Neutrophil Elastase Promotes Linker Cleavage and Paclitaxel Release from an Integrin-Targeted Conjugate

Synthesis and biological evaluation of RGD and isoDGR peptidomimetic-α-amanitin conjugates for tumor-targeting

(2018) Lizeth Bodero et al.   Beilstein Journal of Organic Chemistry

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

(2018) Samuele Cazzamalli et al.   CLINICAL CANCER RESEARCH

Synthesis and Biological Evaluation of Paclitaxel Conjugates Involving Linkers Cleavable by Lysosomal Enzymes and αV β3 -Integrin Ligands for Tumor Targeting

(2018) Paula López Rivas et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

Succinimide-Based Conjugates Improve IsoDGR Cyclopeptide Affinity to αvβ3 without Promoting Integrin Allosteric Activation

(2018) Francesca Nardelli et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2018) Samuele Cazzamalli et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Neutrophil elastase in the tumor microenvironment

(2018) Irina Lerman et al.   STEROIDS

Advances in targeting the folate receptor in the treatment/imaging of cancers

(2018) Marcos Fernández et al.   Chemical Science

Cancer-targeted delivery systems based on peptides

(2018) Theodora Chatzisideri et al.   Future Medicinal Chemistry

Chemotherapy payload of anti-insoluble fibrin antibody-drug conjugate is released specifically upon binding to fibrin

(2018) Hirobumi Fuchigami et al.   Scientific Reports

Towards antibody-drug conjugates and prodrug strategies with extracellular stimuli-responsive drug delivery in the tumor microenvironment for cancer therapy

(2017) Nicolas Joubert et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

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

(2017) Samuele Cazzamalli et al.   JOURNAL OF CONTROLLED RELEASE

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

(2017) Alberto Dal Corso et al.   JOURNAL OF CONTROLLED RELEASE

Strategies and challenges for the next generation of antibody–drug conjugates

(2017) Alain Beck et al.   NATURE REVIEWS DRUG DISCOVERY

Targeting the tumour microenvironment with an enzyme-responsive drug delivery system for the efficient therapy of breast and pancreatic cancers

(2017) Brigitte Renoux et al.   Chemical Science

Targeting Integrin αV β3 with Theranostic RGD-Camptothecin Conjugates Bearing a Disulfide Linker: Biological Evaluation Reveals a Complex Scenario

(2017) Arianna Pina et al.   ChemistrySelect

Can Integrin Agonists Have Cards to Play against Cancer? A Literature Survey of Small Molecules Integrin Activators

(2017) Alessandra Tolomelli et al.   Cancers

Intracellular Released Payload Influences Potency and Bystander-Killing Effects of Antibody-Drug Conjugates in Preclinical Models

(2016) F. Li et al.   CANCER RESEARCH

Development of BT1718, a Bicycle Drug Conjugate® (BDC) targeting MT1-MMP for treatment of solid tumours

(2016) G. Bennett et al.   EUROPEAN JOURNAL OF CANCER

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

(2016) Rémy Gébleux et al.   INTERNATIONAL JOURNAL OF CANCER

Synthesis of Novel c(AmpRGD)–Sunitinib Dual Conjugates as Molecular Tools Targeting the αvβ3 Integrin/VEGFR2 Couple and Impairing Tumor-Associated Angiogenesis

(2016) Andrea Sartori et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2016) Samuele Cazzamalli et al.   MOLECULAR CANCER THERAPEUTICS

Antibody-drug conjugates: Current status and future perspectives

(2016) Rémy Gébleux et al.   PHARMACOLOGY & THERAPEUTICS

CyclicisoDGR and RGD Peptidomimetics Containing Bifunctional Diketopiperazine Scaffolds are Integrin Antagonists

(2015) Silvia Panzeri et al.   CHEMISTRY-A EUROPEAN JOURNAL

Synthesis and Biological Evaluation of RGD Peptidomimetic-Paclitaxel Conjugates Bearing Lysosomally Cleavable Linkers

