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 Chemistry, 2022 - jbc.org
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 …

Cyclin D1, cancer progression, and opportunities in cancer treatment

S Qie, JA Diehl - Journal of molecular medicine, 2016 - Springer
Mammalian cells encode three D cyclins (D1, D2, and D3) that coordinately function as
allosteric regulators of cyclin-dependent kinase 4 (CDK4) and CDK6 to regulate cell cycle …

Conformational states dynamically populated by a kinase determine its function

T **e, T Saleh, P Rossi, CG Kalodimos - Science, 2020 - science.org
INTRODUCTION Protein kinases mediate many cell signaling processes. Central to their
physiological function is the regulation of their binding and enzymatic activities, which is …

Structural insights into the functional diversity of the CDK–cyclin family

DJ Wood, JA Endicott - Open biology, 2018 - royalsocietypublishing.org
Since their characterization as conserved modules that regulate progression through the
eukaryotic cell cycle, cyclin-dependent protein kinases (CDKs) in higher eukaryotic cells are …

Activating HER2 mutations in HER2 gene amplification negative breast cancer

R Bose, SM Kavuri, AC Searleman, W Shen… - Cancer …, 2013 - aacrjournals.org
Data from 8 breast cancer genome-sequencing projects identified 25 patients with HER2
somatic mutations in cancers lacking HER2 gene amplification. To determine the phenotype …

[HTML][HTML] Allostery in disease and in drug discovery

R Nussinov, CJ Tsai - Cell, 2013 - cell.com
Allostery is largely associated with conformational and functional transitions in individual
proteins. This concept can be extended to consider the impact of conformational …

Ten things you should know about protein kinases: IUPHAR R eview 14

D Fabbro, SW Cowan‐Jacob… - British journal of …, 2015 - Wiley Online Library
Many human malignancies are associated with aberrant regulation of protein or lipid
kinases due to mutations, chromosomal rearrangements and/or gene amplification. Protein …

The EGFR family: not so prototypical receptor tyrosine kinases

MA Lemmon, J Schlessinger… - Cold Spring Harbor …, 2014 - cshperspectives.cshlp.org
The epidermal growth factor receptor (EGFR) was among the first receptor tyrosine kinases
(RTKs) for which ligand binding was studied and for which the importance of ligand-induced …

Structural basis of AMPK regulation by small molecule activators

B **ao, MJ Sanders, D Carmena, NJ Bright… - Nature …, 2013 - nature.com
AMP-activated protein kinase (AMPK) plays a major role in regulating cellular energy
balance by sensing and responding to increases in AMP/ADP concentration relative to ATP …

Structural insight and development of EGFR tyrosine kinase inhibitors

T Amelia, RE Kartasasmita, T Ohwada, DH Tjahjono - Molecules, 2022 - mdpi.com
Lung cancer has a high prevalence, with a growing number of new cases and mortality
every year. Furthermore, the survival rate of patients with non-small-cell lung carcinoma …