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Fulfilling Paul Ehrlich’s Dream: therapeutics with activity on demand


Protease-Cleavable Linkers Modulate the Anticancer Activity of Noninternalizing Antibody–Drug Conjugates

Autores: Alberto Dal Corso, Samuele Cazzamalli, Rémy Gébleux, Martin Mattarella, Dario Neri
Publicado en: Bioconjugate Chemistry, Issue 28/7, 2017, Page(s) 1826-1833, ISSN 1043-1802
DOI: 10.1021/acs.bioconjchem.7b00304

A Specific and Covalent JNK-1 Ligand Selected from an Encoded Self-Assembling Chemical Library

Autores: Gunther Zimmermann, Ulrike Rieder, Davor Bajic, Sara Vanetti, Apirat Chaikuad, Stefan Knapp, Jörg Scheuermann, Martin Mattarella, Dario Neri
Publicado en: Chemistry - A European Journal, Issue 23/34, 2017, Page(s) 8152-8155, ISSN 0947-6539
DOI: 10.1002/chem.201701644

DNA-Encoded Chemical Libraries: A Selection System Based On Endowing Organic Compounds with Amplifiable Information

Autores: Dario Neri, Richard A. Lerner
Publicado en: Annual Review of Biochemistry, Issue 87/1, 2018, ISSN 0066-4154
DOI: 10.1146/annurev-biochem-062917-012550

Sarcoma Eradication by Doxorubicin and Targeted TNF Relies upon CD8 + T-cell Recognition of a Retroviral Antigen

Autores: Philipp Probst, Janine Kopp, Annette Oxenius, Mario P. Colombo, Danilo Ritz, Tim Fugmann, Dario Neri
Publicado en: Cancer Research, Issue 77/13, 2017, Page(s) 3644-3654, ISSN 0008-5472
DOI: 10.1158/0008-5472.CAN-16-2946

A non-internalizing antibody-drug conjugate based on an anthracycline payload displays potent therapeutic activity in vivo

Autores: Alberto Dal Corso, Rémy Gébleux, Patrizia Murer, Alex Soltermann, Dario Neri
Publicado en: Journal of Controlled Release, Issue 264, 2017, Page(s) 211-218, ISSN 0168-3659
DOI: 10.1016/j.jconrel.2017.08.040

Intratumoral administration of IL2- and TNF-based fusion proteins cures cancer without establishing protective immunity

Autores: Barbara Ziffels, Francesca Pretto, Dario Neri
Publicado en: Immunotherapy, Issue 10/3, 2018, Page(s) 177-188, ISSN 1750-743X
DOI: 10.2217/imt-2017-0119

Potency-matched Dual Cytokine–Antibody Fusion Proteins for Cancer Therapy

Autores: Roberto De Luca, Alex Soltermann, Francesca Pretto, Catherine Pemberton-Ross, Giovanni Pellegrini, Sarah Wulhfard, Dario Neri
Publicado en: Molecular Cancer Therapeutics, Issue 16/11, 2017, Page(s) 2442-2451, ISSN 1535-7163
DOI: 10.1158/1535-7163.MCT-17-0211

Antibody-based targeted delivery of interleukin-4 synergizes with dexamethasone for the reduction of inflammation in arthritis

Autores: Anja Sophie Schmid, Teresa Hemmerle, Francesca Pretto, Anja Kipar, Dario Neri
Publicado en: Rheumatology, 2018, ISSN 1462-0324
DOI: 10.1093/rheumatology/kex447

Data-Independent Acquisition of HLA Class I Peptidomes on the Q Exactive Mass Spectrometer Platform

Autores: Danilo Ritz, Jonny Kinzi, Dario Neri, Tim Fugmann
Publicado en: PROTEOMICS, Issue 17/19, 2017, Page(s) 1700177, ISSN 1615-9853
DOI: 10.1002/pmic.201700177

Chemically Defined Antibody– and Small Molecule–Drug Conjugates for in Vivo Tumor Targeting Applications: A Comparative Analysis

