Mediaspace scheduled maintenance: Aug 25, 2026 07:00 - 12:00 AM. During this time, videos will be temporarily unavailable. Check status updates.

Concept

Binding selectivity

Related publications (27)

From Sequence to Dynamics to Function: Computational Design of Allostery and Ligand Selectivity in G-Protein Coupled Receptors

Mahdi Hijazi

The phenomenon of allostery, a general property in proteins that has been heralded as "the second secret of life" remains elusive to our understanding and even more challenging to incorporate into protein design. One example of allosteric proteins with gre ...

EPFL2024

Antibodies expand the scope of angiotensin receptor pharmacology

Patrick Daniel Barth, Shuhao Zhang

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

Enantio- and diastereoselective construction of vicinal C(sp(3)) centres via nickel-catalysed hydroalkylation of alkenes

Xile Hu, Srikrishna Bera, Chao Fan

In drug discovery, the proportion of aliphatic carbons (C(sp(3))) and the presence of chiral carbons in organic molecules are positively correlated to their chance of clinical success. Although methods exist for the synthesis of chiral C(sp(3))-rich molecu ...

2022

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

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

Targeting the oncogenic signaling of the transcription factor STAT3 with potent and selective monobody inhibitors

Grégory La Sala

Many targeted cancer therapies fail to improve the overall survival of patients. Limitations involve low drug selectivity and the rapid development of resistance. Moreover, the majority of oncogenic drivers presently remain considered as undruggable as th ...

EPFL2020

A wearable electrochemical sensing system for non-invasive monitoring of lithium drug in bipolar disorder

Giovanni De Micheli, Sandro Carrara, Irene Taurino, Francesca Criscuolo

Lithium represents the main drug for the treatment of Bipolar Disorder (BD) as it acts as a mood stabilizer. However, because of its narrow therapeutic window, psychiatric patients are obliged to frequent tests in hospital to control their lithium blood co ...

2021

Sustainable Hydrogenation of Nitroarenes to Anilines with Highly Active in-situ Generated Copper Nanoparticles

Berend Smit, Mounir Driss Mensi, Kyriakos Stylianou, Christopher Patrick Ireland, Ngoc Tú Nguyên, Fatma Pelin Uran

Metal nanoparticles (NPs) are usually stabilized by a capping agent, a surfactant, or a support material, to maintain their integrity. However, these strategies can impact their intrinsic catalytic activity. Here, we demonstrate that the in-situ formation ...

Wiley-VCH Verlag2020

Asymmetric Alkenyl C−H Functionalization by Cp x Rh III forms 2 H ‐Pyrrol‐2‐ones through [4+1]‐Annulation of Acryl Amides and Allenes

Nicolai Cramer, Shouguo Wang

An efficient CpxRhIII‐catalyzed enantioselective alkenyl C−H functionalization/[4+1] annulation of acryl amides and allenes is reported. The described transformation provides straightforward access to enantioenriched α,β‐unsaturated‐γ‐lactams bearing a qua ...

Wiley-VCH Verlag GmbH2019

Engineered peptide macrocycles can inhibit matrix metalloproteinases with high selectivity

Christian Heinis, Xudong Kong, Jonas Alfred Karl Wilbs, Kaycie Marie Butler, Jeremy Touati, Maola Khan Mohammad Golam, Michal Sabisz

Matrix metalloproteinases (MMPs) are zinc‐dependent endopeptidases at the intersection of health and disease due to their involvement in processes such as tissue repair and immunity as well as cancer and inflammation. Because of the high structural conserv ...

2019

Probing the interaction of nanoparticles with small molecules in real time via quartz crystal microbalance monitoring

Stefan Guldin, Nikolaos Nianias

Despite extensive advances in the field of molecular recognition, the real-time monitoring of small molecule binding to nanoparticles (NP) remains a challenge. To this end, we report on a versatile approach, based on quartz crystal microbalance with dissip ...

2019

Single-molecule sensing of peptides and nucleic acids by engineered aerolysin nanopores

Aleksandra Radenovic, Matteo Dal Peraro, Chan Cao

Nanopore sensing is a powerful single-molecule approach for the detection of biomolecules. Recent studies have demonstrated that aerolysin is a promising candidate to improve the accuracy of DNA sequencing and to develop novel single-molecule proteomic str ...

Nature Research2019

Cyclic peptide therapeutics: past, present and future

Christian Heinis, Alessandro Zorzi, Kaycie Marie Butler

Cyclic peptides combine several favorable properties such as good binding affinity, target selectivity and low toxicity that make them an attractive modality for the development of therapeutics. Over 40 cyclic peptide drugs are currently in clinical use an ...

2017

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

New methods for developing (bi)cyclic peptides by phage display

Camille Villequey

Cyclic peptide ligands are a promising molecular format for the development of therapeutics. They combine some of the advantages of large protein therapeutics (high affinity and specificity) and of small molecule drugs (accessibility to chemical synthesis ...

EPFL2017

Novel Chemosensors for Biologically Important Analytes

Ziya Köstereli

In this work, fluorescent-based chemosensors for the detection of important analytes in aqueous solution are described. The sensors are based on different detection concepts, including analyte-induced aggregation/de-aggregation, pattern-based sensing and m ...

EPFL2015

Catalyst Development for Selective Hydrogenation of Functionalized Alkynes and Nitroarenes

Artur Elterovich Yarulin

Catalyst design is of major importance for fine chemicals industry due to complexity of the synthesis and high product quality requirements. Moreover, the catalyst formulation has to comply with the standards of health, safety and environmental regulati ...

EPFL2014

Generation and characterization of a single-chain anti-EphA2 antibody

Elisa Oricchio

Recombinant antibody phage library technology provides multiple advantages, including that human antibodies can be generated against proteins that are highly conserved between species. We used this technology to isolate and characterize an anti-EphA2 singl ...

2014

Polycyclic Peptide Therapeutics

Christian Heinis, Vanessa Baeriswyl

Owing to their excellent binding properties, high stability, and low off-target toxicity, polycyclic peptides are an attractive molecule format for the development of therapeutics. Currently, only a handful of polycyclic peptides are used in the clinic; ex ...

Wiley-V C H Verlag Gmbh2013

Rational Design of 4-Aryl-1,2,3-Triazoles for Indoleamine 2,3-Dioxygenase 1 Inhibition

Pierre Vogel, Somi Reddy Majjigapu

Indoleamine 2,3-dioxygenase 1 (IDO1) is an important therapeutic target treatment of diseases such as cancer that involve pathological immune escape. Starting from the scaffold of our previously discovered IDO1 inhibitor 4-phenyl-1,2,3-triazole, we used co ...

2012