Ligand-Directed Site-Selective Cysteine Bioconjugation of the KELCH Domain of KEAP1 with Hypervalent Iodine Reagents

C. A. J. Marty; X. Ji; S. Nicolai; C. Heinis; J. Waser 

Yeast display technology enables rapid discovery of low-nanomolar macrocyclic peptide inhibitors of human angiotensin-converting enzyme 2

A. Angelini; Z. Romanyuk; G. Bettin; P. Brear; S. Linciano et al. 

Screening macrocyclic peptide libraries by yeast display allows control of selection process and affinity ranking

S. Linciano; Y. Mazzocato; Z. Romanyuk; F. Vascon; L. Farrera‐Soler et al. 

Biodiversity2Drugs—Renaissance of exploring nature‐derived peptides for GPCR ligand discovery

C. W. Gruber; I. Beets; P. T. Boudreault; V. da Silva Bolzani; J. Carlsson et al. 

Structure‐affinity relationship analysis and affinity maturation of a calprotectin‐binding peptide

L. Farrera Soler; C-W. Hu; B. Ricken; C. Diaz-Perlas; C-B. Gerhold et al. 

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

A. L. Nielsen; C. R. O. Bartling; A. Zarda; N. M. De Sadeleer; R. M. Neeser et al. 

Discovery of De Novo Macrocycle Inhibitors of Histone Deacetylase 11

D. Danková; A. L. Nielsen; A. Zarda; T. N. Hansen; M. Hesse et al. 

Large Libraries of Structurally Diverse Macrocycles Suitable for Membrane Permeation

A. L. Nielsen; Z. Bognar; G. K. Mothukuri; A. S. L. Zarda; M. Schuttel et al. 

Solid-phase peptide synthesis in 384-well plates

M. Schuttel; E. Will; G. Sangouard; A. S. L. Zarda; S. Habeshian et al. 

Cyclic Peptides for Drug Development

X. Ji; A. L. Nielsen; C. Heinis 

Methods for high-throughput synthesis and screening of peptide libraries

Discovery of macrocyclic inhibitors of challenging protein-protein interactions

De novo development of small cyclic peptides that are orally bioavailable

M. L. Merz; S. Habeshian; B. Li; J-A. G. L. David; A. L. Nielsen et al. 

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

M. L. Merz; C. Heinis 

High-Density Immobilization of TCEP on Silica Beads for Efficient Disulfide Reduction and Thiol Alkylation in Peptides

M. Schuettel; C. Heinis 

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

X-Y. Liu; X. Ji; C. Heinis; J. Waser 

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

C. Diaz-Perlas; B. Ricken; L. Farrera-Soler; D. Guschin; F. Pojer et al. 

Motifs for making tricycles

C. Heinis 

Development of methods for the synthesis of large combinatorial libraries of macrocyclic compounds

Solid-phase peptide synthesis on disulfide-linker resin followed by reductive release affords pure thiol-functionalized peptides

Z. Bognar; G. K. Mothukuri; A. L. Nielsen; M. L. Merz; P. M. F. Panzar et al. 

Synthesis and direct assay of large macrocycle diversities by combinatorial late-stage modification at picomole scale

S. Habeshian; M. L. Merz; G. Sangouard; G. K. Mothukuri; M. Schüttel et al. 

Phage Display Selected Cyclic Peptide Inhibitors of Kallikrein-Related Peptidases 5 and 7 and Their In Vivo Delivery to the Skin