(2015) Alberto Dal Corso et al.   CHEMISTRY-A EUROPEAN JOURNAL

?v?3 Integrin-Targeted Peptide/Peptidomimetic-Drug Conjugates: In-Depth Analysis of the Linker Technology

(2015) Alberto Dal Corso et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Design, Synthesis, and Biological Evaluation of Theranostic Vitamin–Linker–Taxoid Conjugates

(2015) Jacob G. Vineberg et al.   JOURNAL OF MEDICINAL CHEMISTRY

DUPA Conjugation of a Cytotoxic Indenoisoquinoline Topoisomerase I Inhibitor for Selective Prostate Cancer Cell Targeting

(2015) Jyoti Roy et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2015) R. Gebleux et al.   MOLECULAR CANCER THERAPEUTICS

Principles in the design of ligand-targeted cancer therapeutics and imaging agents

(2015) Madduri Srinivasarao et al.   NATURE REVIEWS DRUG DISCOVERY

A Small-Molecule Drug Conjugate for the Treatment of Carbonic Anhydrase IX Expressing Tumors

(2014) Nikolaus Krall et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Antibody-Drug Conjugates: An Emerging Concept in Cancer Therapy

(2014) Ravi V. J. Chari et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Curative Properties of Noninternalizing Antibody-Drug Conjugates Based on Maytansinoids

(2014) E. Perrino et al.   CANCER RESEARCH

Small Targeted Cytotoxics: Current State and Promises from DNA-Encoded Chemical Libraries

(2013) Nikolaus Krall et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Conjugates of Modified Cryptophycins and RGD-Peptides Enter Target Cells by Endocytosis

(2013) Markus Nahrwold et al.   JOURNAL OF MEDICINAL CHEMISTRY

The First Generation of β-Galactosidase-Responsive Prodrugs Designed for the Selective Treatment of Solid Tumors in Prodrug Monotherapy

(2012) Thibaut Legigan et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Targeting the Estrogen Receptor using Steroid–Therapeutic Drug Conjugates (Hybrids)

(2012) Kinh-Luan Dao et al.   BIOCONJUGATE CHEMISTRY

Cyclic RGD Peptidomimetics Containing Bifunctional Diketopiperazine Scaffolds as New Potent Integrin Ligands

(2012) Mattia Marchini et al.   CHEMISTRY-A EUROPEAN JOURNAL

Synthesis and Biological Evaluation (in Vitro and in Vivo) of Cyclic Arginine–Glycine–Aspartate (RGD) Peptidomimetic–Paclitaxel Conjugates Targeting Integrin αVβ3

(2012) Raffaele Colombo et al.   JOURNAL OF MEDICINAL CHEMISTRY

Direct Fluorescence Monitoring of the Delivery and Cellular Uptake of a Cancer-Targeted RGD Peptide-Appended Naphthalimide Theragnostic Prodrug

(2012) Min Hee Lee et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

A Traceless Vascular-Targeting Antibody-Drug Conjugate for Cancer Therapy

(2011) Gonçalo J. L. Bernardes et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Cancer-Stroma Targeting Therapy by Cytotoxic Immunoconjugate Bound to the Collagen 4 Network in the Tumor Tissue

(2011) Masahiro Yasunaga et al.   BIOCONJUGATE CHEMISTRY

Hallmarks of Cancer: The Next Generation

(2011) Douglas Hanahan et al.   CELL

In Vitro and In Vivo Responses of Advanced Prostate Tumors to PSMA ADC, an Auristatin-Conjugated Antibody to Prostate-Specific Membrane Antigen

(2011) X. Wang et al.   MOLECULAR CANCER THERAPEUTICS

Antibody drug-conjugates targeting the tumor vasculature

(2010) Hans-Peter Gerber et al.   mAbs

Prostate-Specific Membrane Antigen Targeted Imaging and Therapy of Prostate Cancer Using a PSMA Inhibitor as a Homing Ligand

(2009) Sumith A. Kularatne et al.   MOLECULAR PHARMACEUTICS