Dario Neri
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View article: Translational and First-in-Human Positron Emission Tomography Targeting Prostatic Acid Phosphatase in Prostate Cancer Using the Ligand [68Ga]Ga-OncoACP3-DOTA
Translational and First-in-Human Positron Emission Tomography Targeting Prostatic Acid Phosphatase in Prostate Cancer Using the Ligand [68Ga]Ga-OncoACP3-DOTA Open
Prostate-specific membrane antigen (PSMA)-targeted theranostic agents have transformed prostate cancer (PC) management, but their performance is limited by variable PSMA expression and off-target uptake. We investigates the first-in-human …
View article: Figure S2 from Development of Multivalent FAP-Targeted Small Molecule–Drug Conjugates with Tailored MMAE Release Kinetics
Figure S2 from Development of Multivalent FAP-Targeted Small Molecule–Drug Conjugates with Tailored MMAE Release Kinetics Open
FAP release assay. Analysis of MMAE released from compounds 1, 2, and 7 in the presence of human recombinant Fibroblast Activation Protein (hFAP). Compound 7 was included as a negative control due to its inability to inhibit FAP for the ab…
View article: Supplementary Figure S8 from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer
Supplementary Figure S8 from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer Open
LC chromatogram of I8
View article: Supplementary Figure S3 from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer
Supplementary Figure S3 from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer Open
LC chromatogram of I3
View article: Supplementary Figure S11 from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer
Supplementary Figure S11 from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer Open
LC- and HRMS-traces of compound 3
View article: Supplementary Table S1 from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer
Supplementary Table S1 from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer Open
Two-way ANOVA multiple comparisons (Bonferroni test) of tumor volume of mice bearing HT1080.hPSMA tumor xenografts after treatment. Tumor growth is depicted in Figure 3.
View article: Figure S1 from Development of Multivalent FAP-Targeted Small Molecule–Drug Conjugates with Tailored MMAE Release Kinetics
Figure S1 from Development of Multivalent FAP-Targeted Small Molecule–Drug Conjugates with Tailored MMAE Release Kinetics Open
Chemical structures of the previously described compounds.
View article: Supplementary FIgure S7 from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer
Supplementary FIgure S7 from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer Open
LC chromatogram of I7
View article: Supplementary Figure S16 from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer
Supplementary Figure S16 from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer Open
Ex vivo pharmacokinetic study of OncoPSMA-GlyPro-MMAE (1). Plasma was extracted from mice (n = 3) after 1, 6, or 24hours, and SMDC content was quantified via MS using an internal standard (OncoPSMA-GlyPro-MMAE-d5).
View article: Supplementary Figure S1 from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer
Supplementary Figure S1 from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer Open
LC chromatogram of I1
View article: Supplementary Figure S13 from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer
Supplementary Figure S13 from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer Open
LC- and HRMS-traces of compound 5
View article: Supplementary Figure S12 from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer
Supplementary Figure S12 from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer Open
LC- and HRMS-traces of compound 4
View article: Supplementary Figure S9 from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer
Supplementary Figure S9 from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer Open
LC- and HRMS-traces of compound 1
View article: Generation and characterization of novel high-affinity fully human antibodies targeting prostate-specific membrane antigen and prostatic acid phosphatase
Generation and characterization of novel high-affinity fully human antibodies targeting prostate-specific membrane antigen and prostatic acid phosphatase Open
Background Prostate-specific membrane antigen (PSMA)-targeted therapies have revolutionized the management of patients with prostate cancer. However, not all patients benefit from such agents. Prostatic acid phosphatase (ACP3), a tyrosine …
View article: Supplementary Figure S5 from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer
Supplementary Figure S5 from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer Open
LC chromatogram of I5
View article: Figure S4 from Development of Multivalent FAP-Targeted Small Molecule–Drug Conjugates with Tailored MMAE Release Kinetics
Figure S4 from Development of Multivalent FAP-Targeted Small Molecule–Drug Conjugates with Tailored MMAE Release Kinetics Open
Single mouse plots presenting tumor-growth in mice with HT-1080.hFAP (based on HT1080.wt, RRID: CVCL_0317) CDX model after treatment with OncoFAP-GlyPro-MMAE (1) or TriOncoFAP-GlyPro-MMAE (2) (dose = 250 nmol/kg, 125 nmol/kg, or 50 nmol/kg…
View article: Supplementary Information (SI) from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer
Supplementary Information (SI) from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer Open
Detailed synthetic procedures and characterization of the presented compounds are described in the Supplementary Information , together with additional serum stability data, biodistribution data, and statistical analysis of therapy experim…
View article: Supplementary Information from Development of Multivalent FAP-Targeted Small Molecule–Drug Conjugates with Tailored MMAE Release Kinetics
Supplementary Information from Development of Multivalent FAP-Targeted Small Molecule–Drug Conjugates with Tailored MMAE Release Kinetics Open
Supplementary Information
View article: Supplementary Table S2 from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer
Supplementary Table S2 from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer Open
Two-way ANOVA multiple comparisons (Bonferroni test) of tumor volume of mice bearing HT1080.hPSMA tumor xenografts after treatment. Tumor growth is depicted in Figure 4C.
