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Christian Heinis

Publications associées (85)

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We report the discovery of a small phenyl molecule with four isosteric thiolate-reactive groups of sequentially varied reactivity. This molecule was exploited in combination with cysteine/penicillamine thiolates of different nucleophilic reactivity for pre ...

Wiley-Blackwell2017

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Cyclic peptides binding to targets of interest can be generated efficiently with powerful in vitro display techniques, such as phage display or mRNA display. The cyclic peptide libraries screened with these methods are generated by altering in a combinator ...

2016

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Upregulation of b-catenin, the primary mediator of the Wnt signaling pathway, plays an important role in the tumorigenesis of several types of human cancer. Targeting b-catenin to interfere with its ability to serve as a translational co-activator is consi ...

2016

Phage selection of chemically stabilized alpha-helical peptide ligands

Christian Heinis, Pierre Vincent Dessen, Philippe Diderich, Davide Bertoldo, Maola Khan Mohammad Golam

Short alpha-helical peptides stabilized by linkages between constituent amino acids offer an attractive format for ligand development. In recent years, a range of excellent ligands based on stabilized alpha-helices were generated by rational design using a ...

2016

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The present invention relates to a bicyclic inhibitor of the coagulation enzyme activated factor XII (FXIIa) comprising or consisting of the peptide (X1)(X2)(X3)n(X4)(X5)(X6)m(X7)(X9)l(X10)(X11)(X12)(X13)(X14)k(X15)(X16), wherein (X1) is present or absent ...

2016

Development of potent and selective S. aureus sortase A inhibitors Based on Peptide Macrocycles

Christian Heinis, Inmaculada Rentero Rebollo, Davide Bertoldo

Sortases are transpeptidase enzymes that anchor surface proteins, including virulence factors, to the cell wall of Gram-positive bacteria, and they are potential targets for the development of anti-infective agents. While several large compound libraries w ...

2016

Phage Selection of Bicyclic Peptide Ligands of the Notch1 Receptor

Freddy Radtke, Christian Heinis, Charlotte Marie Urech-Varenne

Precise regulation of the Notch signaling pathway is crucial, as increases or deficiencies in signaling are associated with diseases, including a wide range of cancers. Recent studies have demonstrated that monoclonal antibodies that bind and stabilize the ...

Wiley-Blackwell2015

A Synthetic Factor XIIa Inhibitor Blocks Selectively Intrinsic Coagulation Initiation

Christian Heinis, Shiyu Chen, Alessandro Zorzi, Vanessa Baeriswyl, Luca Bologna

Coagulation factor XII (FXII) inhibitors are of interest for the study of the protease in the intrinsic coagulation pathway, for the suppression of contact activation in blood coagulation assays, and they have potential application in antithrombotic therap ...

American Chemical Society2015

Bicyclic Peptides Conjugated to an Albumin-Binding Tag Diffuse Efficiently into Solid Tumors

Christian Heinis, Stephane Kontos, Alessandro Angelini, Sandeep Raghunathan, Lisa Pollaro, Julia Morales Sanfrutos

Monoclonal antibodies have long in vivo half-lives and reach high concentrations in tumors but cannot access all regions in the tissue, whereas smaller ligands such as peptides distribute better but are limited by low concentrations due to fast renal clear ...

Amer Assoc Cancer Research2015

Encoded libraries of chemically modified peptides

Christian Heinis

The use of powerful technologies for generating and screening DNA-encoded protein libraries has helped drive the development of proteins as pharmaceutical ligands. However the development of peptides as pharmaceutical ligands has been more limited. Althoug ...

Elsevier2015