Results 71 to 80 of about 10,740 (213)
Chemistry – A European Journal, EarlyView.A modular, de novo α/β‐peptide design strategy allows fine‐tuning of ligand properties, resulting in multivalent ligands that simultaneously target separate binding sites on the protein surface. ABSTRACT Protein‐protein interactions that regulate gene expression in the nucleus are increasingly recognized as potential therapeutic targets but present ...
Márk V. Tresztián +4 more
wiley +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 +3 more
core +1 more source
PLoS Computational Biology, 2018 Intrinsically disordered proteins/regions (IDPs/IDRs) are prevalent in allosteric regulation. It was previously thought that intrinsic disorder is favorable for maximizing the allosteric coupling.
Luhao Zhang, Maodong Li, Zhirong Liu
doaj +1 more source
eLife, 2022 In eukaryotic cells, stressors reprogram the cellular proteome by activating the integrated stress response (ISR). In its canonical form, stress-sensing kinases phosphorylate the eukaryotic translation initiation factor eIF2 (eIF2-P), which ultimately ...
Morgane Boone +5 more
doaj +1 more source
Proteins: Structure, Function, and Bioinformatics, EarlyView.ABSTRACT The GTPase KRAS executes a conformational switch between a GTP‐bound active state and a GDP‐bound inactive state, a process central to oncogenic signaling. However, the structural basis of this switching at the level of residue‐contact organization remains incompletely characterized by traditional binary structural models.
Fatma Senguler Ciftci, Burak Erman
wiley +1 more source
Elasticity as the Basis of Allostery in DNA [PDF]
The Journal of Physical Chemistry B, 2018 Allosteric interactions in DNA are crucial for various biological processes. These interactions are quantified by measuring the change in free energy as a function of the distance between the binding sites for two ligands. Here we show that trends in the interaction energy of ligands binding to DNA can be explained within an elastic birod model.
Jaspreet Singh, Prashant K. Purohit
openaire +3 more sources
Allosteric modulation of the adenosine A2A receptor by cholesterol
eLife, 2022 Cholesterol is a major component of the cell membrane and commonly regulates membrane protein function. Here, we investigate how cholesterol modulates the conformational equilibria and signaling of the adenosine A2A receptor (A2AR) in reconstituted ...
Shuya Kate Huang +8 more
doaj +1 more source
British Journal of Pharmacology, EarlyView.Abstract Background and Purpose β2‐adrenoceptor (β2AR) agonists are the cornerstone of asthma therapy and promote bronchodilation through Gαs signalling in airway smooth muscle (ASM), but their efficacy is limited by β‐arrestin‐mediated β2AR desensitization.
Sushrut D. Shah +7 more
wiley +1 more source
Engineering Allostery into Proteins
, 2019 Our ability to engineer protein structure and function has grown dramatically over recent years. Perhaps the next level in protein design is to develop proteins whose function can be regulated in response to various stimuli, including ligand binding, pH changes, and light.
Scott D, Gorman +3 more
openaire +3 more sources
Convergent Allostery in Ribonucleotide Reductase [PDF]
Nature Communications, 2018 Abstract Ribonucleotide reductases (RNRs) use a conserved radical-based mechanism to catalyze the conversion of ribonucleotides to deoxyribonucleotides. Within the RNR family, class Ib RNRs are notable for being largely restricted to bacteria, including many pathogens, and for lacking an evolutionarily mobile ATP-cone
William C. Thomas +7 more
openaire +3 more sources