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Article ; Online: Generation of a homozygous CIITA knockout iPS cell line using the CRISPR-Cas9 system.

Romano, Elena / Trionfini, Piera / Giampietro, Roberta / Benigni, Ariela / Tomasoni, Susanna

2021 Volume 57, Page(s) 102580

Abstract: Human induced pluripotent stem cells (iPSCs) have great promise in regenerative medicine. However, several limitations, including immune-incompatibility, have raised concerns regarding their clinical application. Recent studies have shown that human ... ...

Abstract	Human induced pluripotent stem cells (iPSCs) have great promise in regenerative medicine. However, several limitations, including immune-incompatibility, have raised concerns regarding their clinical application. Recent studies have shown that human iPSCs and their derivatives lose their immunogenicity when major histocompatibility complex (MHC) class I and II genes are inactivated and CD47 is over-expressed. In this study, we used CRISPR-Cas9 technology to generate an isogenic iPSC line with a homozygous frameshift mutation in the MHC II transactivator (CIITA) gene. The CIITA
Language	English
Publishing date	2021-10-18
Publishing country	England
Document type	Journal Article
ZDB-ID	2393143-7
ISSN	1876-7753 ; 1873-5061
ISSN (online)	1876-7753
ISSN	1873-5061
DOI	10.1016/j.scr.2021.102580
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Article ; Online: Hypoimmunogenic Human Pluripotent Stem Cells as a Powerful Tool for Liver Regenerative Medicine.

Trionfini, Piera / Romano, Elena / Varinelli, Marco / Longaretti, Lorena / Rizzo, Paola / Giampietro, Roberta / Caroli, Annalina / Aiello, Sistiana / Todeschini, Marta / Casiraghi, Federica / Remuzzi, Giuseppe / Benigni, Ariela / Tomasoni, Susanna

International journal of molecular sciences

2023 Volume 24, Issue 14

Abstract: Induced pluripotent stem cells (iPSC) have huge potential as cell therapy for various diseases, given their potential for unlimited self-renewal and capability to differentiate into a wide range of cell types. Although autologous iPSCs represents the ... ...

Abstract	Induced pluripotent stem cells (iPSC) have huge potential as cell therapy for various diseases, given their potential for unlimited self-renewal and capability to differentiate into a wide range of cell types. Although autologous iPSCs represents the ideal source for patient-tailored regenerative medicine, the high costs of the extensive and time-consuming production process and the impracticability for treating acute conditions hinder their use for broad applications. An allogeneic iPSC-based strategy may overcome these issues, but it carries the risk of triggering an immune response. So far, several approaches based on genome-editing techniques to silence human leukocyte antigen class I (HLA-I) or II (HLA-II) expression have been explored to overcome the immune rejection of allogeneic iPSCs. In this study, we employed the CRISPR/Cas9 (clustered regularly interspaced short palindromic repeats/CRISPR associated protein 9) system to delete the β2-Microglobulin (
MeSH term(s)	Humans ; Regenerative Medicine ; Pluripotent Stem Cells ; Gene Editing/methods ; Induced Pluripotent Stem Cells ; Histocompatibility Antigens Class I/genetics ; Histocompatibility Antigens Class I/metabolism ; Liver
Chemical Substances	Histocompatibility Antigens Class I
Language	English
Publishing date	2023-07-22
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2019364-6
ISSN	1422-0067 ; 1422-0067 ; 1661-6596
ISSN (online)	1422-0067
ISSN	1422-0067 ; 1661-6596
DOI	10.3390/ijms241411810
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Article ; Online: The Pivotal Role of Copper in Neurodegeneration: A New Strategy for the Therapy of Neurodegenerative Disorders.

Giampietro, Roberta / Spinelli, Francesco / Contino, Marialessandra / Colabufo, Nicola Antonio

Molecular pharmaceutics

2018 Volume 15, Issue 3, Page(s) 808–820

Abstract: Copper is an essential trace element for the human body since it is a cofactor of several enzymes and proteins and plays a pivotal role in several biological functions (e.g., respiration, protection from oxidative damage, iron metabolism, etc.), also ... ...

