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Christian Heinis

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Publications associées (86)

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

A Synthetic Factor XIIa Inhibitor Blocks Selectively Intrinsic Coagulation Initiation

Christian Heinis, Shiyu Chen, Vanessa Baeriswyl, Alessandro Zorzi, 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, Sandeep Raghunathan, Stephane Kontos, Alessandro Angelini, 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

Phage Selection of Bicyclic Peptide Ligands of the Notch1 Receptor

Christian Heinis, Freddy Radtke, 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

Phage selection of bicyclic peptides binding Her2

Christian Heinis, Philippe Diderich

Aberrant expression of the epidermal growth factor receptor Her2 has been implicated in various malignancies including breast cancer. Monoclonal antibodies and an antibody drug conjugate targeting Her2 have found wide clinical application. Herein, we aimed ...

Pergamon-Elsevier Science Ltd2014

Chemical biology & drug discovery

Christian Heinis

Elsevier2014

Dithiol amino acids can structurally shape and enhance the ligand-binding properties of polypeptides

Rudolf Hovius, Christian Heinis, Florence Pojer, Shiyu Chen, Ranganath Gopalakrishnan

The disulfide bonds that form between two cysteine residues are important in defining and rigidifying the structures of proteins and peptides. In polypeptides containing multiple cysteine residues, disulfide isomerization can lead to multiple products with ...

Nature Publishing Group2014

Identification of target-binding peptide motifs by high-throughput sequencing of phage-selected peptides

Christian Heinis, Inmaculada Rentero Rebollo, Vanessa Baeriswyl, Michal Sabisz

High-throughput sequencing was previously applied to phage-selected peptides in order to gain insight into the abundance and diversity of isolated peptides. Herein we developed a procedure to efficiently compare the sequences of large numbers of phage-sele ...

Oxford Univ Press2014

Phage Selection of Photoswitchable Peptide Ligands

Christian Heinis, Shiyu Chen, Inmaculada Rentero Rebollo, Silvia Bellotto, Hermann A. Wegner

Photoswitchable ligands are powerful tools to control biological processes at high spatial and temporal resolution. Unfortunately, such ligands exist only for a limited number of proteins and their development by rational design is not trivial. We have dev ...

2014

Phage selection of bicyclic peptides

Christian Heinis, Inmaculada Rentero Rebollo

Bicyclic peptides are small, constrained peptides that can bind with high affinity and selectivity to protein targets. Their small size provides a number of advantages over larger protein-based ligands, including access to chemical synthesis, better tissue ...

Academic Press Inc Elsevier Science2013

Polypeptide inhibitors of urokinase type plasminogen activator

Christian Heinis, Alessandro Angelini

A conjugate which is capable of specific binding to and inhibition of urokinase-type plasminigen activator (UPA) comprising a polypeptide molecule and a scaffold molecule, wherein said polypeptide molecule is attached to said scaffold molecule by at least ...

2013

Directed Evolution of Bicyclic Peptides for Therapeutic Application

Christian Heinis, Philippe Diderich

Many naturally occurring cyclic peptides or derivatives thereof are used as therapeutics such as the human hormones vasopressin and oxytocin or the antibiotics vancomycin and daptomycin. The success of cyclic peptide therapeutics is based on their ability ...

Schweizerische Chemische Gesellschaft2013

Phage display libraries of differently sized bicyclic peptides

Christian Heinis, Alessandro Angelini, Inmaculada Rentero Rebollo

Phage selections with combinatorial libraries of uniformly sized bicyclic peptides have recently yielded potent and selective binders of several protein targets. In this work we varied in a combinatorial fashion the ring sizes of bicyclic peptides in phage ...

Royal Soc Chemistry2013

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

Bicyclic peptide ligands pulled out of cysteine-rich peptide libraries

Christian Heinis, Jeremy Touati, Petr Leiman, Shiyu Chen, Julia Morales Sanfrutos, Inmaculada Rentero Rebollo

Bicyclic peptide ligands were found to have good binding affinity and target specificity. However, the method applied to generate bicyclic ligands based on phage-peptide alkylation is technically complex and limits its application to specialized laboratori ...

2013

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

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

Structurally Diverse Cyclisation Linkers Impose Different Backbone Conformations in Bicyclic Peptides

Christian Heinis, Alessandro Angelini, Shiyu Chen, Julia Morales Sanfrutos

Combinatorial libraries of structurally diverse peptide macrocycles offer a rich source for the development of high-affinity ligands to targets of interest. In this work we have developed linkers for the generation of genetically encoded bicyclic peptides ...

2012

Chemical Biology Approaches to Membrane Homeostasis and Function

Gerardo Turcatti, Kai Johnsson, Luc Reymond, Christian Heinis, Stefan Matile, Howard Riezman

The study of membranes is at a turning point. New theories about membrane structure and function have recently been proposed, however, new technologies, combining chemical, physical, and biochemical approaches are necessary to test these hypotheses. In par ...

2011

Measuring In Vivo Protein Half-Life

Kai Johnsson, Christian Heinis, Didier Trono, Isabelle Barde, Sonia Verp, Karolina Bojkowska, Francesca Santoni de Sio, Sandra Eloise Kjeldsen

Protein turnover critically influences many biological functions, yet methods have been lacking to assess this parameter in vivo. Here, we demonstrate how chemical labeling of SNAP-tag fusion proteins can be exploited to measure the half-life of resident i ...

Elsevier2011

Strategies to prolong the plasma residence time of peptide drugs

Christian Heinis, Lisa Pollaro

Peptides are an attractive class of molecules for the development of therapeutics because they combine unique properties such as high binding affinity, excellent target specificity, low toxicity and a relatively small mass. However, the short in vivo half- ...

2010

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