Autores: Samuele Cazzamalli, Alberto Dal Corso, Fontaine Widmayer, Dario Neri
Publicado en: Journal of the American Chemical Society, Issue 140/5, 2018, Page(s) 1617-1621, ISSN 0002-7863
DOI: 10.1021/jacs.7b13361

Novel antibody-cytokine fusion proteins featuring granulocyte-colony stimulating factor, interleukin-3 and interleukin-4 as payloads

Autores: Anja Sophie Schmid, Diana Tintor, Dario Neri
Publicado en: Journal of Biotechnology, Issue 271, 2018, Page(s) 29-36, ISSN 0168-1656
DOI: 10.1016/j.jbiotec.2018.02.004

Membranal and blood-soluble HLA class II peptidome analyses using data-dependent and independent acquisition

Autores: Danilo Ritz, Emiliano Sani, Hanna Debiec, Pierre Ronco, Dario Neri, Tim Fugmann
Publicado en: PROTEOMICS, 2018, ISSN 1615-9853
DOI: 10.1002/pmic.201700246

Targeted Delivery of Cytotoxic Drugs: Challenges, Opportunities and New Developments

Autores: Samuele Cazzamalli, Alberto Dal Corso, Dario Neri
Publicado en: CHIMIA International Journal for Chemistry, Issue 71/10, 2017, Page(s) 712-715, ISSN 0009-4293
DOI: 10.2533/chimia.2017.712

Versatile protein recognition by the encoded display of multiple chemical elements on a constant macrocyclic scaffold

Autores: Yizhou Li, Roberto De Luca, Samuele Cazzamalli, Francesca Pretto, Davor Bajic, Jörg Scheuermann, Dario Neri
Publicado en: Nature Chemistry, Issue 10/4, 2018, Page(s) 441-448, ISSN 1755-4330
DOI: 10.1038/s41557-018-0017-8

DNA-encoded chemical libraries - achievements and remaining challenges

Autores: Nicholas Favalli, Gabriele Bassi, Jörg Scheuermann, Dario Neri
Publicado en: FEBS Letters, Issue 592/12, 2018, Page(s) 2168-2180, ISSN 0014-5793
DOI: 10.1002/1873-3468.13068

A DNA-Encoded Library of Chemical Compounds Based on Common Scaffolding Structures Reveals the Impact of Ligand Geometry on Protein Recognition

Autores: Nicholas Favalli, Stefan Biendl, Marco Hartmann, Jacopo Piazzi, Filippo Sladojevich, Susanne Gräslund, Peter J. Brown, Katja Näreoja, Herwig Schüler, Jörg Scheuermann, Raphael Franzini, Dario Neri
Publicado en: ChemMedChem, Issue 13/13, 2018, Page(s) 1303-1307, ISSN 1860-7179
DOI: 10.1002/cmdc.201800193

Enhanced Therapeutic Activity of Non-Internalizing Small-Molecule-Drug Conjugates Targeting Carbonic Anhydrase IX in Combination with Targeted Interleukin-2

Autores: Samuele Cazzamalli, Barbara Ziffels, Fontaine Widmayer, Patrizia Murer, Giovanni Pellegrini, Francesca Pretto, Sarah Wulhfard, Dario Neri
Publicado en: Clinical Cancer Research, Issue 24/15, 2018, Page(s) 3656-3667, ISSN 1078-0432
DOI: 10.1158/1078-0432.CCR-17-3457

DNA-encoded chemical libraries: foundations and applications in lead discovery

Autores: Gunther Zimmermann, Dario Neri
Publicado en: Drug Discovery Today, Issue 21/11, 2016, Page(s) 1828-1834, ISSN 1359-6446
DOI: 10.1016/j.drudis.2016.07.013

Purification of soluble HLA class I complexes from human serum or plasma deliver high quality immuno peptidomes required for biomarker discovery

Autores: Danilo Ritz, Andreas Gloger, Dario Neri, Tim Fugmann
Publicado en: PROTEOMICS, Issue 17/1-2, 2017, Page(s) 1600364, ISSN 1615-9853
DOI: 10.1002/pmic.201600364

