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Papers by Angelina Boccarelli
European journal of medicinal chemistry, Mar 1, 2024
Antioxidants, Jan 21, 2024
This article is an open access article distributed under the terms and conditions of the Creative... more This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY
International journal of molecular sciences, Apr 17, 2024
This article is an open access article distributed under the terms and conditions of the Creative... more This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY
Pathology Research and Practice, Feb 1, 2023
European Journal of Inorganic Chemistry, Oct 1, 2008
New cis-and trans-dichloridoplatinum(II) complexes, which contain two amidine ligands or one amid... more New cis-and trans-dichloridoplatinum(II) complexes, which contain two amidine ligands or one amidine and one ammine ligand, cis-and trans-[PtCl 2 {(Z)-HN=C(NH 2)CH 3 } 2 ] (1) and cis-and trans-[PtCl 2 (NH 3){(Z)-HN=C(NH 2)CH 3 }] (2), have been prepared from the corresponding nitrile complexes by amminolysis in thf solution. All synthesized compounds were characterized by elemental analysis, ESI-MS, and IR and NMR spectroscopy. Amidines are isosters of iminoethers and ketimines. The trans isomers of the platinum complexes of the latter are endowed with an unexpectedly high antitumor activity. An important feature of complexes 1 and 2, as compared to iminoethers, is the exclusive preference for the Z [a] Dipartimento Farmaco-Chimico,
PDF file, 113K, Effect of SU11274 treatment on PCs of newly diagnosed MM patients.
This was performed by SYBR Green and the StepOne system (Applied Biosystems, Foster City, CA, USA... more This was performed by SYBR Green and the StepOne system (Applied Biosystems, Foster City, CA, USA) (1). The PCR was conducted using HGF (5'-TCCACGGAAGAGGAGATGAGA-3'/5'-GGCCATATACCAGCTGGGAAA-3'), cMET (5'-GCTAAAATGCTGGCACCCTAA-3'/5'-ATATCCGGGACACCAGTTCAGA-3'), and control glyceraldehyde 3 phosphate dehydrogenase (GAPDH; 5′-GAAGGTGAAGGTCGGAGT-3′/5′-CATGGGTGGAATCATATTGGAA-3′) primers (Invitrogen, Paisley, UK). The mRNA was quantified using GAPDH as the reference gene and the 2-∆∆CT formula (2). Immunoprecipitation and Western blot Total proteins from the MM patients' plasma cells (PCs, 5×10 5 /patient) and the MM cell lines (2×10 6 /sample) were incubated with anti-cMET antibody, and antigen-antibody complexes immunoprecipitated by Protein G/agarose. Protein aliquots (50 μg) were immunoblotted with anti-cMET and anti-phospho(p)-cMET (p-cMET, Tyr1349) antibodies (both from Cell Signaling Technology, Danvers, MA, USA) (3). Immunoreactive bands were detected with enhanced chemiluminescence (LiteAblot ® , Euroclone, Milan, Italy) and the Gel-Logic1500 system (Eastman Kodak Co., Rochester, NY, USA), and quantified as optical density (OD) units by the Kodak imaging software. Florescence-activated cell sorting (FACS) Patients' bone marrow mononuclear cells (BMMCs, 1×10 6 cells/tube) and the MM cell lines (5×10 5 cells/tube) were incubated with fluorescein isothiocyanate (FITC)-conjugated mouse anti-cMET, rabbit anti-p-cMET (Y1234/1235), and isotype matched control antibodies (R&D Systems, Inc.,
PDF file, 91K, Functional analysis of differentially expressed genes in RPMI8226 or R5 cells afte... more PDF file, 91K, Functional analysis of differentially expressed genes in RPMI8226 or R5 cells after SU11274 treatment.
FACS analysis of cMET/phospho(p)-cMET expression in MM.1R vs. MM.1S cells. (A) The cell rate as c... more FACS analysis of cMET/phospho(p)-cMET expression in MM.1R vs. MM.1S cells. (A) The cell rate as co-expression or mono-expression is given. Note the higher expression of p-cMET in MM.1R cells. (B) p-cMET expression upon a 6-h treatment with SU11274 at 1 µM: only MM.1R cells reduced the expression substantially. A representative experiment out of five is shown. Supplementary Figure S2 Effect of SU11274 treatment on cMET/phospho(p)-cMET expression in R5 vs. RPMI8226 cells; and plasma cells (PCs) from relapsed/resistant vs. newly diagnosed MM patients. (A)
PDF file, 97K, SU11274 impacts marginally on in vivo growth of RPMI8226 plasmocytomas. It reverts... more PDF file, 97K, SU11274 impacts marginally on in vivo growth of RPMI8226 plasmocytomas. It reverts bortezomib-resistance in R5 plasmocytomas.
