CyclicisoDGR and RGD Peptidomimetics Containing Bifunctional Diketopiperazine Scaffolds are Integrin Antagonists

Cilengitide combined with standard treatment for patients with newly diagnosed glioblastoma with methylated MGMT promoter (CENTRIC EORTC 26071-22072 study): a multicentre, randomised, open-label, phase 3 trial

(2014) Roger Stupp et al.   LANCET ONCOLOGY

Targeting of Alpha-V Integrins Reduces Malignancy of Bladder Carcinoma

(2014) Geertje van der Horst et al.   PLoS One

CyclicisoDGR Peptidomimetics as Low-Nanomolar αvβ3Integrin Ligands

(2013) Michele Mingozzi et al.   CHEMISTRY-A EUROPEAN JOURNAL

Determination of the binding epitope of RGD-peptidomimetics to αvβ3 and αIIbβ3 integrin-rich intact cells by NMR and computational studies

(2013) Ileana Guzzetti et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Molecular Dynamics Reveal that isoDGR-Containing Cyclopeptides Are True αvβ3 Antagonists Unable To Promote Integrin Allostery and Activation

(2012) Michela Ghitti et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

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

Use of Metadynamics in the Design of isoDGR-Based αvβ3 Antagonists To Fine-Tune the Conformational Ensemble

(2011) Andrea Spitaleri et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Increasing αvβ3 Selectivity of the Anti-Angiogenic Drug Cilengitide by N-Methylation

(2011) Carlos Mas-Moruno et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Cilengitide: The First Anti-Angiogenic Small Molecule Drug Candidate. Design, Synthesis and Clinical Evaluation

(2011) Carlos Mas-Moruno et al.   Anti-Cancer Agents in Medicinal Chemistry

Isoaspartate-dependent molecular switches for integrin-ligand recognition

(2011) A. Corti et al.   JOURNAL OF CELL SCIENCE

Cilengitide in patients with recurrent glioblastoma: the results of NABTC 03-02, a phase II trial with measures of treatment delivery

(2011) Mark R. Gilbert et al.   JOURNAL OF NEURO-ONCOLOGY

Conformational Control of Integrin-Subtype Selectivity in isoDGR Peptide Motifs: A Biological Switch

(2010) Andreas O. Frank et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Targeting αvβ3 Integrin: Design and Applications of Mono- and Multifunctional RGD-Based Peptides and Semipeptides

(2010) L. Auzzas et al.   CURRENT MEDICINAL CHEMISTRY

Critical Role of Flanking Residues in NGR-to-isoDGR Transition and CD13/Integrin Receptor Switching

(2010) Flavio Curnis et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Integrins as therapeutic targets: lessons and opportunities

(2010) Dermot Cox et al.   NATURE REVIEWS DRUG DISCOVERY

Selective O-acylation of unprotected N-benzylserine methyl ester and O,N-acyl transfer in the formation of cyclo[Asp-Ser] diketopiperazines

(2010) Mattia Marchini et al.   TETRAHEDRON

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

(2009) Ana Sofia M. da Ressurreição et al.   CHEMISTRY-A EUROPEAN JOURNAL

Small Molecule Integrin Antagonists in Cancer Therapy

(2009) Mayra Paolillo et al.   MINI-REVIEWS IN MEDICINAL CHEMISTRY

Stimulation of tumor growth and angiogenesis by low concentrations of RGD-mimetic integrin inhibitors

(2009) Andrew R Reynolds et al.   NATURE MEDICINE

The Integrin Antagonist Cilengitide Activates αVβ3, Disrupts VE-Cadherin Localization at Cell Junctions and Enhances Permeability in Endothelial Cells

(2009) Gian Carlo Alghisi et al.   PLoS One

Isoaspartate-Glycine-Arginine: A New Tumor Vasculature-Targeting Motif

(2008) F. Curnis et al.   CANCER RESEARCH

Structural Basis for the Interaction ofisoDGR with the RGD-binding Site of αvβ3 Integrin

(2008) Andrea Spitaleri et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Cilengitide induces cellular detachment and apoptosis in endothelial and glioma cells mediated by inhibition of FAK/src/AKT pathway

(2008) Leticia Oliveira-Ferrer et al.   JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH

Synthesis and Conformational Studies of Peptidomimetics Containing a New Bifunctional Diketopiperazine Scaffold Acting as a β-Hairpin Inducer

(2007) Ana Sofia M. Ressurreição et al.   JOURNAL OF ORGANIC CHEMISTRY