Results 41 to 50 of about 115,266,211 (193)

Beyond Simple Mimicry: Next‐Generation Geometric Architectures and Future Paradigms in Small‐Molecule and Macrocyclic Peptidomimetics

Angewandte Chemie, Volume 138, Issue 40, 28 September 2026.
Peptide‐to‐Small Molecule Paradigm: Peptidomimetics have evolved from simple mimicry toward drug‐like scaffolds supported by increasing clinical successes. This Perspective highlights the geometric design principles—linear repetition, convergent fusion, and cyclization—defining the next‐generation peptidomimetic architectures capable of targeting ...
Jesang Lee, Sumin Son, Jeong Yeon Yoo, Ji Hyae Lee, Meehyun Chun, Seung Bum Park   +5 more
wiley   +2 more sources

PKA, PKC, and AKAP localization in and around the neuromuscular junction

BMC Neuroscience, 2001
Background One mechanism that directs the action of the second messengers, cAMP and diacylglycerol, is the compartmentalization of protein kinase A (PKA) and protein kinase C (PKC). A-kinase anchoring proteins (AKAPs) can recruit both enzymes to specific
Newton Alexandra, Smith Donelson, Violin Jonathan D, Barraclough David M, Deerinck Thomas J, Martone Maryann, Yao Virginia J, Humphries Kenneth, Huang Lily, Wang Lin, Perkins Guy A, Scott John D, Taylor Susan S, Ellisman Mark H   +13 more
doaj   +1 more source

Cloning and Characterization of a Protein Kinase A Anchoring Protein (AKAP)-related Protein That Interacts with and Regulates Sphingosine Kinase 1 Activity [PDF]

Journal of Biological Chemistry, 2002
Sphingosine-1-phosphate (S1P) is a bioactive sphingolipid metabolite that has novel dual actions. S1P is the ligand for a family of G protein-coupled receptors known as S1PRs that mediate various physiological functions. Growth factors rapidly activate sphingosine kinase type 1 (SPHK1) resulting in phosphorylation of sphingosine to form S1P, which ...
Emanuela, Lacaná, Michael, Maceyka, Sheldon, Milstien, Sarah, Spiegel   +3 more
openaire   +2 more sources

Spoonbill positively regulates JNK signalling mediated apoptosis in Drosophila melanogaster

European Journal of Cell Biology, 2023
A-kinase anchoring protein (AKAP) comprises a family of scaffold proteins, which decides the subcellular localisation of a combination of signalling molecules. Spoonbill (Spoon) is a putative A-kinase anchoring protein in Drosophila.
Rituparna Das, Pranjali Pandey, Bhawana Maurya, Priyadarshika Pradhan, Devanjan Sinha, Ashim Mukherjee, Mousumi Mutsuddi   +6 more
doaj   +1 more source

Therapeutic strategies for anchored kinases and phosphatases: exploiting short linear motifs and intrinsic disorder

Frontiers in Pharmacology, 2015
Phosphorylation events that occur in response to the second messenger cAMP are controlled spatially and temporally by protein kinase A (PKA) interacting with A-kinase anchoring proteins (AKAPs).
Patrick J Nygren, Patrick J Nygren, John D. Scott, John D. Scott   +3 more
doaj   +1 more source

A-Kinase Anchoring Proteins Diminish TGF-β₁/Cigarette Smoke-Induced Epithelial-To-Mesenchymal Transition

Cells, 2020
Epithelial-to-mesenchymal transition (EMT) plays a role in chronic obstructive pulmonary diseases (COPD). Cyclic adenosine monophosphate (cAMP) can inhibit transforming growth factor-β1 (TGF-β1) mediated EMT. Although compartmentalization via A-
Haoxiao Zuo, Marina Trombetta-Lima, Irene H. Heijink, Christina H. T. J. van der Veen, Laura Hesse, Klaas Nico Faber, Wilfred J. Poppinga, Harm Maarsingh, Viacheslav O. Nikolaev, Martina Schmidt   +9 more
doaj   +1 more source

The Stapled AKAP Disruptor Peptide STAD-2 Displays Antimalarial Activity through a PKA-Independent Mechanism. [PDF]

PLoS ONE, 2015
Drug resistance poses a significant threat to ongoing malaria control efforts. Coupled with lack of a malaria vaccine, there is an urgent need for the development of new antimalarials with novel mechanisms of action and low susceptibility to parasite ...
Briana R Flaherty, Yuxiao Wang, Edward C Trope, Tienhuei G Ho, Vasant Muralidharan, Eileen J Kennedy, David S Peterson   +6 more
doaj   +1 more source

Role for A Kinase-anchoring Proteins (AKAPS) in Glutamate Receptor Trafficking and Long Term Synaptic Depression [PDF]

Journal of Biological Chemistry, 2005
Expression of N-methyl d-aspartate (NMDA) receptor-dependent homosynaptic long term depression at synapses in the hippocampus and neocortex requires the persistent dephosphorylation of postsynaptic protein kinase A substrates. An attractive mechanism for expression of long term depression is the loss of surface AMPA (alpha-amino-3-hydroxy-5 ...
Eric M, Snyder, Marcie, Colledge, Robert A, Crozier, Wendy S, Chen, John D, Scott, Mark F, Bear   +5 more
openaire   +2 more sources

AKAP6 and phospholamban colocalize and interact in HEK‐293T cells and primary murine cardiomyocytes

Physiological Reports, 2019
Phospholamban (PLN) is an important Ca2+ modulator at the sarcoplasmic reticulum (SR) of striated muscles. It physically interacts and inhibits sarcoplasmic reticulum Ca2+ ATPase (SERCA2) function, whereas a protein kinase A (PKA)‐dependent ...
Farigol Hakem Zadeh, Allen C. T. Teng, Uros Kuzmanov, Paige J. Chambers, Allan R. Tupling, Anthony O. Gramolini   +5 more
doaj   +1 more source

GABAC-Receptor Stimulation Activates cAMP-Dependent Protein Kinase via A-Kinase Anchoring Protein 220

Journal of Pharmacological Sciences, 2008
In our previous study, anti-apoptotic effects of GABAC-receptor stimulation was suppressed by inhibitors of cAMP-dependent protein kinase (PKA), implying GABACreceptor–mediated PKA activation. The present study showed that GABAC-receptor stimulation with
Li Yang, Yasuhisa Nakayama, Naoki Hattori, Bing Liu, Chiyoko Inagaki   +4 more
doaj   +1 more source