Cazzamalli Samuele, Figueras Eduard, Pethő Lilla, Borbély Adina, Steinkühler Christian, Neri Dario, Sewald Norbert (2018), In Vivo Antitumor Activity of a Novel Acetazolamide–Cryptophycin Conjugate for the Treatment of Renal Cell Carcinomas, in ACS Omega
, 3(11), 14726-14731.
De Luca Roberto, Neri Dario (2018), Potentiation of PD-L1 blockade with a potency-matched dual cytokine–antibody fusion protein leads to cancer eradication in BALB/c-derived tumors but not in other mouse strains, in Cancer Immunology, Immunotherapy
, 67(9), 1381-1391.
Cazzamalli Samuele, Ziffels Barbara, Widmayer Fontaine, Murer Patrizia, Pellegrini Giovanni, Pretto Francesca, Wulhfard Sarah, Neri Dario (2018), Enhanced Therapeutic Activity of Non-Internalizing Small-Molecule-Drug Conjugates Targeting Carbonic Anhydrase IX in Combination with Targeted Interleukin-2, in Clinical Cancer Research
, 24(15), 3656-3667.
Favalli Nicholas, Biendl Stefan, Hartmann Marco, Piazzi Jacopo, Sladojevich Filippo, Gräslund Susanne, Brown Peter J., Näreoja Katja, Schüler Herwig, Scheuermann Jörg, Franzini Raphael, Neri Dario (2018), A DNA-Encoded Library of Chemical Compounds Based on Common Scaffolding Structures Reveals the Impact of Ligand Geometry on Protein Recognition, in ChemMedChem
, 13(13), 1303-1307.
Neri Dario, Lerner Richard A. (2018), DNA-Encoded Chemical Libraries: A Selection System Based on Endowing Organic Compounds with Amplifiable Information, in Annual Review of Biochemistry
, 87(1), 479-502.
Favalli Nicholas, Bassi Gabriele, Scheuermann Jörg, Neri Dario (2018), DNA-encoded chemical libraries - achievements and remaining challenges, in FEBS Letters
, 592(12), 2168-2180.
De Luca Roberto, Kachel Paul, Kropivsek Klara, Snijder Berend, Manz Markus G, Neri Dario (2018), A novel dual-cytokine–antibody fusion protein for the treatment of CD38-positive malignancies, in Protein Engineering, Design and Selection
, 31(5), 173-179.
Li Yizhou, De Luca Roberto, Cazzamalli Samuele, Pretto Francesca, Bajic Davor, Scheuermann Jörg, Neri Dario (2018), Versatile protein recognition by the encoded display of multiple chemical elements on a constant macrocyclic scaffold, in Nature Chemistry
, 10(4), 441-448.
Schmid Anja Sophie, Hemmerle Teresa, Pretto Francesca, Kipar Anja, Neri Dario (2018), Antibody-based targeted delivery of interleukin-4 synergizes with dexamethasone for the reduction of inflammation in arthritis, in Rheumatology
, 57(4), 748-755.
Schmid Anja Sophie, Tintor Diana, Neri Dario (2018), Novel antibody-cytokine fusion proteins featuring granulocyte-colony stimulating factor, interleukin-3 and interleukin-4 as payloads, in Journal of Biotechnology
, 271, 29-36.
Ritz Danilo, Sani Emiliano, Debiec Hanna, Ronco Pierre, Neri Dario, Fugmann Tim (2018), Membranal and Blood-Soluble HLA Class II Peptidome Analyses Using Data-Dependent and Independent Acquisition, in PROTEOMICS
Ziffels Barbara, Pretto Francesca, Neri Dario (2018), Intratumoral administration of IL2- and TNF-based fusion proteins cures cancer without establishing protective immunity, in Immunotherapy
, (3), 177-188.
Cazzamalli Samuele, Dal Corso Alberto, Widmayer Fontaine, Neri Dario (2018), Chemically Defined Antibody– and Small Molecule–Drug Conjugates for in Vivo Tumor Targeting Applications: A Comparative Analysis, in Journal of the American Chemical Society
, (5), 1617-1621.