Abstract	Copper is an essential trace element for the human body since it is a cofactor of several enzymes and proteins and plays a pivotal role in several biological functions (e.g., respiration, protection from oxidative damage, iron metabolism, etc.), also including the central nervous system development and functioning (e.g., synthesis of neurotransmitters, myelination, activation of neuropeptides, etc.). Therefore, copper dysmetabolism is associated with different toxic effects, mainly represented by oxidative stress, and it has been reported in many neurodegenerative disorders, such as Wilson's disease, Menkes disease, Alzheimer's disease, Parkinson's disease, and amyotrophic lateral sclerosis. This paper shows a detailed report of how copper is involved in the pathophysiology of these diseases. Moreover, a hint on novel therapeutic approaches based on restoring copper homeostasis through metal chelators will be pointed out.
MeSH term(s)	Animals ; Brain Chemistry/drug effects ; Chelating Agents/pharmacology ; Chelating Agents/therapeutic use ; Copper/metabolism ; Copper/toxicity ; Copper-transporting ATPases/genetics ; Copper-transporting ATPases/metabolism ; Disease Models, Animal ; Humans ; Neurodegenerative Diseases/drug therapy ; Neurodegenerative Diseases/genetics ; Neurodegenerative Diseases/metabolism ; Neurodegenerative Diseases/pathology ; Oxidative Stress/drug effects ; Superoxide Dismutase-1/genetics ; Superoxide Dismutase-1/metabolism
Chemical Substances	Chelating Agents ; SOD1 protein, human ; Copper (789U1901C5) ; Superoxide Dismutase-1 (EC 1.15.1.1) ; Copper-transporting ATPases (EC 3.6.3.54)
Language	English
Publishing date	2018-02-02
Publishing country	United States
Document type	Journal Article ; Review
ZDB-ID	2138405-8
ISSN	1543-8392 ; 1543-8384
ISSN (online)	1543-8392
ISSN	1543-8384
DOI	10.1021/acs.molpharmaceut.7b00841
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Article ; Online: MRP1-Collateral Sensitizers as a Novel Therapeutic Approach in Resistant Cancer Therapy: An In Vitro and In Vivo Study in Lung Resistant Tumor.

Riganti, Chiara / Giampietro, Roberta / Kopecka, Joanna / Costamagna, Costanzo / Abatematteo, Francesca Serena / Contino, Marialessandra / Abate, Carmen

International journal of molecular sciences

2020 Volume 21, Issue 9

Abstract: Multidrug resistance (MDR) is the main obstacle to current chemotherapy and it is mainly due to the overexpression of some efflux transporters such as MRP1. One of the most studied strategies to overcome MDR has been the inhibition of MDR pumps through ... ...

Abstract	Multidrug resistance (MDR) is the main obstacle to current chemotherapy and it is mainly due to the overexpression of some efflux transporters such as MRP1. One of the most studied strategies to overcome MDR has been the inhibition of MDR pumps through small molecules, but its translation into the clinic unfortunately failed. Recently, a phenomenon called collateral sensitivity (CS) emerged as a new strategy to hamper MDR acting as a synthetic lethality, where the genetic changes developed upon the acquisition of resistance towards a specific agent are followed by the development of hypersensitivity towards a second agent. Among our library of sigma ligands acting as MDR modulators, we identified three compounds,
MeSH term(s)	Animals ; Antineoplastic Agents/pharmacology ; Carcinoma, Non-Small-Cell Lung/drug therapy ; Carcinoma, Non-Small-Cell Lung/enzymology ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Cell Survival/drug effects ; Drug Collateral Sensitivity ; Drug Resistance, Multiple ; Drug Resistance, Neoplasm ; Female ; Glutathione/metabolism ; Humans ; Ligands ; Lung Neoplasms/drug therapy ; Lung Neoplasms/enzymology ; Mice ; Mice, Inbred BALB C ; Multidrug Resistance-Associated Proteins/metabolism ; Reactive Oxygen Species/metabolism ; Xenograft Model Antitumor Assays
Chemical Substances	Antineoplastic Agents ; Ligands ; Multidrug Resistance-Associated Proteins ; Reactive Oxygen Species ; Glutathione (GAN16C9B8O) ; multidrug resistance-associated protein 1 (Y49M64GZ4Q)
Language	English
Publishing date	2020-05-08
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2019364-6
ISSN	1422-0067 ; 1422-0067 ; 1661-6596
ISSN (online)	1422-0067
ISSN	1422-0067 ; 1661-6596
DOI	10.3390/ijms21093333
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Article ; Online: One molecule two goals: A selective P-glycoprotein modulator increases drug transport across gastro-intestinal barrier and recovers doxorubicin toxicity in multidrug resistant cancer cells.

Contino, Marialessandra / Guglielmo, Stefano / Riganti, Chiara / Antonello, Giulia / Perrone, Maria Grazia / Giampietro, Roberta / Rolando, Barbara / Fruttero, Roberta / Colabufo, Nicola A

European journal of medicinal chemistry

2020 Volume 208, Page(s) 112843

Abstract: In the present study a series of tetrahydroisoquinoline derivatives were synthesized and evaluated for their activity towards three ABC transporters, P-gp, MRP1 and BCRP. The compounds proved to be selective against P-gp. One of them, 8b, displayed ... ...

