Publications associées à 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