De Luca Roberto, Soltermann Alex, Pretto Francesca, Pemberton-Ross Catherine, Pellegrini Giovanni, Wulhfard Sarah, Neri Dario (2017), Potency-matched Dual Cytokine–Antibody Fusion Proteins for Cancer Therapy, in Molecular Cancer Therapeutics
, (11), 2442-2451.
Cazzamalli Samuele, Corso Alberto Dal, Neri Dario (2017), Targeted Delivery of Cytotoxic Drugs: Challenges, Opportunities and New Developments, in CHIMIA International Journal for Chemistry
, (10), 712-715.
Ritz Danilo, Kinzi Jonny, Neri Dario, Fugmann Tim (2017), Data-Independent Acquisition of HLA Class I Peptidomes on the Q Exactive Mass Spectrometer Platform, in PROTEOMICS
, (19), 1700177-1700177.
Dal Corso Alberto, Gébleux Rémy, Murer Patrizia, Soltermann Alex, Neri Dario (2017), A non-internalizing antibody-drug conjugate based on an anthracycline payload displays potent therapeutic activity in vivo, in Journal of Controlled Release
Dal Corso Alberto, Cazzamalli Samuele, Gebleux Remy, Mattarella Martin, Neri Dario (2017), Protease-Cleavable Linkers Modulate the Anticancer Activity of Noninternalizing Antibody-Drug Conjugates, in BIOCONJUGATE CHEMISTRY
, (7), 1826-1833.
Probst Philipp, Kopp Janine, Oxenius Annette, Colombo Mario P., Ritz Danilo, Fugmann Tim, Neri Dario (2017), Sarcoma Eradication by Doxorubicin and Targeted TNF Relies upon CD8(+) T-cell Recognition of a Retroviral Antigen, in CANCER RESEARCH
, (13), 3644-3654.
Zimmermann Gunther, Rieder Ulrike, Bajic Davor, Vanetti Sara, Chaikuad Apirat, Knapp Stefan, Scheuermann Jorg, Mattarella Martin, Neri Dario (2017), A Specific and Covalent JNK-1 Ligand Selected from an Encoded Self-Assembling Chemical Library, in CHEMISTRY-A EUROPEAN JOURNAL
, (34), 8152-8155.
Weide Benjamin, Neri Dario, Elia Giuliano (2017), Intralesional treatment of metastatic melanoma: a review of therapeutic options, in CANCER IMMUNOLOGY IMMUNOTHERAPY
, (5), 647-656.
Zimmermann Gunther, Li Yizhou, Rieder Ulrike, Mattarella Martin, Neri Dario, Scheuermann Jorg (2017), Hit-Validation Methodologies for Ligands Isolated from DNA-Encoded Chemical Libraries, in CHEMBIOCHEM
, (9), 853-857.
Li Yizhou, Zimmermann Gunther, Scheuermann Joerg, Neri Dario (2017), Quantitative PCR is a Valuable Tool to Monitor the Performance of DNA-Encoded Chemical Library Selections, in CHEMBIOCHEM
, (9), 848-852.
Fugmann Tim, Sofron Adriana, Ritz Danilo, Bootz Franziska, Neri Dario (2017), The MHC Class II Immunopeptidome of Lymph Nodes in Health and in Chemically Induced Colitis, in The Journal of Immunology
, (3), 1357-1364.
Cazzamalli Samuele, Corso Alberto Dal, Neri Dario (2017), Linker stability influences the anti-tumor activity of acetazolamide-drug conjugates for the therapy of renal cell carcinoma, in Journal of Controlled Release
Krall N., Pretto F., Mattarella M., Muller C., Neri D. (2016), A 99mTc-Labeled Ligand of Carbonic Anhydrase IX Selectively Targets Renal Cell Carcinoma In Vivo, in Journal of Nuclear Medicine
, (6), 943-949.
Cazzamalli S., Dal Corso A., Neri D. (2016), Acetazolamide Serves as Selective Delivery Vehicle for Dipeptide-Linked Drugs to Renal Cell Carcinoma, in Molecular Cancer Therapeutics
, (12), 2926-2935.
