Small-Molecule Drug Conjugates for Targeted Delivery in Tumor Therapy

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A fast and sensitive absolute quantification assay for the detection of SARS-CoV-2 peptides using parallel reaction monitoring mass spectrometry

Auteurs: Akshada Gajbhiye, Atakan Nalbant, Tiaan Heunis, Frances Sidgwick, Andrew Porter, Yusri Taha, Matthias Trost
Publié dans: Journal of Proteomics, Numéro Volume 265, 15 August 2022,, 2022, Page(s) 104664, ISSN 1874-3919
Éditeur: Elsevier BV
DOI: 10.1016/j.jprot.2022.104664

Immunotherapy with immunocytokines and PD-1 blockade enhances the anticancer activity of Small Molecule-Drug Conjugates targeting Carbonic Anhydrase IX

Auteurs: Jacopo Millul; Christiane Krudewig; Aureliano Zana; Sheila Dakhel Plaza; Emanuele Puca; Alessandra Villa; Dario Neri; Samuele Cazzamalli
Publié dans: Millul, Jacopo; Krudewig, Christiane; Zana, Aureliano; Plaza, Sheila Dakhel; Puca, Emanuele; Villa, Alessandra; Neri, Dario; Cazzamalli, Samuele (2021). Immunotherapy with immunocytokines and PD-1 blockade enhances the anticancer activity of small molecule-drug conjugates targeting carbonic anhydrase IX. Molecular Cancer Therapeutics, 20(3):512-522., Numéro 20(3), 2020, Page(s) 512–522, ISSN 1535-7163
Éditeur: American Association for Cancer Research
DOI: 10.1158/1535-7163.mct-20-0361

Efficacy of selective histone deacetylase 6 inhibition in mouse models of Pseudomonasaeruginosa infection: A new glimpse for reducing inflammation and infection in cystic fibrosis.

Auteurs: Brindisi M, Barone S, Rossi A, Cassese E, Del Gaudio N, Feliz Morel ÁJ, Filocamo G, Alberico A, De Fino I, Gugliandolo D, Babaei M, Bove G, Croce M, Montesano C, Altucci L, Bragonzi A, Summa V
Publié dans: European Journal of Pharmacology, 2022, ISSN 1879-0712
Éditeur: Elsevier B.V. All
DOI: 10.1016/j.ejphar.2022.175349

Oxime-Linked Peptide–Daunomycin Conjugates as Good Tools for Selection of Suitable Homing Devices in Targeted Tumor Therapy: An Overview

Auteurs: Gábor Mezo, Jacopo Gomena, Ivan Randelovic, Endre Levente Dókus, Krisztina Kiss, Lilla Petho, Sabine Schuster, Balázs Vári, Diána Vári-Mezo, Eszter Lajkó, Lívia Polgár, László Kohidai, József Tóvári and Ildikó Szabó
Publié dans: International Journal of Molecular Sciences, Numéro 25, 2024, Page(s) 186, ISSN 1422-0067
Éditeur: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/ijms25031864

Amine‐Carbamate Self‐Immolative Spacers Counterintuitively Release 3° Alcohol at Much Faster Rates than 1° Alcohol Payloads

Auteurs: Mattia Mason; Lydia Bisbal Lopez; Fazel Bashiri; Aurélie Herrero; Aurélien Baron; Raffaella Bucci; Luca Pignataro; Cesare Gennari; Alberto Dal Corso
Publié dans: ChemBioChem, Numéro 3, 2024, Page(s) e202400174, ISSN 1439-4227
Éditeur: John Wiley & Sons Ltd.
DOI: 10.1002/cbic.202400174

Targeting the Gastrin-Releasing Peptide Receptor (GRP-R) in Cancer Therapy: Development of Bombesin-Based Peptide–Drug Conjugates

Auteurs: Jacopo Gomena, Balázs Vári, Rita Oláh-Szabó, Beáta Biri-Kovács, Szilvia Bősze, Adina Borbély, Ádám Soós, Ivan Ranđelović, József Tóvári and Gábor Mező
Publié dans: Int. J. Mol. Sci., Numéro 24(4), 2023, Page(s) 3400, ISSN 1422-0067
Éditeur: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/ijms24043400

A novel dimeric FAP-targeting small molecule-radio conjugate with high and prolonged tumour uptake

