Focal adhesion kinase confers lenvatinib resistance in hepatocellular carcinoma via the regulation of lysine‐deficient kinase 1

W Hou, SA Gad, X Ding, A Dhanarajan… - Molecular …, 2024 - Wiley Online Library
Lenvatinib is a clinically effective multikinase inhibitor approved for first‐line therapy of
advanced hepatocellular carcinoma (HCC). Although resistance against lenvatinib often …

An in vitro analysis of TKI-based sequence therapy in renal cell carcinoma cell lines

A Zaccagnino, B Vynnytska-Myronovska… - International Journal of …, 2023 - mdpi.com
The tyrosine kinase inhibitor (TKI) cabozantinib might impede the growth of the sunitinib-
resistant cell lines by targeting MET and AXL overexpression in metastatic renal cell …

Inhibition of focal adhesion kinase/paxillin axis by caffeic acid phenethyl ester restrains aggressive behaviors of head and neck squamous cell carcinoma in vitro

HJ Yu, JA Shin, SD Cho - Archives of oral biology, 2023 - Elsevier
Objective Caffeic acid phenethyl ester (CAPE), one of the components of propolis that is
produced by honeybees, reportedly suppresses multiple diseases, including bacterial …

FAK regulates tension transmission to the nucleus and endothelial transcriptome independent of kinase activity

MZ Akhter, P Yazbeck, M Tauseef, M Anwar, F Hossen… - Cell Reports, 2024 - cell.com
The mechanical environment generated through the adhesive interaction of endothelial cells
(ECs) with the matrix controls nuclear tension, preventing aberrant gene synthesis and the …

Integrin β6 mediates epithelial–mesenchymal transition in diabetic kidney disease

X Li, Y Miao, T Li, X Liu, L Xu, J Guo, X Yu… - Molecular and Cellular …, 2023 - Elsevier
The progression of diabetic kidney disease (DKD) is associated with increased fibronectin
(FN) levels in proximal tubular epithelial cells. Bioinformatics analysis showed that integrin …

Off-target pharmacological activity at various kinases: Potential functional and pathological side effects

JR Green, PKS Mahalingaiah… - … of Pharmacological and …, 2023 - Elsevier
In drug discovery, during the lead optimization and candidate characterization stages, novel
small molecules are frequently evaluated in a battery of in vitro pharmacology assays to …

DCUN1D1 and neddylation: Potential targets for cancer therapy

JD Paccez, CLM Foret, JF de Vasconcellos… - … et Biophysica Acta (BBA …, 2024 - Elsevier
Cancer affects millions of people and understanding the molecular mechanisms related to
disease development and progression is essential to manage the disease. Post …

Dynamics Playing a Key Role in the Covalent Binding of Inhibitors to Focal Adhesion Kinase

Y Liu, J Tan, S Hu, M Hussain, C Qiao… - Journal of Chemical …, 2024 - ACS Publications
Covalent kinase inhibitors (CKIs) have recently garnered considerable attention, yet the
rational design of CKIs continues to pose a great challenge. In the discovery of CKIs …

Rho-associated kinase1 promotes laryngeal squamous cell carcinoma tumorigenesis and progression via the FAK signaling pathway

L Yang, P Qiao, J Zhang, S Huang, A Hu - Discover Oncology, 2022 - Springer
Laryngeal squamous cell carcinoma (LSCC) is one of the most common head and neck
squamous cell carcinomas (HNSCC). Rho-associated kinase1 (ROCK1) is considered to …

A novel FAK-degrading PROTAC molecule exhibited both anti-tumor activities and efficient MDR reversal effects

M Xu, X Gu, C Li, L Pan, Z Zhu, M Fan, Y Zhao… - Acta Pharmacologica …, 2024 - nature.com
FAK (focal adhesion kinase) is widely involved in cancer growth and drug resistance
development. Thus, FAK inhibition has emerged as an effective strategy for tumor treatment …