Bootz Franziska, Ziffels Barbara, Neri Dario (2016), Antibody-Based Targeted Delivery of Interleukin-22 Promotes Rapid Clinical Recovery in Mice With DSS-Induced Colitis, in Inflammatory Bowel Diseases
, (9), 2098-2105.
Decurtins W., Wichert M., Franzini R.M., Buller F., Stravs M.A., Zhang Y., Neri D., Scheuermann J. (2016), Automated screening for small organic ligands using DNA-encoded chemical libraries., in Nature Protocols
, (11), 764-780.
Bootz F., Venetz D., Ziffels B., Neri D. (2016), Different tissue distribution properties for glycosylation variants of fusion proteins containing the p40 subunit of murine interleukin-12, in Protein Engineering Design and Selection
, (10), 445-455.
Zimmermann Gunther, Neri Dario (2016), DNA-encoded chemical libraries: foundations and applications in lead discovery, in Drug Discovery Today
, (11), 1828-1834.
Ritz Danilo, Gloger Andreas, Weide Benjamin, Garbe Claus, Neri Dario, Fugmann Tim (2016), High-sensitivity HLA class I peptidome analysis enables a precise definition of peptide motifs and the identification of peptides from cell lines and patients’ sera, in PROTEOMICS
, 16(10), 1570-1580.
Kiefer Jonathan, Neri Dario (2016), Immunocytokines and bispecific antibodies: two complementary strategies for the selective activation of immune cells at the tumor site, in Immunological Reviews
Neri Dario, Sondel Paul M (2016), Immunocytokines for cancer treatment: past, present and future, in Current Opinion in Immunology
Bootz Franziska, Neri Dario (2016), Immunocytokines: a novel class of products for the treatment of chronic inflammation and autoimmune conditions, in Drug Discovery Today
, (1), 180-189.
Gloger Andreas, Ritz Danilo, Fugmann Tim, Neri Dario (2016), Mass spectrometric analysis of the HLA class I peptidome of melanoma cell lines as a promising tool for the identification of putative tumor-associated HLA epitopes, in Cancer Immunology, Immunotherapy
, (11), 1377-1393.
Li Yizhou, Gabriele Elena, Samain Florent, Favalli Nicholas, Sladojevich Filippo, Scheuermann Jörg, Neri Dario (2016), Optimized Reaction Conditions for Amide Bond Formation in DNA-Encoded Combinatorial Libraries, in ACS Combinatorial Science
, (8), 438-443.
Venetz Dario, Koovely Danil, Weder Bruce, Neri Dario (2016), Targeted Reconstitution of Cytokine Activity upon Antigen Binding using Split Cytokine Antibody Fusion Proteins, in Journal of Biological Chemistry
, (35), 18139-18147.
Gebleux R., Wulhfard S., Casi G., Neri D. (2015), Antibody Format and Drug Release Rate Determine the Therapeutic Activity of Noninternalizing Antibody-Drug Conjugates, in Molecular Cancer Therapeutics
, (11), 2606-2612.
One avenue towards the development of more potent and selective anti-cancer therapeutics consists in the use of antibody derivatives (“armed antibodies”) for the targeted delivery of bioactive molecules to the tumor environment, helping spare normal tissues. In this context, the selective delivery of therapeutic agents to markers of pathology expressed around newly-formed blood vessels (“vascular targeting”) is particularly attractive, not only for cancer applications, but also for other indications (e.g., arthritis, blinding ocular disorders).We have previously generated and validated human monoclonal antibodies, capable of selective localisation to neo-vascular structures in vivo. In the next three years, we wish to extend our work, focusing on novel antibody-cytokine fusion proteins ("immunocytokines") and on novel versions of targeted cytotoxics (e.g., antibody-drug conjugates and small molecule drug-conjugates). In the field of immunocytokines, we see the greatest therapeutic opportunities in the investigation of combination modalities (e.g., combination of two cytokine payloads) and in the design of products with "activity on demand " (e.g., proteolytic activation at the site of disease, or conformational changes upon antigen binding).In the area of targeted cytotoxics, we will investigate the opportunity of releasing anti-cancer drugs at the tumor environment with non-internalising antibodies. In addition, we will study the possibility to by-pass antibodies with small organic ligands as pharmacodelivery vehicles.