Different tissue distribution properties for glycosylation variants of fusion proteins containing the p40 subunit of murine interleukin-12

Autores: F. Bootz, D. Venetz, B. Ziffels, D. Neri
Publicado en: Protein Engineering Design and Selection, Issue 29/10, 2016, Page(s) 445-455, ISSN 1741-0126
DOI: 10.1093/protein/gzw038

Acetazolamide Serves as Selective Delivery Vehicle for Dipeptide-Linked Drugs to Renal Cell Carcinoma

Autores: Samuele Cazzamalli, Alberto Dal Corso, Dario Neri
Publicado en: Molecular Cancer Therapeutics, Issue 15/12, 2016, Page(s) 2926-2935, ISSN 1535-7163
DOI: 10.1158/1535-7163.MCT-16-0283

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

Autores: Andreas Gloger, Danilo Ritz, Tim Fugmann, Dario Neri
Publicado en: Cancer Immunology, Immunotherapy, Issue 65/11, 2016, Page(s) 1377-1393, ISSN 0340-7004
DOI: 10.1007/s00262-016-1897-3

Targeted Reconstitution of Cytokine Activity upon Antigen Binding using Split Cytokine Antibody Fusion Proteins

Autores: Dario Venetz, Danil Koovely, Bruce Weder, Dario Neri
Publicado en: Journal of Biological Chemistry, Issue 291/35, 2016, Page(s) 18139-18147, ISSN 0021-9258
DOI: 10.1074/jbc.M116.737734

Optimized Reaction Conditions for Amide Bond Formation in DNA-Encoded Combinatorial Libraries

Autores: Yizhou Li, Elena Gabriele, Florent Samain, Nicholas Favalli, Filippo Sladojevich, Jörg Scheuermann, Dario Neri
Publicado en: ACS Combinatorial Science, Issue 18/8, 2016, Page(s) 438-443, ISSN 2156-8952
DOI: 10.1021/acscombsci.6b00058

Linker stability influences the anti-tumor activity of acetazolamide-drug conjugates for the therapy of renal cell carcinoma

Autores: Samuele Cazzamalli, Alberto Dal Corso, Dario Neri
Publicado en: Journal of Controlled Release, Issue 246, 2017, Page(s) 39-45, ISSN 0168-3659
DOI: 10.1016/j.jconrel.2016.11.023

Non-internalizing antibody-drug conjugates display potent anti-cancer activity upon proteolytic release of monomethyl auristatin E in the subendothelial extracellular matrix

Autores: Rémy Gébleux, Marco Stringhini, Ruben Casanova, Alex Soltermann, Dario Neri
Publicado en: International Journal of Cancer, Issue 140/7, 2017, Page(s) 1670-1679, ISSN 0020-7136
DOI: 10.1002/ijc.30569

The MHC Class II Immunopeptidome of Lymph Nodes in Health and in Chemically Induced Colitis

Autores: Tim Fugmann, Adriana Sofron, Danilo Ritz, Franziska Bootz, Dario Neri
Publicado en: The Journal of Immunology, Issue 198/3, 2017, Page(s) 1357-1364, ISSN 0022-1767
DOI: 10.4049/jimmunol.1601157

Intralesional treatment of metastatic melanoma: a review of therapeutic options

Autores: Benjamin Weide, Dario Neri, Giuliano Elia
Publicado en: Cancer Immunology, Immunotherapy, 2017, ISSN 0340-7004
DOI: 10.1007/s00262-016-1952-0

Hit-Validation Methodologies for Ligands Isolated from DNA-Encoded Chemical Libraries

Autores: Gunther Zimmermann, Yizhou Li, Ulrike Rieder, Martin Mattarella, Dario Neri, Jörg Scheuermann
Publicado en: ChemBioChem, 2017, ISSN 1439-4227
DOI: 10.1002/cbic.201600637

