Results 61 to 70 of about 4,627,885 (297)

Targeting autophagy-related protein kinases for potential therapeutic purpose

open access: yesActa Pharmaceutica Sinica B, 2020
Autophagy, defined as a scavenging process of protein aggregates and damaged organelles mediated by lysosomes, plays a significant role in the quality control of macromolecules and organelles.
Honggang Xiang   +5 more
doaj   +1 more source

Reconstructing enzyme evolution by protein engineering

open access: yesFEBS 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   +2 more
wiley   +1 more source

PKD1 3D Structure Model and Docking Studies for New PKD Inhibitors [PDF]

open access: yes, 2013
Protein kinase Ds (PKDs) are diacylglycerol (DAG)-regulated serine/threonine protein kinases. In intact cells, PKDs are key mediators in cellular processes pertaining to multiple diseases, including cancer, heart diseases, angiogenesis and immune ...
Xu, Qi
core  

Presynaptically localized cyclic GMP-dependent protein kinase 1 is a key determinant of spinal synaptic potentiation and pain hypersensitivity [PDF]

open access: yes, 2012
Synaptic long-term potentiation (LTP) at spinal neurons directly communicating pain-specific inputs from the periphery to the brain has been proposed to serve as a trigger for pain hypersensitivity in pathological states.
Todd, A. J.   +103 more
core   +2 more sources

Transcriptomic profiling of human cardiac cells predicts protein kinase inhibitor-associated cardiotoxicity

open access: yesNature Communications, 2020
Cardiotoxic adverse events associated with kinase inhibitors are a growing concern in clinical oncology. Here the authors use cellular transcriptomic responses of human cardiomyocytes treated with protein kinase inhibitors and the associated drug ...
J. G. Coen van Hasselt   +16 more
doaj   +1 more source

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

open access: yesFEBS 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   +4 more
wiley   +1 more source

6-Br-5methylindirubin-3′oxime (5-Me-6-BIO) targeting the leishmanial glycogen synthase kinase-3 (GSK-3) short form affects cell-cycle progression and induces apoptosis-like death: Exploitation of GSK-3 for treating leishmaniasis [PDF]

open access: yes, 2009
Indirubins known to target mammalian cyclin-dependent kinases (CDKs) and glycogen synthase kinase (GSK-3) were tested for their antileishmanial activity.
Smirlis, Despina   +8 more
core   +4 more sources

Selective inhibition of the kinase DYRK1A by targeting its folding process

open access: yesNature Communications, 2016
Kinase inhibitors are important drugs and usually target the ATP binding pocket of kinases. Here, Kii et al.report a completely new type of kinase inhibitor that specifically targets the protein folding intermediate state, but not the mature form, of the
Isao Kii   +14 more
doaj   +1 more source

Structure-based design and activity modeling of novel epidermal growth factor receptor kinase inhibitors; an in silico approach

open access: yesScientific African, 2020
The development of EGFR kinase inhibitors to treat non-small cell lung cancers is an important medical necessity due to persistent development of resistance by the mutations.
Muhammad Tukur Ibrahim   +3 more
doaj   +1 more source

Liver organoids: modelling complexity in homeostasis and disease

open access: yesFEBS Letters, EarlyView.
Studying liver in vitro has been challenging because simple 2D cell cultures fail to capture liver's cellular and architectural complexity. To bridge this gap, scientists increasingly use organoids, 3D liver models which better mimic liver composition and function. This review examines recent advances in liver organoid complexity and realism, discusses
Anna M. Dowbaj, Meritxell Huch
wiley   +1 more source

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