PDF file, 93K, FACS analysis of cMET/phospho(p)-cMET expression in MM.1R vs. MM.1S cells.
PDF file, 121K, SU11274 inhibits p-cMET expression and chemotaxis toward fibroblasts' conditi... more PDF file, 121K, SU11274 inhibits p-cMET expression and chemotaxis toward fibroblasts' conditioned medium more intensely in R5 cells.
Purpose: The aim of the study was to verify the hypothesis that the cMet oncogene is implicated i... more Purpose: The aim of the study was to verify the hypothesis that the cMet oncogene is implicated in chemio- and novel drug resistance in multiple myeloma.Experimental Design: We have evaluated the expression levels of cMET/phospho-cMET (p-cMET) and the activity of the novel selective p-cMET inhibitor (SU11274) in multiple myeloma cells, either sensitive (RPMI-8226 and MM.1S) or resistant (R5 and MM.1R) to anti–multiple myeloma drugs, in primary plasma cells and in multiple myeloma xenograft models.Results: We found that resistant R5 and MM.1R cells presented with higher cMET phosphorylation, thus leading to constitutive activation of cMET-dependent signaling pathways. R5 cells exhibited a higher susceptibility to the SU11274 inhibitory effects on viability, proliferation, chemotaxis, adhesion, and to its apoptogenic effects. SU11274 was able to revert drug resistance in R5 cells. R5 but not RPMI-8226 cells displayed cMET-dependent activation of mitogen-activated protein kinase pathwa...
PDF file, 77K, An anti-cMET neutralizing antibody leads to modulation of phospho(p)-proteins in M... more PDF file, 77K, An anti-cMET neutralizing antibody leads to modulation of phospho(p)-proteins in MM cell lines.
European journal of medicinal chemistry, Mar 1, 2024
Antioxidants, Jan 21, 2024
This article is an open access article distributed under the terms and conditions of the Creative... more This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY
International journal of molecular sciences, Apr 17, 2024
This article is an open access article distributed under the terms and conditions of the Creative... more This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY
Pathology Research and Practice, Feb 1, 2023
European Journal of Inorganic Chemistry, Oct 1, 2008
New cis-and trans-dichloridoplatinum(II) complexes, which contain two amidine ligands or one amid... more New cis-and trans-dichloridoplatinum(II) complexes, which contain two amidine ligands or one amidine and one ammine ligand, cis-and trans-[PtCl 2 {(Z)-HN=C(NH 2)CH 3 } 2 ] (1) and cis-and trans-[PtCl 2 (NH 3){(Z)-HN=C(NH 2)CH 3 }] (2), have been prepared from the corresponding nitrile complexes by amminolysis in thf solution. All synthesized compounds were characterized by elemental analysis, ESI-MS, and IR and NMR spectroscopy. Amidines are isosters of iminoethers and ketimines. The trans isomers of the platinum complexes of the latter are endowed with an unexpectedly high antitumor activity. An important feature of complexes 1 and 2, as compared to iminoethers, is the exclusive preference for the Z [a] Dipartimento Farmaco-Chimico,
PDF file, 113K, Effect of SU11274 treatment on PCs of newly diagnosed MM patients.
