Complete Publication List


J. A. K. Wilbs : Development of cyclic peptide inhibitors of coagulation factor XII and matrix metalloproteinase 2. Lausanne, EPFL, 2018. DOI : 10.5075/epfl-thesis-8467.


C. Villequey : New methods for developing (bi)cyclic peptides by phage display. Lausanne, EPFL, 2017. DOI : 10.5075/epfl-thesis-8092.
K. Deyle; X.-D. Kong; C. Heinis : Phage Selection of Cyclic Peptides for Application in Research and Drug Development; Accounts Of Chemical Research. 2017. DOI : 10.1021/acs.accounts.7b00184.
A. Zorzi; K. Deyle; C. Heinis : Cyclic peptide therapeutics: past, present and future; Current Opinion In Chemical Biology. 2017. DOI : 10.1016/j.cbpa.2017.02.006.
A. Zorzi; S. J. Middendorp; J. Wilbs; K. Deyle; C. Heinis : Acylated heptapeptide binds albumin with high affinity and application as tag furnishes long-acting peptides; Nature Communications. 2017. DOI : 10.1038/ncomms16092.
A. Zorzi : Development of an albumin-binding ligand for prolonging the plasma half-life of peptide therapeutics. Lausanne, EPFL, 2017. DOI : 10.5075/epfl-thesis-7728.
H. Van De Langemheen; V. Korotkovs; J. Bijl; C. Wilson; S. S. Kale et al. : Polar Hinges as Functionalized Conformational Constraints in (Bi) cyclic Peptides; Chembiochem. 2017. DOI : 10.1002/cbic.201600612.
W. Liu; Y. Zheng; X. Kong; C. Heinis; Y. Zhao et al. : Precisely Regulated and Efficient Locking of Linear Peptides into Stable Multicyclic Topologies through a One-Pot Reaction; Angewandte Chemie-International Edition. 2017. DOI : 10.1002/anie.201610942.
S. J. Middendorp; J. Wilbs; C. Quarroz; S. Calzavarini; A. Angelillo-Scherrer et al. : Peptide Macrocycle Inhibitor of Coagulation Factor XII with Subnanomolar Affinity and High Target Selectivity; Journal Of Medicinal Chemistry. 2017. DOI : 10.1021/acs.jmedchem.6b01548.


C. Heinis; V. Baeriswyl; S. Middendorp; J. A. K. Wilbs ; Novel inhibitors of the enzyme activated factor xii (fxiia). AU2016256226 ; CA2982413 ; WO2016174103 . 2016.
J. Wilbs; S. J. Middendorp; C. Heinis : Improving the Binding Affinity of in-Vitro-Evolved Cyclic Peptides by Inserting Atoms into the Macrocycle Backbone; Chembiochem. 2016. DOI : 10.1002/cbic.201600336.
D. Bertoldo : Screening of structurally diverse bicyclic peptide libraries by phage display. Lausanne, EPFL, 2016. DOI : 10.5075/epfl-thesis-7293.
P. Diderich; D. Bertoldo; P. Dessen; M. M. Khan; I. Pizzitola et al. : Phage Selection of Chemically Stabilized alpha-Helical Peptide Ligands; Acs Chemical Biology. 2016. DOI : 10.1021/acschembio.5b00963.
I. R. Rebollo; S. Mccallin; D. Bertoldo; J. M. Entenza; P. Moreillon et al. : Development of Potent and Selective S. aureus Sortase A Inhibitors Based on Peptide Macrocycles; Acs Medicinal Chemistry Letters. 2016. DOI : 10.1021/acsmedchemlett.6b00045.
D. Bertoldo; M. M. G. Khan; P. Dessen; W. Held; J. Huelsken et al. : Phage Selection of Peptide Macrocycles against -Catenin To Interfere with Wnt Signaling; Chemmedchem. 2016. DOI : 10.1002/cmdc.201500557.


