Publications related to Functional selectivity

Antibodies expand the scope of angiotensin receptor pharmacology

G-protein-coupled receptors (GPCRs) are key regulators of human physiology and are the targets of many small-molecule research compounds and therapeutic drugs. While most of these ligands bind to their target GPCR with high affinity, selectivity is often l ...

2024

Rules and mechanisms governing G protein coupling selectivity of GPCRs

Bruno Emanuel Ferreira De Sousa Correia, Pablo Gainza Cirauqui

G protein-coupled receptors (GPCRs) convert extracellular stimuli into intracellular signaling by coupling to heterotrimeric G proteins of four classes: Gi/o, Gq, Gs, and G12/13. However, our understanding of the G protein selectivity of GPCRs is incomplet ...

Cell Press2023

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

Corey Alfred Stevens

Carbohydrate recognition by lectins governs critical host-microbe interactions. MpPA14 (Marinomonas primoryensis PA14 domain) lectin is a domain of a 1.5-MDa adhesin responsible for a symbiotic bacterium-diatom interaction in Antarctica. Here, we show that ...

Amer Soc Microbiology2021

Bias-Adaptable CO2-to-CO Conversion via Tuning the Binding of Competing Intermediates

Yelin Hu, Jun Li, Shilong Wang, Han Zhang, An Zhang

CO2 electroreduction powered by renewable electricity represents a promising method to enclose anthropogenic carbon cycle. Current catalysts display high selectivity toward the desired product only over a narrow potential window due primarily to unoptimize ...

AMER CHEMICAL SOC2021

A One-Step Biofunctionalization Strategy of Electrospun Scaffolds Enables Spatially Selective Presentation of Biological Cues

Silvestro Micera

To recapitulate the heterogeneous complexity of tissues in the human body with synthetic mimics of the extracellular matrix (ECM), it is important to develop methods that can easily allow the selective functionalization of defined spatial domains. Here, a ...

Wiley2020

Functionalization of second harmonic generation nanoparticles for theranostic applications

Jérémy Vuilleumier

Nowadays, cancer is one of the leading causes of death in developed countries. The actual medical tools to detect cancer at early stage suffer to their low sensitivity. The design of multimodal nanodevices for in vivo imaging offers the perspective of canc ...

EPFL2019

Anticancer Potential of Diiron Vinyliminium Complexes

Paul Joseph Dyson, Lucinda Kate Batchelor, Silvia Schoch

Although ferrocene derivatives have attracted considerable attention as possible anticancer agents, the medicinal potential of diiron complexes has remained largely unexplored. Herein, we describe the straightforward multigram-scale synthesis and the antip ...

WILEY-V C H VERLAG GMBH2019

Mining the Potential of Label-Free Biosensors for In Vitro Antipsychotic Drug Screening

Sandro Carrara, Tugba Kilic, Hatice Altug, Maria Soler Aznar

The pharmaceutical industry is facing enormous challenges due to high drug attribution rates. For the past decades, novel methods have been developed for safety and efficacy testing, as well as for improving early development stages. In vitro screening met ...

2018

Learning Recruits Neurons Representing Previously Established Associations in the Corvid Endbrain

Galyna Pidpruzhnykova

Crows quickly learn arbitrary associations. As a neuronal correlate of this behavior, single neurons in the corvid endbrain area nidopallium caudolaterale (NCL) change their response properties during association learning. In crows performing a delayed ass ...

Mit Press2017

Selective Targeting of SH2 Domain–Phosphotyrosine Interactions of Src Family Tyrosine Kinases with Monobodies

Florence Pojer, Oliver Hantschel, Nadine Eliane Schmit, Tim Kükenshöner

The binding of Src-homology 2 (SH2) domains to phosphotyrosine (pY) sites is critical for the autoinhibition and substrate recognition of the eight Src family kinases (SFKs). The high sequence conservation of the 120 human SH2 domains poses a significant c ...

Elsevier2017

The HDAC inhibitor SAHA improves depressive-like behavior of CRTC1-deficient mice: Possible relevance for treatment-resistant depression

Pierre Magistretti, Jean-René Cardinaux

Major depression is a highly complex disabling psychiatric disorder affecting millions of people worldwide. Despite the availability of several classes of antidepressants, a substantial percentage of patients are unresponsive to these medications. A better ...

