Concept

Enzyme inhibitor

Related publications (609)

Arene-Ruthenium(II) Complexes with Bioactive ortho-Hydroxydibenzoylmethane Ligands: Synthesis, Structure, and Cytotoxicity

Paul Joseph Dyson, Tina Riedel, Agnese Petrini

The synthesis of a series of neutral arene-ruthenium (II) complexes (arene = p-cymene, hexamethylbenzene, and benzene) [(arene)Ru(HDB) Cl] derived from the reaction of the appropriate arene-ruthenium(II) dimers and ortho-hydroxydibenzoylmethane (HDBH), a p ...

Wiley-Blackwell2017

Generation and Characterization of Anti-VGLUT Nanobodies Acting as Inhibitors of Transport

Andrea Volterra

The uptake of glutamate by synaptic vesicles is mediated by vesicular glutamate transporters (VGLUTs). The central role of these transporters in excitatory neurotransmission underpins their importance as pharmacological targets. Although several compounds ...

Amer Chemical Soc2017

Generation and Analysis of Large-Scale Dynamic Non-Linear Models of Metabolism

Vassily Hatzimanikatis, Ljubisa Miskovic, Georgios Fengos

Understanding complex responses of metabolic processes in biochemical systems requires the quantitative description of the dynamic interplay between metabolite levels, enzyme levels, and reaction rates. Generation and use of such models is hindered by the ...

2017

Allosteric kinase inhibitors

Oliver Hantschel

Background. Inhibition of the kinase activity of the BCR-ABL1 oncoprotein by an allosteric mechanism of action facilitates alternative treatment options for chronic myeloid leukemia (CML) patients who cannot be adequately treated with conventional catalyti ...

Springer Nature2017

Development of an albumin-binding ligand for prolonging the plasma half-life of peptide therapeutics

Alessandro Zorzi

Peptides represent a promising format for the development of therapeutics since they combine the advantages of proteins and small molecules. Several techniques based on rational design or in vitro evolution can be used to develop peptides as therapeutics. ...

EPFL2017

Role of MCT1 and CAII in skeletal muscle pH homeostasis, energetics, and function: in vivo insights from MCT1 haploinsufficient mice

Pierre Magistretti, Sylvain Eric Lengacher, Luc Pellerin

The purpose of this study was to investigate the effects of a partial suppression of monocarboxylate transporter (MCT)-1 on skeletalmuscle pH, energetics, and function (MCT1(+/-) mice). Twenty-fourMCT1(+/-) and 13 wild-type (WT) mice were subjected to a re ...

Federation of American Society of Experimental Biology2017

Phage Selection of Cyclic Peptides for Application in Research and Drug Development

Christian Heinis, Xudong Kong

Cyclic peptides can bind to protein targets with high affinities and selectivities, which makes them an attractive modality for the development of research reagents and therapeutics. Additional properties, including low inherent toxicity, efficient chemica ...

2017

MnO2 nanosheets as an artificial enzyme to mimic oxidase for rapid and sensitive detection of glutathione

Paul Joseph Dyson, Zhaofu Fei, Jing Liu

Nanozymes are increasingly used as components in assays and diagnostics. Here, we describe a rapid and highly sensitive colorimetric assay for the detection and quantification of glutathione (GSH) employing MnO2 nanosheets as an artificial oxidase. In the ...

Elsevier2017

Evaluating Cellular Drug Uptake with Fluorescent Sensor Proteins

Kai Johnsson, Rudolf Hovius, Rudolf Griss, Kui Thong Tan, Silvia Scarabelli

We are introducing a new approach to evaluate cellular uptake of drugs and drug candidates into living cells. The approach is based on converting the protein target of a given class of compounds into a fluorescent biosensor. By measuring the binding of dif ...

Amer Chemical Soc2017

Synthesis and crystal structure of a chiral lactam and three amino alcohols as potential protein tyrosine phosphates 1B inhibitors

Rosario Scopelliti

Chiral lactam 2 and three chiral 3-amino alcohols 3-5 have been synthesized and characterized by Sspectroscopic techniques. Regioselective ring opening reaction of chiral styrene oxide by an amine nucle-ophile was confirmed by X-ray diffraction data. Ligan ...

Pergamon-Elsevier Science Ltd2017

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