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Christian Heinis

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Publications associées (86)

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

Christian Heinis, Manuel Leonardo Merz, Sevan Mleh Habeshian, Ganesh Ashokrao Sable

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

Method for preparing a library of peptides or a peptide

Christian Heinis

The present invention relates to a method for preparing a library of peptides or an isolated peptide comprising (a) releasing one or more linear dithiol peptides carrying a sulfhydryl group in the N-terminal region of the one or more peptides and being imm ...

2022

Towards the development of orally available cyclic peptides

Christian Heinis

WILEY2022

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

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

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

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

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

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

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

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

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

Christian Heinis, Jérôme Waser, Gontran Sangouard, Elija Grinhagena

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

Development of Selective FXIa Inhibitors Based on Cyclic Peptides and Their Application for Safe Anticoagulation

Christian Heinis, Camille Villequey, Xudong Kong, Kaycie Marie Butler, Vanessa Carle, Christina Lamers, Tamara Maric, Chloé Rogg, Cristina Diaz Perlas

Coagulation factor XI (FXI) has emerged as a promising target for the development of safer anticoagulation drugs that limit the risk of severe and life-threatening bleeding. Herein, we report the first cyclic peptide-based FXI inhibitor that selectively an ...

2021

Novel inhibitors of kallikrein proteases and uses thereof

Christian Heinis, Alessandro Zorzi, Patrick Andreas Gonschorek

The present invention relates to a cyclic inhibitor of a kallikrein protease comprising or consisting of (I) the peptide (X)(X)(X)R(X)(X)(X)(X)(X)(X)(X)(X) (Formula (X)), wherein (X) is present or absent and, is prefer ...

2021

Chemical Biology and Drug Discovery Symposium at the LS2 Annual Meeting 2021

Christian Heinis

SWISS CHEMICAL SOC2021

Novel inhibitors of kallikrein proteases and uses thereof

Christian Heinis, Alessandro Zorzi, Patrick Andreas Gonschorek

The present invention relates to a cyclic inhibitor of a kallikrein protease comprising or consisting of (I) the peptide (X1 (X2)(X3)R(X4)(X5)(X6)(X7)(X8)(X9)(X10)(X11) (Formula (X)), wherein (X1) is present or absent and, is preferably present, and if pre ...

2021

Towards the Development of Orally Available Peptide Therapeutics

Christian Heinis, Xudong Kong

Peptides have a number of attractive properties that make them an interesting modality for drug development, including their ability to bind challenging targets, their high target specificity, and their non-toxic metabolic products. However, a major limita ...

2021

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

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

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

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

Christian Heinis, Alessandro Aliotta, 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

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

De novo development of proteolytically resistant therapeutic peptides for oral administration

Christian Heinis, Florence Pojer, Luciano Andres Abriata, Xudong Kong, Kaycie Marie Butler, Vanessa Carle, Jun Moriya

The oral administration of peptide drugs is hampered by their metabolic instability and limited intestinal uptake. Here, we describe a method for the generation of small target-specific peptides (less than 1,600 Da in size) that resist gastrointestinal pro ...

2020

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

Christian Heinis, Alessandro Zorzi, Yu Teng Wu, Jack Peter Christopher Williams

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

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

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

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

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

Christian Heinis, Xudong Kong, Kaycie Marie Butler, 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

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