Publications related to Receptor antagonist

Bioengineering a glucose oxidase nanosensor for near-infrared continuous glucose monitoring

Ardemis Anoush Boghossian, Hanxuan Wang, Vitalijs Zubkovs

Single-walled carbon nanotubes (SWCNTs) emit photostable near-infrared fluorescence that is conducive for optical glucose monitoring. Such SWCNT-based optical sensors often require the immobilization of proteins that can confer glucose selectivity and reac ...

2022

Allosteric modulators enhance agonist efficacy by increasing the residence time of a GPCR in the active state

Anne-Marinette Thi Phuong Hanh Cao

Here, the authors use smFRET to assess the structural dynamics of metabotropic glutamate receptor mGlu2 and show that a positive allosteric modulator or the Gi protein stabilize mGlu2 in the glutamate-induced active state, leading to the full activation of ...

NATURE PORTFOLIO2021

Degradation study on molecules released from laser-based jet injector

Christophe Moser, Jan Krizek, Barbora Lavickova

Development of needle-free methods to administer injectable therapeutics has been researched for a few decades. We focused our attention on a laser-based jet injection technique where the liquid-jet actuation mechanism is based on optical cavitation. This ...

2021

Inhibition of Thiol‐Mediated Uptake with Irreversible Covalent Inhibitors

Jérôme Waser, Stefan Matile, Eliott Hugo Joran Le Du, Elija Grinhagena, Abhaya Kumar Mishra

Thiol-mediated uptake is emerging as method of choice to penetrate cells. This study focuses on irreversible covalent inhibitors of thiol-mediated uptake. High-content high-throughput screening of the so far largest collection of hypervalent iodine reagent ...

2021

Novel irreversible covalent BTK inhibitors discovered using DNA-encoded chemistry

Sevan Mleh Habeshian, Ying Zhang

Libraries of DNA-Encoded small molecules created using combinatorial chemistry and synthetic oligonucleotides are being applied to drug discovery projects across the pharmaceutical industry. The majority of reported projects describe the discovery of rever ...

PERGAMON-ELSEVIER SCIENCE LTD2021

The role of metal ions in G protein-coupled receptor signalling and drug discovery

Horst Vogel, Shuguang Yuan, Xueying Wang

Metal ions, such as Na+, Mg2+, Ca2+, and Zn2+, are highly abundant in biological systems. For many G protein-coupled receptors (GPCRs), metal ions, especially Na+, have been found to stabilize the receptors' inactivate state preventing receptor activation. ...

WILEY2021

Pharmacological characterization of mutant huntingtin aggregate-directed PET imaging tracer candidates

Hilal Lashuel, Anass Chiki

Huntington's disease (HD) is caused by a CAG trinucleotide repeat expansion in the first exon of the huntingtin (HTT) gene coding for the huntingtin (HTT) protein. The misfolding and consequential aggregation of CAG-expanded mutant HTT (mHTT) underpin HD p ...

NATURE PORTFOLIO2021

Accuracy of Molecular Simulation-Based Predictions of k(off) Values: A Metadynamics Study

Ursula Röthlisberger, Simone Meloni, Viacheslav Bolnykh, Michele Parrinello, Paolo Carloni

The k(off) values of ligands unbinding to proteins are key parameters for drug discovery. Their predictions based on molecular simulation may under- or overestimate experiment in a system- and/or technique-dependent way. Here we use an established method-i ...

AMER CHEMICAL SOC2020

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Receptor antagonist

Bioengineering a glucose oxidase nanosensor for near-infrared continuous glucose monitoring

Allosteric modulators enhance agonist efficacy by increasing the residence time of a GPCR in the active state

Structural Basis of Ligand Selectivity by a Bacterial Adhesin Lectin Involved in Multispecies Biofilm Formation

Degradation study on molecules released from laser-based jet injector

Inhibition of Thiol‐Mediated Uptake with Irreversible Covalent Inhibitors

Novel broad-spectrum virucidal antivirals

Novel irreversible covalent BTK inhibitors discovered using DNA-encoded chemistry

The role of metal ions in G protein-coupled receptor signalling and drug discovery

Pharmacological characterization of mutant huntingtin aggregate-directed PET imaging tracer candidates

Accuracy of Molecular Simulation-Based Predictions of k(off) Values: A Metadynamics Study

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Chat with Graph Search

Allosteric modulators enhance agonist efficacy by increasing the residence time of a GPCR in the active state

Structural Basis of Ligand Selectivity by a Bacterial Adhesin Lectin Involved in Multispecies Biofilm Formation

Degradation study on molecules released from laser-based jet injector

Inhibition of Thiol‐Mediated Uptake with Irreversible Covalent Inhibitors

Novel broad-spectrum virucidal antivirals

Novel irreversible covalent BTK inhibitors discovered using DNA-encoded chemistry

Bioengineering a glucose oxidase nanosensor for near-infrared continuous glucose monitoring

The role of metal ions in G protein-coupled receptor signalling and drug discovery

Pharmacological characterization of mutant huntingtin aggregate-directed PET imaging tracer candidates

Accuracy of Molecular Simulation-Based Predictions of k(off) Values: A Metadynamics Study