C. Urech-Varenne; F. Radtke; C. Heinis : Phage Selection of Bicyclic Peptide Ligands of the Notch1 Receptor; Chemmedchem. 2015. DOI : 10.1002/cmdc.201500261.
C. Heinis; G. Winter : Encoded libraries of chemically modified peptides; Current Opinion In Chemical Biology. 2015. DOI : 10.1016/j.cbpa.2015.02.008.
V. Baeriswyl; S. Calzavarini; S. Chen; A. Zorzi; L. Bologna et al. : A Synthetic Factor XIIa Inhibitor Blocks Selectively Intrinsic Coagulation Initiation; Acs Chemical Biology. 2015. DOI : 10.1021/acschembio.5b00103.
C. M. Varenne : Phage Selection of Bicyclic Peptides and High-Throughput Screening of Chemical Compounds for the Identification of Novel Inhibitors of the Notch Pathway. Lausanne, EPFL, 2015. DOI : 10.5075/epfl-thesis-6635.
L. Pollaro; S. Raghunathan; J. Morales-Sanfrutos; A. Angelini; S. Kontos et al. : Bicyclic Peptides Conjugated to an Albumin-Binding Tag Diffuse Efficiently into Solid Tumors; Molecular Cancer Therapeutics. 2015. DOI : 10.1158/1535-7163.Mct-14-0534.
S. Bellotto : Generation of photoswitchable peptide ligands by phage display. Lausanne, EPFL, 2015. DOI : 10.5075/epfl-thesis-6483.


I. R. Rebollo; M. Sabisz; V. Baeriswyl; C. Heinis : Identification of target-binding peptide motifs by high-throughput sequencing of phage-selected peptides; Nucleic Acids Research. 2014. DOI : 10.1093/nar/gku940.
L. H. Jones; C. Heinis : Chemical biology & drug discovery; European Journal Of Medicinal Chemistry. 2014. DOI : 10.1016/j.ejmech.2014.10.017.
I. Rentero Rebollo : Improving Bicyclic Peptide Phage Display and Development of Sortase A Inhibitors. Lausanne, EPFL, 2014. DOI : 10.5075/epfl-thesis-6413.
P. Diderich; C. Heinis : Phage selection of bicyclic peptides binding Her2; Tetrahedron. 2014. DOI : 10.1016/j.tet.2014.05.106.
P. Diderich : Development of bicyclic peptide Her2 binders and phage selection of alpha-helical peptide ligands. Lausanne, EPFL, 2014. DOI : 10.5075/epfl-thesis-6427.
C. Heinis : Drug discovery: tools and rules for macrocycles; Nature chemical biology. 2014. DOI : 10.1038/nchembio.1605.
S. Bellotto; S. Chen; I. R. Rebollo; H. A. Wegner; C. Heinis : Phage Selection of Photoswitchable Peptide Ligands; Journal Of The American Chemical Society. 2014. DOI : 10.1021/ja501861m.
S. Chen; R. Gopalakrishnan; T. Schaer; F. Marger; R. Hovius et al. : Dithiol amino acids can structurally shape and enhance the ligand-binding properties of polypeptides; Nature Chemistry. 2014. DOI : 10.1038/nchem.2043.
L. Pollaro : Therapeutic effect and biodistribution of a bicyclic peptide inhibitor of urokinase-type plasminogen activator. Lausanne, EPFL, 2014. DOI : 10.5075/epfl-thesis-6181.
S. Chen; D. Bertoldo; A. Angelini; F. Pojer; C. Heinis : Peptide ligands stabilized by small molecules; Angewandte Chemie (International ed. in English). 2014. DOI : 10.1002/anie.201309459.


C. Heinis; A. Angelini; G. Winter ; Polypeptide inhibitors of urokinase type plasminogen activator. EP2420255 ; EP2420255 . 2013.
S. Chen; J. Touati; C. Heinis : Tracking chemical reactions on the surface of filamentous phage using mass spectrometry; Chemical communications (Cambridge, England). 2013. DOI : 10.1039/c3cc47496h.
P. Diderich; C. Heinis : Directed Evolution of Bicyclic Peptides for Therapeutic Application; Chimia. 2013. DOI : 10.2533/chimia.2013.910.
S. Chen; D. Gfeller; S. A. Buth; O. Michielin; P. G. Leiman et al. : Improving binding affinity and stability of peptide ligands by substituting glycines with D-amino acids; Chembiochem : a European journal of chemical biology. 2013. DOI : 10.1002/cbic.201300228.
V. Baeriswyl; S. Calzavarini; C. Gerschheimer; P. Diderich; A. Angelillo-Scherrer et al. : Development of a selective peptide macrocycle inhibitor of coagulation factor XII toward the generation of a safe antithrombotic therapy; Journal of medicinal chemistry. 2013. DOI : 10.1021/jm400236j.
S. Chen : Development of New Bicyclic Peptide Formats and their Application in Directed Evolution. Lausanne, EPFL, 2013. DOI : 10.5075/epfl-thesis-5947.
I. R. Rebollo; C. Heinis : Phage selection of bicyclic peptides; Methods. 2013. DOI : 10.1016/j.ymeth.2012.12.008.
S. Venet-Bonnot : Human Antibody Libraries Capturing Purpose Oriented CDRH3 Repertoires. Lausanne, EPFL, 2013. DOI : 10.5075/epfl-thesis-5815.
B. R. Lee; S. Chen; C. Heinis; R. Scopelliti; K. Severin : Pattern-Based Sensing of Peptides and Aminoglycosides with a Single Molecular Probe; Organic Letters. 2013. DOI : 10.1021/ol401495c.
S. Chen; R. R. Inmaculada; S. A. Buth; J. Morales-Sanfrutos; J. Touati et al. : Bicyclic peptide ligands pulled out of cysteine-rich peptide libraries; Journal of the American Chemical Society. 2013. DOI : 10.1021/ja400461h.
I. R. Rebollo; A. Angelini; C. Heinis : Phage display libraries of differently sized bicyclic peptides; Medchemcomm. 2013. DOI : 10.1039/c2md20171b.
V. Baeriswyl; C. Heinis : Polycyclic Peptide Therapeutics; Chemmedchem. 2013. DOI : 10.1002/cmdc.201200513.
V. Baeriswyl; C. Heinis : Phage selection of cyclic peptide antagonists with increased stability toward intestinal proteases; Protein engineering, design & selection : PEDS. 2013. DOI : 10.1093/protein/gzs085.