View article: Data from Development of Multivalent FAP-Targeted Small Molecule–Drug Conjugates with Tailored MMAE Release Kinetics
Data from Development of Multivalent FAP-Targeted Small Molecule–Drug Conjugates with Tailored MMAE Release Kinetics Open
Antibody–drug conjugates are one of the most diffused targeted therapeutic modalities for cancer treatment and consist of a tumor-targeted monoclonal antibody connected to a cytotoxic payload, which is released selectively at the tumor sit…
View article: Data from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer
Data from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer Open
Prostate-specific membrane antigen (PSMA) is a transmembrane glycoprotein that is overexpressed on the surface of cancerous prostate cells both in primary tumors and in metastases. Small organic ligands targeting PSMA have been broadly and…
View article: Supplementary Figure S2 from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer
Supplementary Figure S2 from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer Open
LC chromatogram of I2
View article: Supplementary Figure S10 from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer
Supplementary Figure S10 from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer Open
LC- and HRMS-traces of compound 2
View article: Supplementary Figure S6 from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer
Supplementary Figure S6 from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer Open
LC chromatogram of I6
View article: Supplementary Figure S4 from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer
Supplementary Figure S4 from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer Open
LC chromatogram of I4
View article: KS04.7.A L19TNF IN COMBINATION WITH TEMOZOLOMIDE-BASED CHEMORADIATION FOR PATIENTS WITH NEWLY DIAGNOSED GLIOBLASTOMA SHOWS PROMISING SAFETY AND OVERALL SURVIVAL SIGNALS IN A PHASE I STUDY
KS04.7.A L19TNF IN COMBINATION WITH TEMOZOLOMIDE-BASED CHEMORADIATION FOR PATIENTS WITH NEWLY DIAGNOSED GLIOBLASTOMA SHOWS PROMISING SAFETY AND OVERALL SURVIVAL SIGNALS IN A PHASE I STUDY Open
BACKGROUND Targeted cytokine-based therapy is a promising treatment opportunity to potentially convert an immunologically “cold” tumor microenvironment into a “hot” one and trigger a potent antitumor response. L19TNF is a fully human antib…
View article: Figure S6 from Development of Multivalent FAP-Targeted Small Molecule–Drug Conjugates with Tailored MMAE Release Kinetics
Figure S6 from Development of Multivalent FAP-Targeted Small Molecule–Drug Conjugates with Tailored MMAE Release Kinetics Open
MMAE mechanism of action characterization. A) Enriched pathway analysis of the dysregulated proteins at 96 hours after administration of compound 1. B-C) Expression of the most dysregulated proteins for the enriched pathway in A. One-way A…
View article: Figure S3 from Development of Multivalent FAP-Targeted Small Molecule–Drug Conjugates with Tailored MMAE Release Kinetics
Figure S3 from Development of Multivalent FAP-Targeted Small Molecule–Drug Conjugates with Tailored MMAE Release Kinetics Open
Percentage of body weight changes in mice bearing HT-1080.hFAP (based on HT1080.wt, RRID:CVCL_0317) tumor model over the course of the therapy with OncoFAP-GlyPro-MMAE (1) and TriOncoFAP-GlyPro-MMAE (2) (dose = 250 nmol/kg (A), 125 nmol/kg…
View article: Supplementary Figure S14 from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer
Supplementary Figure S14 from PSMA-Targeted Small Molecule–Drug Conjugates Based on a Postprolyl Peptidase–Cleavable Linker for the Treatment of Prostate Cancer Open
LC trace of compound 6
View article: Figure S5 from Development of Multivalent FAP-Targeted Small Molecule–Drug Conjugates with Tailored MMAE Release Kinetics
Figure S5 from Development of Multivalent FAP-Targeted Small Molecule–Drug Conjugates with Tailored MMAE Release Kinetics Open
Ex vivo evaluation of apoptosis induced by the SMDCs over time. Fluorescent detection of the apoptosis marker Caspase-3 in tumor’s cryosection of the untreated group (time 0). Green = Caspase 3, Red = CD31; scale bar = 200 µm.