Results 81 to 90 of about 2,078,396 (299)

Recent developments of protein kinase inhibitors as potential AD therapeutics

Frontiers in Cellular Neuroscience, 2013
Present Alzheimer’s disease (AD) therapies suffer from inefficient effects on AD symptoms like memory or cognition, especially in later states of the disease.
V. Tell, A. Hilgeroth
semanticscholar   +1 more source

Reconstructing enzyme evolution by protein engineering

FEBS Letters, EarlyView.
Natural enzyme evolution can be retraced by protein engineering methods such as directed evolution, rational design, and ancestral sequence reconstruction. These approaches reveal how enzymes emerged from ligand‐binding scaffolds, developed varying substrate preferences, formed oligomeric complexes, adapted to environmental changes, and evolved novel ...
Lukas Drexler, Markus R. Busch, Reinhard Sterner   +2 more
wiley   +1 more source

An epithelial GPR35 isoform supports tumor‐associated transcriptional and metabolic phenotypes

FEBS Letters, EarlyView.
GPR35 generates two functionally distinct isoforms with previously unresolved roles. GPR35‐short mediates immune‐cell chemotaxis, while GPR35‐long is enriched in colorectal cancer epithelium, where it supports increased metabolism, proliferation, and tumor‐associated transcriptional programs.
Jørgen D. Rønneberg, Martine Hjeltnes, Josephine Krieger, Joshua E. Elias, Maria Stensland, Kristian Holm, Xiaojun Jiang, Chuki Khangsar, Tuula A. Nyman, Arthur Kaser, Johannes R. Hov, Tom H. Karlsen, Nicole C. Kaneider, Frode L. Jahnsen, Georg Schneditz   +14 more
wiley   +1 more source

Repression of cholesterol 7 alpha-hydroxylase transcription by bile acids is mediated through protein kinase C in primary cultures of rat hepatocytes.

Journal of Lipid Research, 1995
Inhibitors of protein kinases were screened for the ability to prevent the repression of cholesterol 7 alpha-hydroxylase mRNA by taurocholate in primary cultures of adult rat hepatocytes.
R T Stravitz, Z R Vlahcevic, E C Gurley, P B Hylemon   +3 more
doaj   +1 more source

Discerning protein pools by selective staining with self‐labeling tags

FEBS Letters, EarlyView.
Cell surface proteins have an intra‐ and extracellular pool. Combining genetic fusion to self‐labeling tags that can be addressed with small molecule fluorophores allows separating these pools. We highlight recent developments and techniques for state‐of‐the‐art interrogation of cell surface proteins in the complex tissue setting.
Kati Fischermanns, Johannes Broichhagen
wiley   +1 more source

Unlocking the therapeutic potential of protein kinase inhibitors in neurodegenerative and psychiatric disorders [PDF]

Exploration of Drug Science
Protein phosphorylation is a fundamental regulatory mechanism governing a broad spectrum of cellular processes. In the nervous system, it is critical for modulating neurotransmitter release, synaptic plasticity, neuronal excitability, and cell survival ...
Angela Asir R V, Polina Buzaeva, Izhak Michaelevski   +2 more
doaj   +1 more source

Developing irreversible inhibitors of the protein kinase cysteinome

Chemistry and Biology, 2013
Protein kinases are a large family of approximately 530 highly conserved enzymes that transfer a γ-phosphate group from ATP to a variety of amino acid residues such as tyrosine, serine and threonine which serves as a ubiquitous mechanism for cellular ...
Qingsong Liu, Yogesh Sabnis, Zheng Zhao, Tinghu Zhang, S. Buhrlage, L. Jones, N. Gray   +6 more
semanticscholar   +1 more source

Nutrient/TOR signaling controls adipose mitochondrial transcription factor A (TFAM) to regulate organismal growth in Drosophila

FEBS Letters, EarlyView.
Animals must match their growth rate to available nutrients. We show that in Drosophila larvae, the nutrient‐sensing TOR kinase controls growth by regulating levels of TFAM, a key regulator of mitochondrial function, in the adipose tissue. When nutrients are abundant, high TOR activity suppresses TFAM, lowering mitochondrial bioenergetic activity and ...
Shrivani Sriskanthadevan‐Pirahas, Shahoon Khan, Abhishek Sharma, Byoungchun Lee, Savraj S. Grewal   +4 more
wiley   +1 more source

A Stapled Peptide Mimic of the Pseudosubstrate Inhibitor PKI Inhibits Protein Kinase A

Molecules, 2019
Kinases regulate multiple and diverse signaling pathways and misregulation is implicated in a multitude of diseases. Although significant efforts have been put forth to develop kinase-specific inhibitors, specificity remains a challenge.
Jascha T. Manschwetus, George N. Bendzunas, Ameya J. Limaye, Matthias J. Knape, Friedrich W. Herberg, Eileen J. Kennedy   +5 more
doaj   +1 more source

Protein kinase inhibitors that inhibit induction of lytic program and replication of Epstein-Barr Virus

Antiviral Research, 2012
Signaling pathways mediating Epstein-Barr virus (EBV) reactivation by Ag-bound B-cell receptor (BCR) were analyzed using a panel of 80 protein kinase inhibitors. Broad range protein kinase inhibitors Staurosporin, K252A, and PKC-412 significantly reduced
R. Goswami, Svetlana Gershburg, A. Satorius, Edward Gershburg   +3 more
semanticscholar   +1 more source