Quantitative PCR is a Valuable Tool to Monitor the Performance of DNA-Encoded Chemical Library Selections

Autores: Yizhou Li, Gunther Zimmermann, Jörg Scheuermann, Dario Neri
Publicado en: ChemBioChem, 2017, ISSN 1439-4227
DOI: 10.1002/cbic.201600626

Screening of Three Transition Metal‐Mediated Reactions Compatible with DNA‐Encoded Chemical Libraries

Autores: Nicholas Favalli, Gabriele Bassi, Tania Zanetti, Jörg Scheuermann, Dario Neri
Publicado en: Helvetica Chimica Acta, Issue 102/4, 2019, Page(s) e1900033, ISSN 0018-019X
DOI: 10.1002/hlca.201900033

A novel dual-cytokine–antibody fusion protein for the treatment of CD38-positive malignancies

Autores: Roberto De Luca, Paul Kachel, Klara Kropivsek, Berend Snijder, Markus G Manz, Dario Neri
Publicado en: Protein Engineering, Design and Selection, Issue 31/5, 2018, Page(s) 173-179, ISSN 1741-0126
DOI: 10.1093/protein/gzy015

Antibody-based Delivery of TNF to the Tumor Neovasculature Potentiates the Therapeutic Activity of a Peptide Anticancer Vaccine

Autores: Philipp Probst, Marco Stringhini, Danilo Ritz, Tim Fugmann, Dario Neri
Publicado en: Clinical Cancer Research, Issue 25/2, 2019, Page(s) 698-709, ISSN 1078-0432
DOI: 10.1158/1078-0432.CCR-18-1728

Antibody-mediated delivery of VEGF-C potently reduces chronic skin inflammation

Autores: Simon Schwager, Silvana Renner, Teresa Hemmerle, Sinem Karaman, Steven T. Proulx, Roman Fetz, Alexandra Michaela Golding-Ochsenbein, Philipp Probst, Cornelia Halin, Dario Neri, Michael Detmar
Publicado en: JCI Insight, Issue 3/23, 2018, ISSN 2379-3708
DOI: 10.1172/jci.insight.124850

Quantitative Assessment of Affinity Selection Performance by Using DNA‐Encoded Chemical Libraries

Autores: Alessandro Sannino, Elena Gabriele, Martina Bigatti, Sara Mulatto, Jacopo Piazzi, Jörg Scheuermann, Dario Neri, Etienne J. Donckele, Florent Samain
Publicado en: ChemBioChem, Issue 20/7, 2019, Page(s) 955-962, ISSN 1439-4227
DOI: 10.1002/cbic.201800766

A Novel Fully-Human Potency-Matched Dual Cytokine-Antibody Fusion Protein Targets Carbonic Anhydrase IX in Renal Cell Carcinomas

Autores: Roberto De Luca, Baptiste Gouyou, Tiziano Ongaro, Alessandra Villa, Barbara Ziffels, Alessandro Sannino, Gianluca Buttinoni, Simone Galeazzi, Mirko Mazzacuva, Dario Neri
Publicado en: Frontiers in Oncology, Issue 9, 2019, ISSN 2234-943X
DOI: 10.3389/fonc.2019.01228

Development of a novel fully-human anti-CD123 antibody to target acute myeloid leukemia

Autores: Cornelia Hutmacher, Laura Volta, Francesco Rinaldi, Patrizia Murer, Renier Myburgh, Markus G. Manz, Dario Neri
Publicado en: Leukemia Research, Issue 84, 2019, Page(s) 106178, ISSN 0145-2126
DOI: 10.1016/j.leukres.2019.106178

Targeted Delivery of TNF Potentiates the Antibody-Dependent Cell-Mediated Cytotoxicity of an Anti-Melanoma Immunoglobulin

Autores: Patrizia Murer, Jonathan D. Kiefer, Louis Plüss, Mattia Matasci, Sandra L. Blümich, Marco Stringhini, Dario Neri
Publicado en: Journal of Investigative Dermatology, Issue 139/6, 2019, Page(s) 1339-1348, ISSN 0022-202X
DOI: 10.1016/j.jid.2018.11.028

