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 …
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 …
pathway throughout systems and across species. PKA facilitates the actions of hormones …
Tracking cancer drugs in living cells by thermal profiling of the proteome
INTRODUCTION Understanding drug mechanism poses the daunting challenge of
determining the affinity of the drug for all potential targets. Drug target engagement can be …
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 …
anchoring tool of structural biology, has played an instrumental role in deciphering the …
Assembly of allosteric macromolecular switches: lessons from PKA
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 …
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 …
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 …
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 …
in pioneering work on the cAMP-dependent protein kinase. Also called protein kinase A …
Local protein kinase A action proceeds through intact holoenzymes
Hormones can transmit signals through adenosine 3ʹ, 5ʹ-monophosphate (cAMP) to
precise intracellular locations. The fidelity of these responses relies on the activation of …
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
Nuclear magnetic resonance (NMR) spectroscopy is a powerful high-resolution tool for
characterizing biomacromolecular structure, dynamics, and interactions. However, the …
characterizing biomacromolecular structure, dynamics, and interactions. However, the …