Analysis of neutral mutational drift in an allosteric enzyme. [PDF]
Protein Sci, 2023 Liechty ET +6 more
europepmc +1 more source
Mutations in the PKM2 exon-10 region are associated with reduced allostery and increased nuclear translocation. [PDF]
, 2019 PKM2 is a key metabolic enzyme central to glucose metabolism and energy expenditure. Multiple stimuli regulate PKM2's activity through allosteric modulation and post-translational modifications.
Chen, Tsan-Jan +11 more
core +3 more sources
Advanced Science, EarlyView.DNA‐Based Genetic and Non‐Genetic Tools for Receptor Engineering. This review highlights recent advances in DNA‐based strategies for receptor engineering, including genetic approaches like domain fusion and site‐directed mutagenesis, as well as non‐genetic methods using functional nucleic acids, DNA nanostructures, and dynamic DNA reactions.
Hexin Nan +4 more
wiley +1 more source
Eigenvector Centrality Distribution for Characterization of Protein Allosteric Pathways
, 2018 Determining the principal energy pathways for allosteric communication in biomolecules, that occur as a result of thermal motion, remains challenging due to the intrinsic complexity of the systems involved.
Batista, Victor S. +8 more
core
Phase 1 dose escalation study of the allosteric AKT inhibitor BAY 1125976 in advanced solid cancer-Lack of association between activating AKT mutation and AKT inhibition-derived efficacy [PDF]
, 2019 This open-label, phase I first-in-human study (NCT01915576) of BAY 1125976, a highly specific and potent allosteric inhibitor of AKT1/2, aimed to evaluate the safety, pharmacokinetics, and maximum tolerated dose of BAY 1125976 in patients with advanced ...
Boix, Oliver +14 more
core +3 more sources
Advanced Science, EarlyView.This study identifies PRMT3‐mediated H4R3me2a as a critical driver of tau hyperphosphorylation in primary age‐related tauopathy. Mechanistic insights reveal that the PRMT3/H4R3me2a/miR‐448 axis suppresses IGF1R expression via epigenetic regulation, further dysregulating the PI3K/AKT/GSK3β pathway.
Haotian Liu +9 more
wiley +1 more source
eLife, 2018 Allostery is an inherent feature of proteins, but it remains challenging to reveal the mechanisms by which allosteric signals propagate. A clearer understanding of this intrinsic circuitry would afford new opportunities to modulate protein function. Here,
Daniel A Keedy +9 more
doaj +1 more source
Allo-network drugs: Extension of the allosteric drug concept to protein-protein interaction and signaling networks [PDF]
, 2013 Allosteric drugs are usually more specific and have fewer side effects than orthosteric drugs targeting the same protein. Here, we overview the current knowledge on allosteric signal transmission from the network point of view, and show that most ...
Csermely, Péter +2 more
core +2 more sources
Advanced Science, EarlyView.Through modifying the switchable µ‐oxo bridged FeIII‐porphyrins moiety and NADH mimics into a metal‐organic capsule, multiple responsive manners for O2 activation, chemical oxygenation and metabolic transformation have been demonstrated for upregulating intracellular methionine depletion and accumulation of methionine sulfoxide to achieve effective ...
Chunming Ma +5 more
wiley +1 more source
Chimeric glutamate receptor subunits reveal the transmembrane domain is sufficient for NMDA receptor pore properties but some positive allosteric modulators require additional domains [PDF]
, 2016 NMDA receptors are ligand-gated ion channels that underlie transmission at excitatory synapses and play an important role in regulating synaptic strength and stability.
Huettner, Jmaes E +2 more
core +2 more sources