This was performed by SYBR Green and the StepOne system (Applied Biosystems, Foster City, CA, USA... more This was performed by SYBR Green and the StepOne system (Applied Biosystems, Foster City, CA, USA) (1). The PCR was conducted using HGF (5'-TCCACGGAAGAGGAGATGAGA-3'/5'-GGCCATATACCAGCTGGGAAA-3'), cMET (5'-GCTAAAATGCTGGCACCCTAA-3'/5'-ATATCCGGGACACCAGTTCAGA-3'), and control glyceraldehyde 3 phosphate dehydrogenase (GAPDH; 5′-GAAGGTGAAGGTCGGAGT-3′/5′-CATGGGTGGAATCATATTGGAA-3′) primers (Invitrogen, Paisley, UK). The mRNA was quantified using GAPDH as the reference gene and the 2-∆∆CT formula (2). Immunoprecipitation and Western blot Total proteins from the MM patients' plasma cells (PCs, 5×10 5 /patient) and the MM cell lines (2×10 6 /sample) were incubated with anti-cMET antibody, and antigen-antibody complexes immunoprecipitated by Protein G/agarose. Protein aliquots (50 μg) were immunoblotted with anti-cMET and anti-phospho(p)-cMET (p-cMET, Tyr1349) antibodies (both from Cell Signaling Technology, Danvers, MA, USA) (3). Immunoreactive bands were detected with enhanced chemiluminescence (LiteAblot ® , Euroclone, Milan, Italy) and the Gel-Logic1500 system (Eastman Kodak Co., Rochester, NY, USA), and quantified as optical density (OD) units by the Kodak imaging software. Florescence-activated cell sorting (FACS) Patients' bone marrow mononuclear cells (BMMCs, 1×10 6 cells/tube) and the MM cell lines (5×10 5 cells/tube) were incubated with fluorescein isothiocyanate (FITC)-conjugated mouse anti-cMET, rabbit anti-p-cMET (Y1234/1235), and isotype matched control antibodies (R&D Systems, Inc.,
PDF file, 91K, Functional analysis of differentially expressed genes in RPMI8226 or R5 cells afte... more PDF file, 91K, Functional analysis of differentially expressed genes in RPMI8226 or R5 cells after SU11274 treatment.
FACS analysis of cMET/phospho(p)-cMET expression in MM.1R vs. MM.1S cells. (A) The cell rate as c... more FACS analysis of cMET/phospho(p)-cMET expression in MM.1R vs. MM.1S cells. (A) The cell rate as co-expression or mono-expression is given. Note the higher expression of p-cMET in MM.1R cells. (B) p-cMET expression upon a 6-h treatment with SU11274 at 1 µM: only MM.1R cells reduced the expression substantially. A representative experiment out of five is shown. Supplementary Figure S2 Effect of SU11274 treatment on cMET/phospho(p)-cMET expression in R5 vs. RPMI8226 cells; and plasma cells (PCs) from relapsed/resistant vs. newly diagnosed MM patients. (A)
PDF file, 97K, SU11274 impacts marginally on in vivo growth of RPMI8226 plasmocytomas. It reverts... more PDF file, 97K, SU11274 impacts marginally on in vivo growth of RPMI8226 plasmocytomas. It reverts bortezomib-resistance in R5 plasmocytomas.
PDF file, 93K, FACS analysis of cMET/phospho(p)-cMET expression in MM.1R vs. MM.1S cells.
PDF file, 121K, SU11274 inhibits p-cMET expression and chemotaxis toward fibroblasts' conditi... more PDF file, 121K, SU11274 inhibits p-cMET expression and chemotaxis toward fibroblasts' conditioned medium more intensely in R5 cells.
Purpose: The aim of the study was to verify the hypothesis that the cMet oncogene is implicated i... more Purpose: The aim of the study was to verify the hypothesis that the cMet oncogene is implicated in chemio- and novel drug resistance in multiple myeloma.Experimental Design: We have evaluated the expression levels of cMET/phospho-cMET (p-cMET) and the activity of the novel selective p-cMET inhibitor (SU11274) in multiple myeloma cells, either sensitive (RPMI-8226 and MM.1S) or resistant (R5 and MM.1R) to anti–multiple myeloma drugs, in primary plasma cells and in multiple myeloma xenograft models.Results: We found that resistant R5 and MM.1R cells presented with higher cMET phosphorylation, thus leading to constitutive activation of cMET-dependent signaling pathways. R5 cells exhibited a higher susceptibility to the SU11274 inhibitory effects on viability, proliferation, chemotaxis, adhesion, and to its apoptogenic effects. SU11274 was able to revert drug resistance in R5 cells. R5 but not RPMI-8226 cells displayed cMET-dependent activation of mitogen-activated protein kinase pathwa...
PDF file, 77K, An anti-cMET neutralizing antibody leads to modulation of phospho(p)-proteins in M... more PDF file, 77K, An anti-cMET neutralizing antibody leads to modulation of phospho(p)-proteins in MM cell lines.