings of the Education Research Colloquium between Faculty of Education, Universiti Teknologi Malaysia (UTM) & Universitas Negeri Makassar, Indonesia.
NikoToturup, Patak, Andi Anto
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Frontiers in Bioscience, 2003
Integrin alpha(v)beta3 plays a pivotal role in osteoclastic bone resoprtion by mediating both osteoclast attachments on bone matrix and cytoskeleton reorganization. The focal adhesion kinase (FAK) family kinases including FAK and proline-rich tyrosine kinase 2 (PYK2) are major tyrosine kinases activated by integrin engagement.
Wen-Cheng, Xiong, Xu, Feng
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Integrin alpha(v)beta3 plays a pivotal role in osteoclastic bone resoprtion by mediating both osteoclast attachments on bone matrix and cytoskeleton reorganization. The focal adhesion kinase (FAK) family kinases including FAK and proline-rich tyrosine kinase 2 (PYK2) are major tyrosine kinases activated by integrin engagement.
Wen-Cheng, Xiong, Xu, Feng
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Science Signaling, 2008
Under normal growth conditions, the tumor suppressor protein p53 is ubiquitinated and degraded, and cells proliferate. However, when cells are under stress, p53 accumulates and induces the expression of the gene encoding p21, which triggers cell cycle arrest.
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Under normal growth conditions, the tumor suppressor protein p53 is ubiquitinated and degraded, and cells proliferate. However, when cells are under stress, p53 accumulates and induces the expression of the gene encoding p21, which triggers cell cycle arrest.
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Selectivity switch between FAK and Pyk2: Macrocyclization of FAK inhibitors improves Pyk2 potency
Bioorganic & Medicinal Chemistry Letters, 2016Herein, we describe the synthesis of Pyk2 inhibitors via macrocyclization of FAK and dual Pyk2-FAK inhibitors. We identified macrocycle 25a as a highly potent Pyk2 inhibitor (IC50=0.7nM), with ∼175-fold improvement in Pyk2 potency as compared to its acyclic counterpart.
Julie, Farand +16 more
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Biochemical Pharmacology
Focal adhesion kinase (FAK), a non-receptor tyrosine kinase, plays an essential role in regulating cell proliferation, migration and invasion through both kinase-dependent enzymatic function and kinase-independent scaffolding function. The overexpression and activation of FAK is commonly observed in various cancers and some drug-resistant settings ...
Ming Yang, Hua Xiang, Guoshun Luo
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Focal adhesion kinase (FAK), a non-receptor tyrosine kinase, plays an essential role in regulating cell proliferation, migration and invasion through both kinase-dependent enzymatic function and kinase-independent scaffolding function. The overexpression and activation of FAK is commonly observed in various cancers and some drug-resistant settings ...
Ming Yang, Hua Xiang, Guoshun Luo
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