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Christian Heinis

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Related publications (85)

Page 3 of 5

A Synthetic Factor XIIa Inhibitor Blocks Selectively Intrinsic Coagulation Initiation

Christian Heinis, Alessandro Zorzi, Shiyu Chen, Vanessa Baeriswyl

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

Acylated heptapeptide binds albumin with high affinity and application as tag furnishes long-acting peptides

Christian Heinis, Alessandro Zorzi, Jonas Alfred Karl Wilbs, Kaycie Marie Butler, Simon Jan Middendorp

The rapid renal clearance of peptides in vivo limits this attractive platform for the treatment of a broad range of diseases that require prolonged drug half-lives. An intriguing approach for extending peptide circulation times works through a 'piggy-back' ...

Nature Research2017

Tissue Factor-Independent Coagulation Correlates with Clinical Phenotype in Factor XI Deficiency and Replacement Therapy

Christian Heinis, Vanessa Carle

Background In factor XI (FXI) deficiency, bleeding cannot be predicted by routine analyses. Since FXI is involved in tissue factor (TF)-independent propagation loop of coagulation, we hypothesized that investigating the spatiotemporal separated phases of c ...

GEORG THIEME VERLAG KG2020

Phage Display Selection against a Mixture of Protein Targets

Christian Heinis, Xudong Kong

Affinity selections by phage display or other display techniques are typically performed against single targets immobilized as a purified protein. In order to develop cross-specific binders that engage with multiple proteins, such as members of a related f ...

American Chemical Society (ACS)2025

Phage Selection of Photoswitchable Peptide Ligands

Christian Heinis, Shiyu Chen, Inmaculada Rentero Rebollo, Silvia Bellotto

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

Engineering substrate specificity of O6-alkylguanine-DNA alkyltransferase for specific protein labeling in living cells

Kai Johnsson, Christian Heinis, Alexandre Juillerat, India Christina Sielaff, Béatrice Kunz, Hugues Jaccard

Fusion proteins of human O6-alkylguanine-DNA alkyltransferase (AGT) can be specifically labeled with a wide variety of synthetic probes in mammalian cells; this makes them an attractive tool for studying protein function. However, to avoid undesired labeli ...

2005

Precisely Regulated and Efficient Locking of Linear Peptides into Stable Multicyclic Topologies through a One-Pot Reaction

Christian Heinis, Xudong Kong

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

Bicyclic peptides based on dithiol amino acids

Christian Heinis, Shiyu Chen, Ranganath Gopalakrishnan

Springer Wien2016

Development of cyclic peptides that can be administered orally to inhibit disease targets

Christian Heinis, Manuel Leonardo Merz

Cyclic peptides can bind challenging disease targets, but their oral application is hindered by digestion and absorption issues. We developed a versatile method for the synthesis and functional screening of vast numbers of synthetic cyclic peptides and ide ...

2023

Cyclative Release Strategy to Obtain Pure Cyclic Peptides Directly from the Solid Phase

Christian Heinis, Manuel Leonardo Merz, Sevan Mleh Habeshian

The synthesis of large numbers of cyclic peptides-required, for example, in screens for drug development-is currently limited by the need of chromatographic purification of individual peptides. Herein, we have developed a strategy in which cyclic peptides ...

2022

Picomole-Scale Synthesis and Screening of Macrocyclic Compound Libraries by Acoustic Liquid Transfer

Edouard Ehret, Yu Teng Wu, Christian Heinis, Gerardo Turcatti, Alessandro Zorzi, Jonathan Patrice Vesin, Julien Bortoli Chapalay, Cristina Diaz Perlas, Sangram Shivdas Kale, Gontran Sangouard, Mischa Schüttel

Macrocyclic compounds are an attractive class of therapeutic ligands against challenging targets, such as protein-protein interactions. However, the development of macrocycles as drugs is hindered by the lack of large combinatorial macrocyclic libraries, w ...

Wiley-VCH Verlag GmbH2021

Macrocycle synthesis strategy based on step-wise “adding and reacting” three components enables screening of large combinatorial libraries

Carl Leonard Stenbratt, Christian Heinis, Gerardo Turcatti, Alessandro Angelini, Alessandro Zorzi, Jonathan Patrice Vesin, Kaycie Marie Butler, Julien Bortoli Chapalay, Sangram Shivdas Kale, Ganesh Kumar Mothukuri

Macrocycles provide an attractive modality for drug development, but generating ligands for new targets is hampered by the limited availability of large macrocycle libraries. We have established a solution-phase macrocycle synthesis strategy in which three ...

2020

Fast directed evolution of non-immunoglobulin proteins by somatic hypermutation in immune cells

Kai Johnsson, Christian Heinis

A review. New, improved phenotypes. Somatic hypermutation in immune cells can be used for the fast directed evolution of proteins other than Igs (e.g., autofluorescent proteins). The target gene is inserted into the genome of activated B lymphocytes where ...

2005

Generation of a 100-billion cyclic peptide phage display library having a high skeletal diversity

Christian Heinis, Xudong Kong, Vanessa Carle, Alice Comberlato, Cristina Diaz Perlas

Phage display is a powerful technique routinely used for the generation of peptide- or protein-based ligands. The success of phage display selections critically depends on the size and structural diversity of the libraries, but the generation of large libr ...

2021

Synthesis of DNA‐encoded disulfide‐ and thioether‐cyclized peptides

Christian Heinis, Van Manh Pham, Milan Bergeron-Brlek

DNA-encoded chemical library technologies enable the screening of large combinatorial libraries of chemically and structurally diverse molecules, including short cyclic peptides. A challenge in the combinatorial synthesis of cyclic peptides is the final st ...

2020

Bypassing bacterial infection in phage display by sequencing DNA released from phage particles

Christian Heinis, Xudong Kong, Camille Villequey

Phage display relies on a bacterial infection step in which the phage particles are replicated to perform multiple affinity selection rounds and to enable the identification of isolated clones by DNA sequencing. While this process is efficient for wild-typ ...

2017

In Vitro-Evolved Peptides Bind Monomeric Actin and Mimic Actin-Binding Protein Thymosin-β4

Christian Heinis, Jonas Alfred Karl Wilbs, Davide Bertoldo, Ganesh Kumar Mothukuri, Raphael Johannes Gübeli

Actin is the most abundant protein in eukaryotic cells and is key to many cellular functions. The filamentous form of actin (F-actin) can be studied with help of natural products that specifically recognize it, as for example fluorophore-labeled probes of ...

2021

A releasable disulfide-linked peptide tag facilitates the synthesis and purification of short peptides

Yu Teng Wu, Christian Heinis, Alessandro Zorzi

Combinatorial cyclization of hundreds to thousands of random linear peptides by structurally diverse chemical linkers offers access to large macrocyclic compound libraries. A bottleneck in the development of such libraries is the preparation of large numbe ...

Royal Society of Chemistry2020

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

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