Auteurs: Andrea Galbiati, Aureliano Zana, Matilde Bocci, Jacopo Millul, Abdullah Elsayed, Jacqueline Mock, Dario Neri, Samuele Cazzamalli
Publié dans: Journal of Nuclear Medicine, Numéro Vol. 64, Numéro 8, 2022, Page(s) jnumed.122.264036, ISSN 0097-9058
Éditeur: Society of Nuclear Medicine and Molecular Imaging (SNMMI)
DOI: 10.2967/jnumed.122.264036

Highly pure DNA-encoded chemical libraries by dual-linker solid-phase synthesis

Auteurs: Michelle Keller, Dimitar Petrov, Andreas Gloger, Bastien Dietschi, Kilian Jobin, Timon Gradinger, Adriano Martinelli, Louise Plais, Yuichi Onda, Dario Neri, Jörg Scheuermann
Publié dans: Science, Numéro 384, 2024, Page(s) 1259-1265, ISSN 1095-9203
Éditeur: American Association for the Advancement of Science
DOI: 10.1126/science.adn3412

Optimizing the enzymatic release of MMAE from isoDGR-based small molecule drug conjugate by incorporation of a GPLG-PABC enzymatically cleavable linker

Auteurs: Marco Zambra; Ivan Ranđelović; Francesco Talarico; Adina Borbély; Laura Svajda; Laura Svajda; József Tóvári; Gábor Mező; Gábor Mező; Lizeth Bodero; Sveva Colombo; Sveva Colombo; Federico Arrigoni; Elettra Fasola; Silvia Gazzola; Umberto Piarulli
Publié dans: Frontiers in Pharmacology, Vol 14 (2023), Numéro 14, 2023, Page(s) 1215694, ISSN 1663-9812
Éditeur: Frontiers Media S.A.
DOI: 10.3389/fphar.2023.1215694

Impact of DNA-Encoded Chemical Library Technology on Drug Discovery

Auteurs: Michelle Keller, Kristina Schira, Jörg Scheuermann
Publié dans: Chimia, Numéro 76, 2022, Page(s) 388, ISSN 2673-2424
Éditeur: Swiss Chemical Society
DOI: 10.2533/chimia.2022.388

Targeting the Melanocortin 1 Receptor in Melanoma: Biological Activity of α-MSH–Peptide Conjugates

Auteurs: Ildikó Szabó, Beáta Biri-Kovács, Balázs Vári, Ivan Randelovic, Diána Vári-Mezo, Éva Juhász, Gábor Halmos, Szilvia Bosze, József Tóvári and Gábor Mezo
Publié dans: International Journal of Molecular Sciences, Numéro 25, 2024, Page(s) 1095, ISSN 1422-0067
Éditeur: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/ijms25021095

Ex vivo mass spectrometry-based biodistribution analysis of an antibody-Resiquimod conjugate bearing a protease-cleavable and acid-labile linker

Auteurs: Lydia Bisbal Lopez; Domenico Ravazza; Matilde Bocci; Aureliano Zana; Lucrezia Principi; Sheila Dakhel Plaza; Andrea Galbiati; Ettore Gilardoni; Jörg Scheuermann; Dario Neri; Dario Neri; Dario Neri; Luca Pignataro; Cesare Gennari; Samuele Cazzamalli; Alberto Dal Corso
Publié dans: Frontiers in Pharmacology, Vol 14 (2023), Numéro 4, 2023, Page(s) 1320524, ISSN 1663-9812
Éditeur: Frontiers Media S.A.
DOI: 10.3389/fphar.2023.1320524

Universal encoding of next generation DNA-encoded chemical libraries

Auteurs: Louise Plais; Alice Lessing; Michelle Keller; Adriano Martinelli; Sebastian Oehler; Gabriele Bassi; Dario Neri; Jörg Scheuermann
Publié dans: Chemical Science, 13 (4), Numéro 2, 2022, Page(s) 967-974, ISSN 2633-0679
Éditeur: Royal Society of Chemistry
DOI: 10.3929/ethz-b-000526396

Recent Advances and Trends in Chemical CPP–Drug Conjugation Techniques

Auteurs: Ines Neundorf; Félix Gayraud; Merlin Jan Klußmann
Publié dans: Molecules, Numéro 26(6), 2021, Page(s) 1591, ISSN 1420-3049
Éditeur: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/molecules26061591

