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Christian Heinis

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Publications associées (85)

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

Christian Heinis, 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

Peptide-Hypervalent Iodine Reagent Chimeras: Enabling Peptide Functionalization and Macrocyclization

Jérôme Waser, Christian Heinis, Xinjian Ji, Xingyu Liu

Herein, we report a novel strategy for the modification of peptides based on the introduction of highly reactive hypervalent iodine reagents-ethynylbenziodoxolones (EBXs)-onto peptides. These peptide-EBXs can be readily accessed, by both solution- and soli ...

Wiley-VCH Verlag GmbH2023

Combination of polycarboxybetaine coating and factor XII inhibitor reduces clot formation while preserving normal tissue coagulation during extracorporeal life support

Christian Heinis, Jonas Alfred Karl Wilbs

Blood contact with high surface area medical devices, such as dialysis and extracorporeal life support (ECLS), induces rapid surface coagulation. Systemic anticoagulation, such as heparin, is thus necessary to slow clot formation, but some patients suffer ...

ELSEVIER SCI LTD2021

Phage selection of chemically stabilized alpha-helical peptide ligands

Christian Heinis, Jörg Hülsken, Davide Bertoldo, Pierre Vincent Dessen, Philippe Diderich, 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

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

Bulk measurement of membrane permeability for random cyclic peptides in living cells to guide drug development

Nathan Moïse De Sadeleer, Christian Heinis, Alexander Lund Nielsen, Anne Sofie Luise Zarda, Rebecca Manuela Neeser

Cyclic peptides are attractive for drug discovery due to their excellent binding properties and the potential to cross cell membranes. However, by far not all cyclic peptides are cell permeable, and measuring or predicting their membrane permeability is no ...

Wiley2025

Cyclic Peptides for Drug Development

Christian Heinis, Alexander Lund Nielsen, Xinjian Ji

Cyclic peptides are fascinating molecules abundantly found in nature and exploited as molecular format for drug development as well as other applications, ranging from research tools to food additives. Advances in peptide technologies made over many years ...

Wiley-VCH Verlag GmbH2024

Generation of a Large Peptide Phage Display Library by Self-Ligation of Whole-Plasmid PCR Product

Kaycie Marie Butler, Christian Heinis, Xudong Kong, Vanessa Carle, Cristina Diaz Perlas

The success of phage display, used for developing target-specific binders based on peptides and proteins, depends on the size and diversity of the library screened, but generating large libraries of phage-encoded polypeptides remains challenging. New pepti ...

2020

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

De novo development of small cyclic peptides that are orally bioavailable

Maury Mariano Duany Benitez, Phoukham Phothirath, Khaled Il Khwildy, Christian Heinis, Alexander Lund Nielsen, Sevan Mleh Habeshian, Manuel Leonardo Merz, Xinjian Ji, Bo Li

Cyclic peptides can bind challenging disease targets with high affinity and specificity, offering enormous opportunities for addressing unmet medical needs. However, as with biological drugs, most cyclic peptides cannot be applied orally because they are r ...

2023

Novel inhibitors of the enzyme activated factor xii (fxiia)

Christian Heinis, Jonas Alfred Karl Wilbs, Vanessa Baeriswyl, Simon Jan Middendorp

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

Bicyclic peptide ligands pulled out of cysteine-rich peptide libraries

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

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, Nicola Salvi, Simone Ulzega, Alessandro Angelini, Roberto Buratto, Inmaculada Rentero Rebollo

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

Thiol-to-amine cyclization reaction enables screening of large libraries of macrocyclic compounds and the generation of sub-kilodalton ligands

João Miguel Franco Machado, Christian Heinis, Gerardo Turcatti, Yu Wu, Xudong Kong, Jonathan Patrice Vesin, Patrick Andreas Gonschorek, Van Manh Pham, Julien Bortoli Chapalay, Sangram Shivdas Kale, Milan Bergeron-Brlek

Macrocyclic compounds are an attractive modality for drug development, but the limited availability of large, structurally diverse macrocyclic libraries hampers the discovery of leads. Here, we describe the discovery of efficient macrocyclization reactions ...

2019

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

Cyclic peptide FXII inhibitor provides safe anticoagulation in a thrombosis model and in artificial lungs

Christina Lamers, Christian Heinis, Xudong Kong, Jonas Alfred Karl Wilbs, Patrick Andreas Gonschorek, Simon Jan Middendorp

Inhibiting thrombosis without generating bleeding risks is a major challenge in medicine. A promising solution may be the inhibition of coagulation factor XII (FXII), because its knock-out or inhibition in animals reduced thrombosis without causing abnorma ...

Nature Research2020

Mutants of o6-alkylguanine-dna alkyltransferase

Kai Johnsson, Christian Heinis, Christopher Chidley, Alexandre Juillerat, Antje Keppler, Thomas Gronemeyer

The invention relates to AGT mutants showing, when compared to the wild type human AGT, two or more advantageous properties selected from (a) reduced DNA interaction (b) localisation of the expressed protein in eukaryotic cells that is no longer restricted ...

2006

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

Cys-Cys and Cys-Lys Stapling of Unprotected Peptides Enabled by Hypervalent Iodine Reagents

Jérôme Waser, Christian Heinis, Elija Grinhagena, Gontran Sangouard, Javier De Ceballos Cerrajeria

Easy access to a wide range of structurally diverse stapled peptides is crucial for the development of inhibitors of protein-protein interactions. Herein, we report bis-functional hypervalent iodine reagents for two-component cysteine-cysteine and cysteine ...

Wiley-VCH Verlag GmbH2021

High-affinity peptides developed against calprotectin and their application as synthetic ligands in diagnostic assays

Christian Heinis, Florence Pojer, Kelvin Ka Ching Lau, Cristina Diaz Perlas, Lluc Farrera Soler

A peptide was developed that binds to calprotectin, a marker of major inflammatory disorders, and found to be suited for diagnostic tests. The use of synthetic peptides in assays is of great interest due to their high precision, robustness and low price. ...

Nature Portfolio2023