Structural features of the protein kinase domain and targeted binding by small-molecule inhibitors
C Arter, L Trask, S Ward, S Yeoh, R Bayliss - Journal of Biological …, 2022 - ASBMB
Protein kinases are key components in cellular signaling pathways as they carry out the
phosphorylation of proteins, primarily on Ser, Thr, and Tyr residues. The catalytic activity of …
phosphorylation of proteins, primarily on Ser, Thr, and Tyr residues. The catalytic activity of …
An overview of kinase downregulators and recent advances in discovery approaches
B Wang, H Wu, C Hu, H Wang, J Liu… - Signal Transduction and …, 2021 - nature.com
Since the clinical approval of imatinib, the discovery of protein kinase downregulators
entered a prosperous age. However, challenges still exist in the discovery of kinase …
entered a prosperous age. However, challenges still exist in the discovery of kinase …
An atlas of substrate specificities for the human serine/threonine kinome
Protein phosphorylation is one of the most widespread post-translational modifications in
biology,. With advances in mass-spectrometry-based phosphoproteomics, 90,000 sites of …
biology,. With advances in mass-spectrometry-based phosphoproteomics, 90,000 sites of …
Epithelial memory of inflammation limits tissue damage while promoting pancreatic tumorigenesis
INTRODUCTION The association between tumors and inflammation is a long-established
clinical observation. Although many studies have demonstrated that the inflammatory …
clinical observation. Although many studies have demonstrated that the inflammatory …
Rapid and direct control of target protein levels with VHL-recruiting dTAG molecules
Chemical biology strategies for directly perturbing protein homeostasis including the
degradation tag (dTAG) system provide temporal advantages over genetic approaches and …
degradation tag (dTAG) system provide temporal advantages over genetic approaches and …
A pan-cancer organoid platform for precision medicine
BM Larsen, M Kannan, LF Langer, BD Leibowitz… - Cell reports, 2021 - cell.com
Patient-derived tumor organoids (TOs) are emerging as high-fidelity models to study cancer
biology and develop novel precision medicine therapeutics. However, utilizing TOs for …
biology and develop novel precision medicine therapeutics. However, utilizing TOs for …
Macrophage DCLK1 promotes obesity-induced cardiomyopathy via activating RIP2/TAK1 signaling pathway
B Yang, Y Zhao, W Luo, W Zhu, L Jin, M Wang… - Cell Death & …, 2023 - nature.com
Obesity increases the risk for cardiovascular diseases and induces cardiomyopathy. Chronic
inflammation plays a significant role in obesity-induced cardiomyopathy and may provide …
inflammation plays a significant role in obesity-induced cardiomyopathy and may provide …
[HTML][HTML] Inhibition of DCLK1 sensitizes resistant lung adenocarcinomas to EGFR-TKI through suppression of Wnt/β-Catenin activity and cancer stemness
R Yan, X Fan, Z Xiao, H Liu, X Huang, J Liu, S Zhang… - Cancer letters, 2022 - Elsevier
Lung adenocarcinoma is the most common form of lung cancer, accounting for 60% of non-
small cell lung cancer (NSCLC) cases in Asian patients. Importantly, nearly half of these …
small cell lung cancer (NSCLC) cases in Asian patients. Importantly, nearly half of these …
Macrophage DCLK1 promotes atherosclerosis via binding to IKKβ and inducing inflammatory responses
Z Huang, S Shen, X Han, W Li, W Luo, L Lin… - EMBO molecular …, 2023 - embopress.org
Atherosclerosis is a chronic inflammatory disease with high morbidity and mortality rates
worldwide. Doublecortin‐like kinase 1 (DCLK1), a microtubule‐associated protein kinase, is …
worldwide. Doublecortin‐like kinase 1 (DCLK1), a microtubule‐associated protein kinase, is …
Identification of a potent and selective covalent Pin1 inhibitor
BJ Pinch, ZM Doctor, B Nabet, CM Browne… - Nature chemical …, 2020 - nature.com
Peptidyl-prolyl cis/trans isomerase NIMA-interacting 1 (Pin1) is commonly overexpressed in
human cancers, including pancreatic ductal adenocarcinoma (PDAC). While Pin1 is …
human cancers, including pancreatic ductal adenocarcinoma (PDAC). While Pin1 is …