A. Angelini; J. Morales-Sanfrutos; P. Diderich; S. Chen; C. Heinis : Bicyclization and tethering to albumin yields long-acting Peptide antagonists; Journal of medicinal chemistry. 2012. DOI : 10.1021/jm301276e.
J. Touati : Phage Selection of Bicyclic Peptide Ligands and Development of a New Peptide Cyclisation Method. Lausanne, EPFL, 2012. DOI : 10.5075/epfl-thesis-5536.
A. Angelini; P. Diderich; J. Morales-Sanfrutos; S. Thurnheer; D. Hacker et al. : Chemical macrocyclization of peptides fused to antibody Fc fragments; Bioconjugate chemistry. 2012. DOI : 10.1021/bc300184m.
N. Salvi; R. Buratto; A. Bornet; S. Ulzega; I. R. Rebollo et al. : Boosting the Sensitivity of Ligand-Protein Screening by NMR of Long-Lived States; Journal Of The American Chemical Society. 2012. DOI : 10.1021/ja303301w.
L. Pollaro; P. Diderich; A. Angelini; S. Bellotto; H. Wegner et al. : Measuring net protease activities in biological samples using selective peptidic inhibitors; Analytical biochemistry. 2012. DOI : 10.1016/j.ab.2012.04.025.
A. Angelini; L. Cendron; S. Chen; J. Touati; G. Winter et al. : Bicyclic Peptide inhibitor reveals large contact interface with a protease target; ACS chemical biology. 2012. DOI : 10.1021/cb200478t.
V. Baeriswyl; H. Rapley; L. Pollaro; C. Stace; D. Teufel et al. : Bicyclic peptides with optimized ring size inhibit human plasma kallikrein and its orthologues while sparing paralogous proteases; ChemMedChem. 2012. DOI : 10.1002/cmdc.201200071.
S. Chen; J. Morales-Sanfrutos; A. Angelini; B. Cutting; C. Heinis : Structurally Diverse Cyclisation Linkers Impose Different Backbone Conformations in Bicyclic Peptides; Chembiochem. 2012. DOI : 10.1002/cbic.201200049.
I. Rentero; C. Heinis : Screening of large molecule diversities by phage display; Chimia. 2012. DOI : 10.2533/chimia.2011.843.


M. Takahashi-Umebayashi; L. Pineau; T. Hannich; A. Zumbuehl; D. A. Doval et al. : Chemical Biology Approaches to Membrane Homeostasis and Function; Chimia. 2011. DOI : 10.2533/chimia.2011.849.
S. Bellotto; R. Reuter; C. Heinis; H. A. Wegner : Synthesis and photochemical properties of oligo-ortho-azobenzenes; The Journal of organic chemistry. 2011. DOI : 10.1021/jo201996w.
C. Heinis : Bicyclic peptide antagonists derived from genetically encoded combinatorial libraries; Chimia. 2011. DOI : 10.2533/chimia.2011.677.
K. Bojkowska; F. Santoni De Sio; I. Barde; S. Offner; S. Verp et al. : Measuring In Vivo Protein Half-Life; Chemistry & Biology. 2011. DOI : 10.1016/j.chembiol.2011.03.014.
A. Angelini; C. Heinis : Post-translational modification of genetically encoded polypeptide libraries; Current opinion in chemical biology. 2011. DOI : 10.1016/j.cbpa.2011.03.009.


