Publications

2018

Cyclization of peptides with two chemical bridges affords large scaffold diversities

Kale, S.S., Villequey, C., Kong, X.D., Zorzi, A., Deyle, K. and Heinis, C.

Nature Chemistry, 2018

2017

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

Villequey, C., Kong, X.D. and Heinis, C.

Protein Engineering, Design and Selection, 2017

 

Phage selection of cyclic peptides for application in research and drug development

Deyle, K., Kong, X.D. and Heinis, C.

Accounts of Chemical Research, 2017

 

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

Zorzi, A., Middendorp, S.J., Wilbs, J., Deyle, K. and Heinis, C.

Nature Communications, 2017

 

Cyclic peptide therapeutics: past, present and future

Zorzi, A., Deyle, K. and Heinis, C.

Current Opinion in Chemical Biology, 2017

 

Precisely-regulated and one-pot locking of linear peptides into stable multicyclic topologies

Liu, W., Zheng, Y., Kong, X.D., Heinis, C., Zhao, Y. and Wu, C.

Angew. Chem. Int. Ed., 2017

 

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

Middendorp, S.J., Wilbs, J., Quarroz, C., Calzavarini, S., Angelillo-Scherrer, A. and Heinis, C.

Journal of Medicinal Chemistry, 2017

 

Peptide mit hoher Bindungsaffinität

Lamers, C. and Heinis, C.

Nachrichten aus der Chemie, 2017

2016

Polar hinges as functionalized conformational constraints in (bi)cyclic peptides

Korotkovs, V., Bijl, J., Wilson, C., van de Langemheen, H., Kale, S., Heinis, C. and Liskamp, R.M.

ChemBioChem, 2016

 

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

Wilbs, J., Middendorp, S.J. and Heinis, C.

ChemBioChem, 2016

 

Development of potent and selective S. Aureus sortase A inhibitors based on peptide macrocycles

Rentero Rebollo, I., McCallin, S., Bertoldo, D., Entenza, J., Moreillon, P. and Heinis, C.

ACS Medicinal Chemistry Letters, 2016

 

Phage selection of chemically stabilized alpha-helical peptide ligands

Diderich, P., Bertoldo, D., Dessen, P., Khan, M.M., Pizzitola, I., Held, W., Huelsken, J. and Heinis, C.

ACS Chemical Biology, 2016

 

Phage selection of peptide macrocycles against beta-catenin to interfere with Wnt signalling

Bertoldo, D., Khan, M.M., Dessen, P., Held, W., Huelsken, J. and Heinis, C.

ChemMedChem, 2016

2015

Phage selection of bicyclic peptide ligands of the Notch1 receptor

Urech-Varenne, S., Radtke, F. and Heinis, C.

ChemMedChem, 2015

 

A synthetic factor XIIa inhibitor blocks selectively intrinsic coagulation initiation

Baeriswyl, V., Calzavarini, S., Chen, S., Zorzi, A., Bologna, L., Angelillo-Scherrer, A., and Heinis, C.

ACS Chemical Biology, 2015

 

Encoded libraries of chemically modified peptides

Heinis, C. and Winter G.

Current Opinion in Chemical Biology, 2015

 

Phage selection of bicyclic peptides based on two disulfide bridges

Chen, S. and Heinis, C.

Methods in Molecular Biology, 2015

 

Bicyclic peptides conjugated to an albumin-binding tag diffuse efficiently into solid tumors

Pollaro, L., Ranghunathan, S., Morales-Sanfrutos, J., Angelini, A., Kontos, S. and Heinis, C.

Molecular Cancer Therapeutics, 2015

 

2014

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

Rentero Rebollo, I., Sabisz, M., Baeriswyl, V. and Heinis, C.

Nucleic Acid Research, 2014

 

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

Chen, S., Gopalakrishnan, R., Schaer, T., Heinis, C., Marger, F., Hovius, R., Bertrand, D., Pojer, F. and Heinis, C.

Nature Chemistry, 2014

 

 

Chemical biology & drug discovery

Jones, L. and Heinis, C.

European Journal of Medicinal Chemistry, 2014

 

Drug discovery: Tools and rules for macrocycles

Heinis, C.

Nature Chemical Biology, 2014

 

Phage selection of bicyclic peptides binding Her2

Diderich, P. and Heinis, C.

Tetrahedron, 2014

 

Phage selection of photoswitchable peptides

Bellotto, S., Chen, S., Rentero Rebollo, I., Wegner, H. and Heinis, C.

J. Am. Chem. Soc., 2014

 

Bicyclic peptides structured by small molecules

Chen, S., Bertoldo, D., Angelini, A., Pojer, F. and Heinis, C.

Angew. Chem. Int. Ed., 2014

2013

 

Directed evolution of bicyclic peptides for therapeutic application

Diderich, P. and Heinis, C.

Chimia, 2013

 

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

Chen, S., Touati, J. and Heinis, C.

ChemComm, 2013

 

Phage selection of mono- and bicyclic peptide ligands

Chen, S. and Heinis, C.

