Proteolysis-targeting chimeras (PROTACs) in cancer therapy

X Li, W Pu, Q Zheng, M Ai, S Chen, Y Peng - Molecular cancer, 2022 - Springer
Proteolysis-targeting chimeras (PROTACs) are engineered techniques for targeted protein
degradation. A bifunctional PROTAC molecule with two covalently-linked ligands recruits …

Drug discovery targeting focal adhesion kinase (FAK) as a promising cancer therapy

XJ Pang, XJ Liu, Y Liu, WB Liu, YR Li, GX Yu, XY Tian… - Molecules, 2021 - mdpi.com
FAK is a nonreceptor intracellular tyrosine kinase which plays an important biological
function. Many studies have found that FAK is overexpressed in many human cancer cell …

[HTML][HTML] Recent progress on FAK inhibitors with dual targeting capabilities for cancer treatment

X Wu, J Wang, Q Liang, R Tong, J Huang… - Biomedicine & …, 2022 - Elsevier
Focal adhesion kinase (FAK, also known as PTK2) is a tyrosine kinase that regulates
integrin and growth factor signaling pathways and is involved in the migration, proliferation …

The development of FAK inhibitors: a five-year update

A Spallarossa, B Tasso, E Russo, C Villa… - International Journal of …, 2022 - mdpi.com
Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase over-expressed in different
solid cancers. In recent years, FAK has been recognized as a new target for the …

Focal adhesion kinase (FAK): its structure, characteristics, and signaling in skeletal system

Y Huang, J Liao, R Vlashi, G Chen - Cellular Signalling, 2023 - Elsevier
Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase and distributes important
regulatory functions in skeletal system. Mesenchymal stem cell (MSC) possesses significant …

VHL-based PROTACs as potential therapeutic agents: Recent progress and perspectives

C Wang, Y Zhang, J Wang, D Xing - European Journal of Medicinal …, 2022 - Elsevier
Proteolysis targeting chimeras (PROTACs), which hijack proteins of interest (POIs) and
recruit E3 ligases for target degradation via the ubiquitin-proteasome pathway, are a novel …

New insights on the nuclear functions and targeting of FAK in cancer

S Pomella, M Cassandri, MR Braghini… - International journal of …, 2022 - mdpi.com
Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase over-expressed and
activated in both adult and pediatric cancers, where it plays important roles in the regulation …

Targeting protein kinases degradation by PROTACs

F Yu, M Cai, L Shao, J Zhang - Frontiers in Chemistry, 2021 - frontiersin.org
Kinase dysregulation is greatly associated with cell proliferation, migration and survival,
indicating the importance of kinases as therapeutic targets for anticancer drug development …

[HTML][HTML] Overexpression of BACH1 mediated by IGF2 facilitates hepatocellular carcinoma growth and metastasis via IGF1R and PTK2

M Xie, M Sun, X Ji, D Li, X Chen, B Zhang, W Huang… - Theranostics, 2022 - ncbi.nlm.nih.gov
Background: Accumulating studies manifest that BTB and CNC homology 1 (BACH1)
facilitates multiple malignancies progression and metastasis, and targeting the BACH1 …

The dual FAK-HDAC inhibitor MY-1259 displays potent activities in gastric cancers in vitro and in vivo

J Song, X Liu, YF Zhang, XY Tian, MY Deng… - Bioorganic …, 2023 - Elsevier
Epigenetic regulation and Focal adhesion kinase (FAK) are considered to be two important
targets for the development of antitumor drugs. Studies have shown that the combination of …