Antibody-cytokine fusion proteins: Biopharmaceuticals with immunomodulatory properties for cancer therapy

Autores: Cornelia Hutmacher, Dario Neri
Publicado en: Advanced Drug Delivery Reviews, Issue 141, 2019, Page(s) 67-91, ISSN 0169-409X
DOI: 10.1016/j.addr.2018.09.002

Antibody-cytokine fusion proteins: A novel class of biopharmaceuticals for the therapy of cancer and of chronic inflammation

Autores: Patrizia Murer, Dario Neri
Publicado en: New Biotechnology, Issue 52, 2019, Page(s) 42-53, ISSN 1871-6784
DOI: 10.1016/j.nbt.2019.04.002

Antibody-Based Delivery of Cytokine Payloads to Carbonic Anhydrase IX Leads to Cancer Cures in Immunocompetent Tumor-Bearing Mice

Autores: Barbara Ziffels, Marco Stringhini, Philipp Probst, Tim Fugmann, Theo Sturm, Dario Neri
Publicado en: Molecular Cancer Therapeutics, Issue 18/9, 2019, Page(s) 1544-1554, ISSN 1535-7163
DOI: 10.1158/1535-7163.mct-18-1301

In Vivo Antitumor Activity of a Novel Acetazolamide–Cryptophycin Conjugate for the Treatment of Renal Cell Carcinomas

Autores: Cazzamalli, Samuele; Figueras, Eduard; Pethő, Lilla; Borbély, Adina; Steinkühler, Christian; Neri, Dario; Sewald, Norbert
Publicado en: ACS Omega, 3 (11), Issue 1, 2018, Page(s) 14726-14731, ISSN 2470-1343
DOI: 10.3929/ethz-b-000304161

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

Autores: Roberto De Luca, Dario Neri
Publicado en: Cancer Immunology, Immunotherapy, Issue 67/9, 2018, Page(s) 1381-1391, ISSN 0340-7004
DOI: 10.1007/s00262-018-2194-0

Design and characterisation of a novel interleukin-15 receptor alpha fusion protein and analysis of interleukin-15 complexation

Autores: Anja Sophie Schmid, Dario Neri
Publicado en: PLOS ONE, Issue 14/7, 2019, Page(s) e0219313, ISSN 1932-6203
DOI: 10.1371/journal.pone.0219313

DNA-Compatible Diazo-Transfer Reaction in Aqueous Media Suitable for DNA-Encoded Chemical Library Synthesis

Autores: Adrián Gironda-Martínez, Dario Neri, Florent Samain, Etienne J. Donckele
Publicado en: Organic Letters, Issue 21/23, 2019, Page(s) 9555-9558, ISSN 1523-7060
DOI: 10.1021/acs.orglett.9b03726

Comparative evaluation of bolus and fractionated administration modalities for two antibody-cytokine fusions in immunocompetent tumor-bearing mice

Autores: Emanuele Puca, Roberto De Luca, Frauke Seehusen, Josep Maria Monné Rodriguez, Dario Neri
Publicado en: Journal of Controlled Release, 2019, ISSN 0168-3659
DOI: 10.1016/j.jconrel.2019.11.036

The antibody‐based delivery of interleukin‐12 to solid tumors boosts NK and CD8 + T cell activity and synergizes with immune checkpoint inhibitors

Autores: Emanuele Puca, Philipp Probst, Marco Stringhini, Patrizia Murer, Giovanni Pellegrini, Samuele Cazzamalli, Cornelia Hutmacher, Baptiste Gouyou, Sarah Wulhfard, Mattia Matasci, Alessandra Villa, Dario Neri
Publicado en: International Journal of Cancer, 2019, ISSN 0020-7136
DOI: 10.1002/ijc.32603

Targeted enhancement of the therapeutic window of L19-TNF by transient and selective inhibition of RIPK1-signaling cascade