An ultra-high-affinity small organic ligand of fibroblast activation protein for tumor-targeting applications

Auteurs: Jacopo Millul; Gabriele Bassi; Jacqueline Mock; Abdullah Elsayed; Christian Pellegrino; Aureliano Zana; Sheila Dakhel Plaza; Lisa Nadal; Andreas Gloger; Eleonore Schmidt; Ilaria Biancofiore; Etienne J. Donckele; Florent Samain; Dario Neri; Samuele Cazzamalli
Publié dans: Proc Natl Acad Sci U S A, Numéro 118 (16), 2021, Page(s) e2101852118, ISSN 0027-8424
Éditeur: National Academy of Sciences
DOI: 10.1073/pnas.2101852118

SREKA-targeted liposomes for highly metastatic breast cancer therapy

Auteurs: Balázs Vári, Levente Dókus, Adina Borbély, Anikó Gaál, Diána Vári-Mező, Ivan Ranđelović, Anna Sólyom-Tisza, Zoltán Varga, Norbert Szoboszlai, Gábor Mező, József Tóvári
Publié dans: Drug Delivery, Numéro Volume 30, 2023 - Numéro 1, 2023, Page(s) 2174210, ISSN 1470-1200
Éditeur: Taylor & Francis
DOI: 10.1080/10717544.2023.2174210

Fibroblast Activation Protein Triggers Release of Drug Payload from Non-internalizing Small Molecule Drug Conjugates in Solid Tumors

Auteurs: Aureliano Zana; Andrea Galbiati; Ettore Gilardoni; Matilde Bocci; Jacopo Millul; Theo Sturm; Riccardo Stucchi; Abdullah Elsayed; Lisa Nadal; Martina Cirillo; Wolfgang Roll; Lars Stegger; Inga Asmus; Philipp Backhaus; Michael Schäfers; Dario Neri; Samuele Cazzamalli
Publié dans: Clinical Cancer Research, 28 (24), Numéro 1, 2022, Page(s) 5440–5454, ISSN 1557-3265
Éditeur: American Association for Cancer Research
DOI: 10.1158/1078-0432.ccr-22-1788

Mass Spectrometry-Based Method for the Determination of the Biodistribution of Tumor-Targeting Small Molecule–Metal Conjugates

Auteurs: Ettore Gilardoni, Aureliano Zana, Andrea Galbiati, Theo Sturm, Jacopo Millul, Samuele Cazzamalli, Dario Neri, and Riccardo Stucchi
Publié dans: Anal. Chem., Numéro 94, 30, 2022, Page(s) 10715–10721, ISSN 1520-6882
Éditeur: American Chemical Society
DOI: 10.1021/acs.analchem.2c01104

Ph.D. Journeys Abroad – And so the Adventure Has Begun …

Auteurs: Sveva Colombo
Publié dans: Chemistry Views, Numéro October 4, 2022, 2022, ISSN 2190-3735
Éditeur: Wiley-VCH GmbH
DOI: 10.1002/chemv.202200083

Ph.D. Journeys Abroad – Be Kind to Yourself

Auteurs: Daniela Carraturo
Publié dans: Chemistry Views, Numéro November 1, 2022, 2022, ISSN 2190-3735
Éditeur: Wiley-VCH GmbH
DOI: 10.1002/chemv.202200094

Ph.D. Journeys Abroad – Creating a Second Home

Auteurs: Tine Haesen
Publié dans: Chemistry Views, Numéro December 6, 2022, 2022, ISSN 2190-3735
Éditeur: Wiley-VCH GmbH
DOI: 10.1002/chemv.202200099

Ph.D. Journeys Abroad – Overcoming Impostor Syndrome: Why Did I Feel Like It Was Just Me?

Auteurs: Lieke van Gijzel
Publié dans: Chemistry Views, Numéro January 3, 2023, 2023, ISSN 2190-3735
Éditeur: Wiley-VCH GmbH
DOI: 10.1002/chemv.202200100

Ph.D. Journeys Abroad – The Challenges of Starting a New Life Far from Home

Auteurs: Ana Ferrari
Publié dans: Chemistry Views, Numéro February 7, 2023, 2023, ISSN 2190-3735
Éditeur: Wiley-VCH GmbH
DOI: 10.1002/chemv.202200101

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