A historical overview of protein kinases and their targeted small molecule inhibitors

R Roskoski Jr - Pharmacological research, 2015 - Elsevier
Protein kinases play a predominant regulatory role in nearly every aspect of cell biology and
they can modify the function of a protein in almost every conceivable way. Protein …

The regulation of PKA signaling in obesity and in the maintenance of metabolic health

E London, CA Stratakis - Pharmacology & therapeutics, 2022 - Elsevier
The cAMP-dependent protein kinase (PKA) system represents a primary cell-signaling
pathway throughout systems and across species. PKA facilitates the actions of hormones …

Tracking cancer drugs in living cells by thermal profiling of the proteome

MM Savitski, FBM Reinhard, H Franken, T Werner… - Science, 2014 - science.org
INTRODUCTION Understanding drug mechanism poses the daunting challenge of
determining the affinity of the drug for all potential targets. Drug target engagement can be …

A glimpse of structural biology through X-ray crystallography

Y Shi - Cell, 2014 - cell.com
Since determination of the myoglobin structure in 1957, X-ray crystallography, as the
anchoring tool of structural biology, has played an instrumental role in deciphering the …

Assembly of allosteric macromolecular switches: lessons from PKA

SS Taylor, R Ilouz, P Zhang, AP Kornev - Nature reviews Molecular cell …, 2012 - nature.com
Protein kinases are dynamic molecular switches that have evolved to be only transiently
activated. Kinase activity is embedded within a conserved kinase core, which is typically …

Constitutive activation of PKA catalytic subunit in adrenal Cushing's syndrome

F Beuschlein, M Fassnacht, G Assié… - … England Journal of …, 2014 - Mass Medical Soc
Background Corticotropin-independent Cushing's syndrome is caused by tumors or
hyperplasia of the adrenal cortex. The molecular pathogenesis of cortisol-producing adrenal …

Dynamic architecture of a protein kinase

CL McClendon, AP Kornev… - Proceedings of the …, 2014 - National Acad Sciences
Protein kinases are dynamically regulated signaling proteins that act as switches in the cell
by phosphorylating target proteins. To establish a framework for analyzing linkages between …

Protein kinase A catalytic subunit isoform PRKACA; History, function and physiology

RE Turnham, JD Scott - Gene, 2016 - Elsevier
Our appreciation of the scope and influence of second messenger signaling has its origins
in pioneering work on the cAMP-dependent protein kinase. Also called protein kinase A …

Local protein kinase A action proceeds through intact holoenzymes

FD Smith, JL Esseltine, PJ Nygren, D Veesler… - Science, 2017 - science.org
Hormones can transmit signals through adenosine 3ʹ, 5ʹ-monophosphate (cAMP) to
precise intracellular locations. The fidelity of these responses relies on the activation of …

AI-designed NMR spectroscopy RF pulses for fast acquisition at high and ultra-high magnetic fields

VS Manu, C Olivieri, G Veglia - Nature communications, 2023 - nature.com
Nuclear magnetic resonance (NMR) spectroscopy is a powerful high-resolution tool for
characterizing biomacromolecular structure, dynamics, and interactions. However, the …