Autores: Sheila Dakhel, Tiziano Ongaro, Baptiste Gouyou, Mattia Matasci, Alessandra Villa, Dario Neri, Samuele Cazzamalli
Publicado en: Oncotarget, Issue 10/62, 2019, ISSN 1949-2553
DOI: 10.18632/oncotarget.27320

Targeted Delivery of IL2 to the Tumor Stroma Potentiates the Action of Immune Checkpoint Inhibitors by Preferential Activation of NK and CD8 + T Cells

Autores: Cornelia Hutmacher, Nicolás Gonzalo Núñez, Anna Rita Liuzzi, Burkhard Becher, Dario Neri
Publicado en: Cancer Immunology Research, Issue 7/4, 2019, Page(s) 572-583, ISSN 2326-6066
DOI: 10.1158/2326-6066.cir-18-0566

Antibody–Cytokine Fusions: Versatile Products for the Modulation of Anticancer Immunity

Autores: Dario Neri
Publicado en: Cancer Immunology Research, Issue 7/3, 2019, Page(s) 348-354, ISSN 2326-6066
DOI: 10.1158/2326-6066.cir-18-0622

A fully human anti-IL-7Rα antibody promotes antitumor activity against T-cell acute lymphoblastic leukemia

Autores: Padma Akkapeddi, Rita Fragoso, Julie A. Hixon, Ana Sofia Ramalho, Mariana L. Oliveira, Tânia Carvalho, Andreas Gloger, Mattia Matasci, Francisco Corzana, Scott K. Durum, Dario Neri, Gonçalo J. L. Bernardes, João T. Barata
Publicado en: Leukemia, Issue 33/9, 2019, Page(s) 2155-2168, ISSN 0887-6924
DOI: 10.1038/s41375-019-0434-8

Immunocytokines and bispecific antibodies: two complementary strategies for the selective activation of immune cells at the tumor site

Autores: Jonathan D. Kiefer, Dario Neri
Publicado en: Immunological Reviews, Issue 270/1, 2016, Page(s) 178-192, ISSN 0105-2896
DOI: 10.1111/imr.12391

Antibody Format and Drug Release Rate Determine the Therapeutic Activity of Noninternalizing Antibody-Drug Conjugates

Autores: R. Gebleux, S. Wulhfard, G. Casi, D. Neri
Publicado en: Molecular Cancer Therapeutics, Issue 14/11, 2015, Page(s) 2606-2612, ISSN 1535-7163
DOI: 10.1158/1535-7163.MCT-15-0480

Immunocytokines: a novel class of products for the treatment of chronic inflammation and autoimmune conditions

Autores: Franziska Bootz, Dario Neri
Publicado en: Drug Discovery Today, Issue 21/1, 2016, Page(s) 180-189, ISSN 1359-6446
DOI: 10.1016/j.drudis.2015.10.012

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

Autores: Danilo Ritz, Andreas Gloger, Benjamin Weide, Claus Garbe, Dario Neri, Tim Fugmann
Publicado en: PROTEOMICS, 2016, Page(s) n/a-n/a, ISSN 1615-9853
DOI: 10.1002/pmic.201500445

Immunocytokines for cancer treatment: past, present and future

Autores: Dario Neri, Paul M Sondel
Publicado en: Current Opinion in Immunology, Issue 40, 2016, Page(s) 96-102, ISSN 0952-7915
DOI: 10.1016/j.coi.2016.03.006

A universal reporter cell line for bioactivity evaluation of engineered cytokine products

Autores: Jacqueline Mock, Christian Pellegrino, Dario Neri
Publicado en: Scientific Reports, Issue 10/1, 2020, ISSN 2045-2322
DOI: 10.1038/s41598-020-60182-4

A novel human monoclonal antibody specific to the A33 glycoprotein recognizes colorectal cancer and inhibits metastasis

Autores: Patrizia Murer, Louis Plüss, Dario Neri
Publicado en: mAbs, Issue 12/1, 2020, Page(s) 1714371, ISSN 1942-0870
DOI: 10.1080/19420862.2020.1714371