Concept

Binding selectivity

Related publications (34)

Polycyclic Peptide Therapeutics

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, Olivier Michielin

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

Probing Odorant-Mediated Receptor Activation

Olivia Baud

Molecular interactions of odorants with their olfactory receptors (ORs) are of central importance for the mammalian olfactory system to detect and discriminate a large variety of odors with a limited set of receptors. How a particular OR binds and distingu ...

EPFL2012

Metal-based Chemosensors for Carbohydrates and Biologically Important Ligands

Vera Janowski

Chemosensors based on indicator displacement were developed for the optical detection of different analytes in aqueous solution. The sensing of carbohydrates, including glucose, in aqueous solution at pH 7.4 was achieved by a fluorescent indicator displace ...

EPFL2012

Automated design of ligands to polypharmacological profiles

Daniel Constam

The clinical efficacy and safety of a drug is determined by its activity profile across many proteins in the proteome. However, designing drugs with a specific multi-target profile is both complex and difficult. Therefore methods to design drugs rationally ...

Nature Publishing Group2012

Boosting the Sensitivity of Ligand-Protein Screening by NMR of Long-Lived States

Geoffrey Bodenhausen, Christian Heinis, Aurélien Bornet, Inmaculada Rentero Rebollo, Alessandro Angelini, Simone Ulzega, Nicola Salvi, Roberto Buratto

A new NMR method for the study of ligand protein interactions exploits the unusual lifetimes of long-lived states (LLSs). The new method provides better contrast between bound and free ligands and requires a protein-ligand ratio ca. 25 times lower than for ...

2012

Discovery of a novel pharmacological and structural class of gamma secretase modulators derived from the extract of Actaea racemosa

Patrick Fraering

A screen of a library of synthetic drugs and natural product extracts identified a botanical extract that modulates the processing of amyloid precursor protein (APP) in cultured cells to produce a lowered ratio of amyloid-beta peptide (1-42) (Aβ42) relativ ...

2012

Semisynthetic Fluorescent Sensor Proteins Based on Self-Labeling Protein Tags

Matthias Albert Brun

Genetically encoded fluorescent sensor proteins offer the possibility to probe the concentration of key metabolites in living cells. The approaches currently used to generate such fluorescent sensor proteins lack generality, as they require a protein that ...

EPFL2011

Synthesis and Characterization of a Series of Model Complexes of the Active Site of [Fe]-Hydrogenase (Hmd)

Rosario Scopelliti, Xile Hu, Dafa Chen

A series of Fe complexes were synthesized and characterized as small molecule mimics for the active site of [Fe]-hydrogenase (Hmd). The collection includes both structurally new compounds and analogues of previously reported models. These complexes contain ...

2011

Metal-Based Chemosensors for Important Bioanalytes

Sébastien Rochat

This work describes different strategies for the detection of biologically relevant analytes. The main goal was to achieve sensing in water, which is a prerequisite for application to real biological samples. In several cases, we could demonstrate that our ...

EPFL2010

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