Concept

Allosteric modulator

Related publications (54)

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ABCG2 is an ATP-binding cassette (ABC) transporter that protects tissues against xenobiotics, affects the pharmacokinetics of drugs and contributes to multidrug resistance. Although many inhibitors and modulators of ABCG2 have been developed, understanding ...

Springer Nature2018

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L-Lactate is a positive modulator of NMDAR-mediated signaling resulting in plasticity gene induction and memory consolidation. However, L-Lactate is also able to protect neurons against excito-toxic NMDAR activity, an indication of a mitigating action of L ...

NATURE PUBLISHING GROUP2018

Acetyl-CoA carboxylase catalyses the ATP-dependent carboxylation of acetyl-CoA, a rate-limiting step in fatty acid biosynthesis(1,2). Eukaryotic acetyl-CoA carboxylases are large, homodimeric multienzymes. Human acetyl-CoA carboxylase occurs in two isoform ...

Springer Nature2018

Potent Prearranged Positive Allosteric Modulators of the Glucagon-like Peptide-1 Receptor

Rosario Scopelliti, Johannes Broichhagen

Drugs that allosterically modulate G protein-coupled receptor (GPCR) activity display higher specificity and may improve disease treatment. However, the rational design of compounds that target the allosteric site is difficult, as conformations required fo ...

Wiley-V C H Verlag Gmbh2017

Allosteric cross-talk in chromatin can mediate drug-drug synergy

Paul Joseph Dyson, Ursula Röthlisberger, Tina Riedel, Giulia Palermo

Exploitation of drug-drug synergism and allostery could yield superior therapies by capitalizing on the immensely diverse, but highly specific, potential associated with the biological macromolecular landscape. Here we describe a drug-drug synergy mediated ...

2017

Peripuberty, comprising childhood and adolescence, constitutes an important time window in the brain development and maturation. Exposure to prolonged stress during this period has been shown to increase the risk for the development of psychopathologies la ...

EPFL2017

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A popular strategy for overcoming the limited plasma half-life of peptide heptad repeat 2 (HR2) fusion inhibitors against HIV-1 is conjugation with biocompatible polymers such as poly(ethylene glycol) (PEG). However, despite improved resistance to proteoly ...

2017

Human purinergic Gprotein-coupled receptor P2Y(1) (P2Y(1)R) is activated by adenosine 5'-diphosphate (ADP) to induce platelet activation and thereby serves as an important antithrombotic drug target. Crystal structures of P2Y(1)R revealed that one ligand ( ...

Wiley-Blackwell2016

Allosteric regulation promises to open up new therapeutic avenues by increasing drug specificity at G-protein-coupled receptors (GPCRs). However, drug discovery efforts are at present hampered by an inability to precisely control the allosteric site. Herei ...

Wiley-V C H Verlag Gmbh2016

The lipidome associated with the gamma-secretase complex is required for its integrity and activity

Henning Paul-Julius Stahlberg, Patrick Fraering, Hermeto Gerber, Guillermo Miguel Garcia Osuna

gamma-Secretase is a multi-subunit membrane protease complex that catalyses the final intramembrane cleavage of the beta-amyloid precursor protein (APP) during the neuronal production of amyloid-beta peptides (A beta), which are implicated as the causative ...

Portland Press Ltd2016