P. Gonschorek; A. Zorzi; T. Maric; M. Le Jeune; M. Schuettel et al. 

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

S. Habeshian; G. A. Sable; M. Schuettel; M. L. Merz; C. Heinis 

Generating macrocyclic inhibitors of protein-protein interactions

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

G. Sangouard; A. Zorzi; Y. Wu; E. Ehret; M. Schuettel et al. 

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

V. Carle; X-D. Kong; A. Comberlato; C. Edwards; C. Diaz-Perlas et al. 

Towards the Development of Orally Available Peptide Therapeutics

X-D. Kong; C. Heinis 

Combining biological and chemical diversity

C. Heinis 

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

V. Carle; Y. Wu; R. Mukherjee; X-D. Kong; C. Rogg et al. 

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

R. J. Gübeli; D. Bertoldo; K. Shimada; C. B. Gerhold; V. Hurst et al. 

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

N. Naito; R. Ukita; J. Wilbs; K. Wu; X. Lin et al. 

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

J. Ceballos; E. Grinhagena; G. Sangouard; C. Heinis; J. Waser 

Methods for the generation of large combinatorial macrocycle libraries

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

X-D. Kong; V. Carle; C. Díaz-Perlas; K. Butler; C. Heinis 

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

J. Wilbs; X-D. Kong; S. J. Middendorp; R. Prince; A. Cooke et al. 

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

G. K. Mothukuri; S. S. Kale; C. L. Stenbratt; A. Zorzi; J. Vesin et al. 

De novo development of proteolytically resistant therapeutic peptides for oral administration

X-D. Kong; J. Moriya; V. Carle; F. Pojer; L. A. Abriata et al. 

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

Y. Wu; A. Zorzi; J. Williams; C. Heinis 

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

M. V. Pham; M. Bergeron‐Brlek; C. Heinis 

Engineered peptide macrocycles can inhibit matrix metalloproteinases with high selectivity

K. Maola; J. Wilbs; J. Touati; M. Sabisz; X. Kong et al. 

Development of cyclic peptide inhibitors of coagulation factor XIa for safer anticoagulation

Novel Molecular Probes for Non-invasive Optical Imaging of Fatty Acid and Triglyceride Uptake in Living Animals

Development of Tissue Kallikrein Inhibitors for the Treatment of Netherton Syndrome

Development of cyclic peptide inhibitors of coagulation factor XII and matrix metalloproteinase 2

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

C. Villequey; X-D. Kong; C. Heinis 

Peptide macrocycle inhibitor of coagulation factor XII with subnanomolar affinity and high target selectivity

S. J. Middendorp; J. Wilbs; C. Quarroz; S. Calzavarini; A. Angelillo-Scherrer et al. 

Cyclic peptide therapeutics: past, present and future

A. Zorzi; K. Deyle; C. Heinis 

Development of an albumin-binding ligand for prolonging the plasma half-life of peptide therapeutics

Phage Selection of Cyclic Peptides for Application in Research and Drug Development

K. Deyle; X-D. Kong; C. Heinis 

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

A. Zorzi; S. J. Middendorp; J. Wilbs; K. Deyle; C. Heinis 

New methods for developing (bi)cyclic peptides by phage display

Phage selection of chemically stabilized alpha-helical peptide ligands

P. Diderich; D. Bertoldo; P. Dessen; M. M. Khan; I. Pizzitola et al. 

Phage selection of peptide macrocycles against b-catenin to interfere with Wnt signaling

D. Bertoldo; M. M. G. Khan; P. Dessen; W. Held; J. Huelsken et al. 

Improving the binding affinity of in-vitro-evolved cyclic peptides by inserting atoms into the macrocycle backbone

J. Wilbs; S. J. Middendorp; C. Heinis 

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

I. R. Rebollo; S. Mccallin; D. Bertoldo; J. M. Entenza; P. Moreillon et al. 

Generation of photoswitchable peptide ligands by phage display

Improving Bicyclic Peptide Phage Display and Development of Sortase A Inhibitors

Phage Selection of Photoswitchable Peptide Ligands

S. Bellotto; S. Chen; I. R. Rebollo; H. A. Wegner; C. Heinis 

Peptide ligands stabilized by small molecules

S. Chen; D. Bertoldo; A. Angelini; F. Pojer; C. Heinis 

Phage selection of cyclic peptide antagonists with increased stability toward intestinal proteases

V. Baeriswyl; C. Heinis 

Phage Selection of Bicyclic Peptide Ligands and Development of a New Peptide Cyclisation Method

Measuring In Vivo Protein Half-Life

K. Bojkowska; F. Santoni De Sio; I. Barde; S. Offner; S. Verp et al. 

Phage-encoded combinatorial chemical libraries based on bicyclic peptides

C. Heinis; T. Rutherford; S. Freund; G. Winter 

Directed evolution of O6-alkylguanine-DNA alkyltransferase for applications in protein labeling

T. Gronemeyer; C. Chidley; A. Juillerat; C. Heinis; K. Johnsson