L. Pollaro; C. Heinis : Strategies to prolong the plasma residence time of peptide drugs; Medchemcomm. 2010. DOI : 10.1039/c0md00111b.
J. Touati; A. Angelini; M. J. Hinner; C. Heinis : Enzymatic cyclisation of peptides with a transglutaminase; Chembiochem : a European journal of chemical biology. 2010. DOI : 10.1002/cbic.201000451.
C. Heinis; K. Johnsson : Using peptide loop insertion mutagenesis for the evolution of proteins; Methods in molecular biology (Clifton, N.J.). 2010. DOI : 10.1007/978-1-60761-652-8_16.


C. Heinis; T. Rutherford; S. Freund; G. Winter : Phage-encoded combinatorial chemical libraries based on bicyclic peptides; Nature Chemical Biology. 2009. DOI : 10.1038/nchembio.184.


A. Gautier; A. Juillerat; C. Heinis; I. Reis Correa Jr.; M. Kindermann et al. : An engineered protein tag for multi-protein labeling in living cells; Chemistry & Biology. 2008. DOI : 10.1016/j.chembiol.2008.01.007.


C. Heinis; A. R. Ball; W. W. Ja; O. Wiser; C. A. Ocasio : Introducing our Authors; ACS Chemical Biology. 2006. DOI : 10.1021/cb6004239.
C. Heinis; S. Schmitt; M. Kindermann; G. Godin; K. Johnsson : Evolving the substrate specificity of O6-alkylguanine-DNA alkyltransferase through loop insertion for applications in molecular imaging; ACS Chemical Biology. 2006. DOI : 10.1021/cb6003146.
T. Gronemeyer; C. Chidley; A. Juillerat; C. Heinis; K. Johnsson : Directed evolution of O6-alkylguanine-DNA alkyltransferase for applications in protein labeling; Protein Engineering, Design and Selection. 2006. DOI : 10.1093/protein/gzl014.


J. Bertschinger; C. Heinis ; Use of microcompartmentation of transcription/translation complexes in emulsions in the selection of proteins with novel properties. US7527954 ; ES2300808 ; AT386113 ; EP1668126 ; US2007105117 ; EP1668126 ; WO2005030957 . 2005.
J. Bertschinger; C. Heinis; D. Neri : Selections for enzymatic catalysts; Phage Display in Biotechnology and Drug Discovery; Boca Raton: CRC Press, 2005. p. 461-491.
A. Juillerat; C. Heinis; I. Sielaff; J. Barnikow; H. Jaccard et al. : Engineering substrate specificity of O6-alkylguanine-DNA alkyltransferase for specific protein labeling in living cells; ChemBioChem. 2005. DOI : 10.1002/cbic.200400431.
C. Heinis; K. Johnsson : Fast directed evolution of non-immunoglobulin proteins by somatic hypermutation in immune cells; ChemBioChem. 2005. DOI : 10.1002/cbic.200500011.
J. Barnikov; C. Chidley; T. Gronemeyer; C. Heinis; H. Jaccard et al. ; Mutants of human O6-alkylguanine-DNA alkyltransferase with improved properties. 2005-EP50899 2005085431 . 2005.


C. Heinis; P. Alessi; D. Neri : Engineering a thermostable human prolyl endopeptidase for antibody-directed enzyme prodrug therapy; Biochemistry. 2004. DOI : 10.1021/bi0361160.


C. Heinis; J. Bertschinger; D. Neri : Calmodulin-tagged phage and two-filter sandwich assays for the identification of enzymatic activities; Directed Enzyme Evolution; Totowa: Humana Press, 2003. p. 313-328.


C. Heinis; S. Melkko; S. Demartis; D. Neri : Two General Methods for the Isolation of Enzyme Activities by Colony Filter Screening; Chemistry & Biology. 2002. DOI : 10.1016/S1074-5521(02)00113-8.


U. Hermanns; E. Hahn; P. Sebbel; C. Heinis; P. Wild et al. : Assembly of type 1 pili in Escherichia coli; Structure, Self-Organization and Stability of Proteins: Experiments and Models; Halle: Deutsche Akademie der Naturforscher Leopoldina, 2001. p. 97-98.
C. Heinis; A. Huber; S. Demartis; J. Bertschinger; S. Melkko et al. : Selection of catalytically active biotin ligase and trypsin mutants by phage display; Protein Engineering. 2001. DOI : 10.1093/protein/14.12.1043.