Elsevier2016

Impact of organic-ligand shell on catalytic performance of colloidal Pd nanoparticles for alkyne gas-phase hydrogenation

Lioubov Kiwi, Fernando Cardenas Lizana, Daniel André Samuel Lamey, Irina Prokopyeva

Monodispersed Pd nanoparticles (NPs) have been prepared by colloidal technique and deposited on a structured support consisting of carbon nanofibers (CNF) grown on sintered metal fibres (SMF). The surface properties of Pd NPs have been fine-tuned by (i) ch ...

Elsevier2014

Structure Sensitivity of 2-Methyl-3-butyn-2-ol Hydrogenation on Pd: Computational and Experimental Modeling

Lioubov Kiwi, Rocio Micaela Crespo Quesada

In the frame of DFT paradigms, the adsorption of 2-methyl-3-butyn-2-ol (MBY) and 2-methyl-3-buten-2-ol (MBE) on a Pd-30 cluster, including both {100} and {111} faces, was studied along with the pathways involved in the hydrogenation, taking place on plane ...

American Chemical Society2014

Large scale expression and purification of the mouse 5-HT3 receptor

Horst Vogel, Cédric Deluz, Menno Berend Tol, Ghérici Hassaïne

Receptors of the Cys-loop family are central to neurotransmission and primary therapeutic targets. In order to decipher their gating and modulation mechanisms, structural data is essential. However, structural studies require large amounts of pure, functio ...

Elsevier Science Bv2013

Elucidating the role of C-terminal post-translational modifications using protein semisynthesis strategies: α-synuclein phosphorylation at tyrosine 125

Hilal Lashuel, Michel Prudent, Bruno Claude Daniel Fauvet, Mirva Hejjaoui, Filip Vercruysse, Yao Zhang

Despite increasing evidence that supports the role of different post-translational modifications (PTMs) in modulating α-synuclein (α-syn) aggregation and toxicity, relatively little is known about the functional consequences of each modification and whethe ...

2012

Tuning the Chemoselectivity of Rh Nanoparticle Catalysts by Site-Selective Poisoning with Phosphine Ligands: The Hydrogenation of Functionalized Aromatic Compounds

Paul Joseph Dyson, Gabor Laurenczy, Ning Yan, Weijia Gan, Dennis Snelders

The hydrogenation of phenylacetone to cyclohexylacetone, in which the aromatic ring is selectively reduced in preference to the carbonyl group, has been achieved with chemoselectivities exceeding 90%. The catalyst (precatalyst) used to achieve this transfo ...

2012

Synthesis and Biological Evaluation of Modified 2-Deoxystreptamine Dimers

Sandrine Gerber, Inmaculada Robina, Gérald Coste

Aminoglycosides are powerful antibiotics, but the emergence of resistant bacterial strains has prompted the search for analogues with better pharmacological profiles. The synthesis of 2-deoxystreptamine (2-DOS) dimers linked by polyamines and analogues bas ...

2011

Novel organometallic ruthenium complexes for selective activation in tumour cells

Anna Katherine Renfrew

In recent years, ruthenium-based antitumour drugs have emerged as an attractive alternative to cisplatin, exhibiting both excellent activity in tumours where cisplatin is of limited use and low general toxicity, leading to reduced side effects. Two rutheni ...

EPFL2010

Guided Bloch Surface Waves on Ultrathin Polymeric Ridges

Olivier Martin, Hans Peter Herzig, Tristan Sfez, Daniele Brunazzo, Francesco Michelotti

We present a direct evidence of Bloch surface waves (BSWs) waveguiding on ultrathin polymeric ridges, supported by near-field measurements. It is demonstrated that near-infrared BSWs sustained by a silicon-based multilayer can be locally coupled and guided ...

American Chemical Society (ACS)2010

A Short and Convenient Synthesis of 1-Deoxymannojirimycin (DMJ) and N-oxy-Analogues from D-Fructose

Pierre Vogel, Sandrine Gerber, Claudia Bello

The ketonitrone 8 was prepared from D-fructose as an inexpensive starting material, and was used in a stereoselective synthesis of 1-deoxymannojirimycin (4), its previously unknown N-hydroxy analogue 15, as well as the polyhydroxylated ketonitrone 14. The ...

2009