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

S. S. Kale; M. Bergeron-Brlek; Y. Wu; M. G. Kumar; M. V. Pham et al. 

Science Advances. 2019-08-21. Vol. 5, num. 8, p. eaaw2851. DOI : 10.1126/sciadv.aaw2851.

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

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

ChemBioChem. 2019-08-05. DOI : 10.1002/cbic.201900390.

Engineered peptide macrocycles can inhibit matrix metalloproteinases with high selectivity

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

Angewandte Chemie. 2019-06-28. Vol. 131, num. 34, p. 11927-11931. DOI : 10.1002/ange.201906791.


Cyclization of peptides with two chemical bridges affords large scaffold diversities

S. Kale; C. Villequey; X. Kong; A. Zorzi; K. Deyle et al. 

Nature Chemistry. 2018. Vol. 10, num. 7, p. 715-723. DOI : 10.1038/s41557-018-0042-7.


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

C. Villequey; X-D. Kong; C. Heinis 

Protein Engineering, Design and Selection. 2017-11-29. Vol. 30, num. 11, p. 761-768. DOI : 10.1093/protein/gzx057.

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 

Nature Communications. 2017. Vol. 8, p. 16092. DOI : 10.1038/ncomms16092.

Polar Hinges as Functionalized Conformational Constraints in (Bi) cyclic Peptides

H. Van De Langemheen; V. Korotkovs; J. Bijl; C. Wilson; S. S. Kale et al. 

Chembiochem. 2017. Vol. 18, num. 4, p. 387-395. DOI : 10.1002/cbic.201600612.

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

W. Liu; Y. Zheng; X. Kong; C. Heinis; Y. Zhao et al. 

Angewandte Chemie-International Edition. 2017. Vol. 56, num. 16, p. 4458-4463. DOI : 10.1002/anie.201610942.

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. 

Journal Of Medicinal Chemistry. 2017. Vol. 60, num. 3, p. 1151-1158. DOI : 10.1021/acs.jmedchem.6b01548.


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

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

Chembiochem. 2016. Vol. 17, num. 24, p. 2299-2303. DOI : 10.1002/cbic.201600336.

Phage selection of chemically stabilized alpha-helical peptide ligands

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

ACS Chemical Biology. 2016. Vol. 11, num. 5, p. 1422-1427. DOI : 10.1021/acschembio.5b00963.

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. 

ACS Medicinal Chemistry Letters. 2016. Vol. 7, num. 6, p. 606-611. DOI : 10.1021/acsmedchemlett.6b00045.

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. 

ChemMedChem. 2016. Vol. 11, num. 8, p. 834-839. DOI : 10.1002/cmdc.201500557.


Phage Selection of Bicyclic Peptide Ligands of the Notch1 Receptor

C. Urech-Varenne; F. Radtke; C. Heinis 

Chemmedchem. 2015. Vol. 10, num. 10, p. 1754-1761. DOI : 10.1002/cmdc.201500261.

A Synthetic Factor XIIa Inhibitor Blocks Selectively Intrinsic Coagulation Initiation

V. Baeriswyl; S. Calzavarini; S. Chen; A. Zorzi; L. Bologna et al. 

Acs Chemical Biology. 2015. Vol. 10, num. 8, p. 1861-1870. DOI : 10.1021/acschembio.5b00103.

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

L. Pollaro; S. Raghunathan; J. Morales-Sanfrutos; A. Angelini; S. Kontos et al. 

Molecular Cancer Therapeutics. 2015. Vol. 14, num. 1, p. 151-161. DOI : 10.1158/1535-7163.Mct-14-0534.


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

I. R. Rebollo; M. Sabisz; V. Baeriswyl; C. Heinis 

Nucleic Acids Research. 2014. Vol. 42, num. 22, p. e169. DOI : 10.1093/nar/gku940.

Chemical biology & drug discovery

L. H. Jones; C. Heinis 

European Journal Of Medicinal Chemistry. 2014. Vol. 88, p. 1-2. DOI : 10.1016/j.ejmech.2014.10.017.

Phage selection of bicyclic peptides binding Her2

P. Diderich; C. Heinis 

Tetrahedron. 2014. Vol. 70, num. 42, p. 7733-7739. DOI : 10.1016/j.tet.2014.05.106.

Drug discovery: tools and rules for macrocycles

C. Heinis 

Nature chemical biology. 2014. Vol. 10, num. 9, p. 696-8. DOI : 10.1038/nchembio.1605.

Phage Selection of Photoswitchable Peptide Ligands

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

Journal Of The American Chemical Society. 2014. Vol. 136, num. 16, p. 5880-5883. DOI : 10.1021/ja501861m.

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

S. Chen; R. Gopalakrishnan; T. Schaer; F. Marger; R. Hovius et al. 

Nature Chemistry. 2014. Vol. 6, p. 1009-1016. DOI : 10.1038/nchem.2043.

Peptide ligands stabilized by small molecules

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

Angewandte Chemie (International ed. in English). 2014. Vol. 53, num. 6, p. 1602-6. DOI : 10.1002/anie.201309459.


Tracking chemical reactions on the surface of filamentous phage using mass spectrometry

S. Chen; J. Touati; C. Heinis 

Chemical communications (Cambridge, England). 2013. Vol. 50, num. 40, p. 5267-5269. DOI : 10.1039/c3cc47496h.

Directed Evolution of Bicyclic Peptides for Therapeutic Application

P. Diderich; C. Heinis 

Chimia. 2013. Vol. 67, num. 12, p. 910-915. DOI : 10.2533/chimia.2013.910.

Improving binding affinity and stability of peptide ligands by substituting glycines with D-amino acids

S. Chen; D. Gfeller; S. A. Buth; O. Michielin; P. G. Leiman et al. 

Chembiochem : a European journal of chemical biology. 2013. Vol. 14, num. 11, p. 1316-1322. DOI : 10.1002/cbic.201300228.

Development of a selective peptide macrocycle inhibitor of coagulation factor XII toward the generation of a safe antithrombotic therapy

V. Baeriswyl; S. Calzavarini; C. Gerschheimer; P. Diderich; A. Angelillo-Scherrer et al. 

Journal of medicinal chemistry. 2013. Vol. 56, num. 9, p. 3742-3746. DOI : 10.1021/jm400236j.

Pattern-Based Sensing of Peptides and Aminoglycosides with a Single Molecular Probe

B. R. Lee; S. Chen; C. Heinis; R. Scopelliti; K. Severin 

Organic Letters. 2013. Vol. 15, p. 3456-3459. DOI : 10.1021/ol401495c.

Bicyclic peptide ligands pulled out of cysteine-rich peptide libraries

S. Chen; R. R. Inmaculada; S. A. Buth; J. Morales-Sanfrutos; J. Touati et al. 

Journal of the American Chemical Society. 2013. Vol. 135, num. 17, p. 6562-6569. DOI : 10.1021/ja400461h.

Phage display libraries of differently sized bicyclic peptides

I. R. Rebollo; A. Angelini; C. Heinis 

Medchemcomm. 2013. Vol. 4, num. 1, p. 145-150. DOI : 10.1039/c2md20171b.

Polycyclic Peptide Therapeutics

V. Baeriswyl; C. Heinis 

Chemmedchem. 2013. Vol. 8, num. 3, p. 377-384. DOI : 10.1002/cmdc.201200513.

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

V. Baeriswyl; C. Heinis 

Protein engineering, design & selection : PEDS. 2013. Vol. 26, num. 1, p. 81-89. DOI : 10.1093/protein/gzs085.