Biotherapeutics – Recent developments using chemical and molecular biology, 2013

 

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

Chen, S., Gfeller, D., Buth, S.A., Michielin, O., Leiman, P.G. and Heinis, C.

ChemBioChem, 2013

 

Development of a selective peptide macrocycle inhibitor of coagulation factor XII toward the generation of a safe anti-thrombotic therapy

Baeriswyl, V., Calzavarini, S., Gerschheimer, C., Diderich, P., Angelillo-Scherrer, A., and Heinis, C.

J. Med. Chem., 2013

 

Bicyclic peptide ligands pulled out of cysteine-rich peptide libraries

Chen, S., Rentero-Rebollo, I., Buth,S.A., Morales-Sanfrutos, J., Touati, J., Leiman, P.G. and Heinis, C.

J. Am. Chem. Soc., 2013

 

Polycyclic peptide therapeutics

Baeriswyl, V. and Heinis, C.

ChemMedChem, 2013

 

Phage selection of bicyclic peptides

Rentero Rebollo, I. and Heinis, C.

Methods, 2013

 

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

Baeriswyl, V. and Heinis, C.

PEDS, 2013

2012

Bicyclization and tethering to albumin yields long-acting peptide antagonist

Angelini, A., Morales-Sanfrutos, J., Diderich, P., Chen, S. and Heinis, C.

J. Med. Chem., 2012

 

Highlighted in SciBX: Distillery: Techniques – Drug platforms

Bicyclic peptides conjugated to an albumin-binding peptide to extend serum half-life

 

 

Phage display libraries of differently sized bicyclic peptides

Rentero-Rebollo, I., Angelini, A. and Heinis, C.

MedChemComm, 2012

 

Chemical macrocyclization of peptides fused to antibody Fc fragments

Angelini, A., Diderich, P., Morales-Sanfrutos, J., Thurnheer, S., Hacker, D., Menin, L., and Heinis, C.

Bioconjugate Chemistry, 2012

 

Boosting the sensitivity of ligand-protein screening by NMR of long-lived states

Salvi, N., Buratto, A., Bornet, A., Ulzega, S., Rentero Rebollo, I., Angelini, A., Heinis, C. and Bodenhausen, G.

J. Am. Chem. Soc., 2012

 

Measuring net protease activities in biological samples using selective peptidic inhibitors

Lisa, P., Diderich, P., Angelini, A., Bellotto, S., Wegner, H. and Heinis, C.

Analytical Biochemistry, 2012

 

Bicyclic peptides with optimized ring size inhibit human plasma kallikrein and its orthologs while sparing paralogous proteases

Baeriswyl, V., Rapley, H., Pollaro, L., Stace, C., Teufel, D., Walker, E., Chen, S., Winter, G., Tite, J. and Heinis, C.

ChemMedChem, 2012

 

 

Structurally diverse cyclization linkers impose different backbone conformations in bicyclic peptides

Chen, S., Morales-Sanfrutos, J., Angelini, A., Cutting, B. and Heinis, C.

ChemBioChem, 2012

 

Bicyclic peptide inhibitor reveals large conact interface with protease target

Angelini, A., Cendron, L., Chen, S., Touati, J., Winter, G., Zanotti, G. and Heinis, C.

ACS Chemical Biology, 2012

2011

Screening of large molecule diversitites by phage display

Rentero, I and Heinis, C.

Chimia, 2011, 65(9)

 

Young Researcher

Heinis, C.

MedChemWatch, 2011, 14, www.efmc.info/medchemwatch-2011-3/index.php

 

Bicyclic peptide antagonists derived from genetically encoded combinatorial libraries

Heinis, C.

Chimia, 2011, 65(11)

 

Synthesis and photochemical properties of oligo-ortho-azobenzenes

Bellotto, S., Reuter, R., Heinis, C. and Wegner, H.A.

J. Org. Chem., 2011, 76(23)

 

Measuring in vivo protein half-life

Bojkowska, K., Santoni de Sio, F., Barde, I., Offner, S., Verp, S., Heinis, C., Johnsson, K. and Trono, D.

Chemistry & Biology, 2011, 18(6)

 

Post-translational modification of genetically encoded polypeptide libraries

Angelini, A. and Heinis, C.

Curr. Opin. Chem. Biol., 2011, 15(3)

 

Enzymatic cyclisation of peptides with transglutaminase

Touati, J., Angelini, A., Hinner, M.J. and Heinis, C.

ChemBioChem, 2011, 12(1)

 

Strategies to prolong the plasma residence time of peptide drugs

Pollaro, L. and Heinis, C.

Med. Chem. Commun., 2011, 1

 

2010

 
Using peptide loop insertion mutagenesis for the evolution of proteins
Christian Heinis and Kai Johnsson*
Methods in Molecular Biology, 2010
 

2009

Phage-encoded combinatorial chemical libraries based on bicyclic peptides
Christian Heinis*, Trevor Rutherford, Stefan Freund, and Greg Winter*
Nature Chemical Biology, 2009