Abstract	In the present study a series of tetrahydroisoquinoline derivatives were synthesized and evaluated for their activity towards three ABC transporters, P-gp, MRP1 and BCRP. The compounds proved to be selective against P-gp. One of them, 8b, displayed activity in the nanomolar range (EC
MeSH term(s)	ATP Binding Cassette Transporter, Subfamily B, Member 1/metabolism ; Animals ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/pharmacology ; Caco-2 Cells ; Dogs ; Doxorubicin/chemical synthesis ; Doxorubicin/pharmacology ; Drug Resistance, Neoplasm/drug effects ; Humans ; Isoquinolines/chemical synthesis ; Isoquinolines/pharmacology ; Madin Darby Canine Kidney Cells ; Proof of Concept Study
Chemical Substances	ATP Binding Cassette Transporter, Subfamily B, Member 1 ; Antineoplastic Agents ; Isoquinolines ; Doxorubicin (80168379AG)
Language	English
Publishing date	2020-09-17
Publishing country	France
Document type	Journal Article
ZDB-ID	188597-2
ISSN	1768-3254 ; 0009-4374 ; 0223-5234
ISSN (online)	1768-3254
ISSN	0009-4374 ; 0223-5234
DOI	10.1016/j.ejmech.2020.112843
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Article ; Online: Insights into P-Glycoprotein Inhibitors: New Inducers of Immunogenic Cell Death.

Kopecka, Joanna / Godel, Martina / Dei, Silvia / Giampietro, Roberta / Belisario, Dimas Carolina / Akman, Muhlis / Contino, Marialessandra / Teodori, Elisabetta / Riganti, Chiara

Cells

2020 Volume 9, Issue 4

Abstract: Doxorubicin is a strong inducer of immunogenic cell death (ICD), but it is ineffective in P-glycoprotein (Pgp)-expressing cells. Indeed, Pgp effluxes doxorubicin and impairs the immunesensitizing functions of calreticulin (CRT), an "eat-me" signal ... ...

Abstract	Doxorubicin is a strong inducer of immunogenic cell death (ICD), but it is ineffective in P-glycoprotein (Pgp)-expressing cells. Indeed, Pgp effluxes doxorubicin and impairs the immunesensitizing functions of calreticulin (CRT), an "eat-me" signal mediating ICD. It is unknown if classical Pgp inhibitors, designed to reverse chemoresistance, may restore ICD. We addressed this question by using Pgp-expressing cancer cells, treated with Tariquidar, a clinically approved Pgp inhibitor, and
MeSH term(s)	ATP Binding Cassette Transporter, Subfamily B, Member 1/antagonists & inhibitors ; ATP Binding Cassette Transporter, Subfamily B, Member 1/metabolism ; Apoptosis/drug effects ; Calreticulin/metabolism ; Cell Line, Tumor ; Doxorubicin/pharmacology ; Drug Resistance, Neoplasm/drug effects ; Endocytosis/drug effects ; Esters/pharmacology ; Humans ; Immunogenic Cell Death/drug effects ; Kinetics ; Proteolysis/drug effects ; Quinolines/pharmacology ; Ubiquitination/drug effects
Chemical Substances	ATP Binding Cassette Transporter, Subfamily B, Member 1 ; Calreticulin ; Esters ; Quinolines ; Doxorubicin (80168379AG) ; tariquidar (J58862DTVD)
Language	English
Publishing date	2020-04-22
Publishing country	Switzerland
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	2661518-6
ISSN	2073-4409 ; 2073-4409
ISSN (online)	2073-4409
ISSN	2073-4409
DOI	10.3390/cells9041033
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Article: Unravelling the Role of PAX2 Mutation in Human Focal Segmental Glomerulosclerosis.

Longaretti, Lorena / Trionfini, Piera / Brizi, Valerio / Xinaris, Christodoulos / Mele, Caterina / Breno, Matteo / Romano, Elena / Giampietro, Roberta / Remuzzi, Giuseppe / Benigni, Ariela / Tomasoni, Susanna

Biomedicines

2021 Volume 9, Issue 12

Abstract: No effective treatments are available for familial steroid-resistant Focal Segmental Glomerulosclerosis (FSGS), characterized by proteinuria due to ultrastructural abnormalities in glomerular podocytes. Here, we studied a private PAX2 mutation identified ...

Abstract	No effective treatments are available for familial steroid-resistant Focal Segmental Glomerulosclerosis (FSGS), characterized by proteinuria due to ultrastructural abnormalities in glomerular podocytes. Here, we studied a private PAX2 mutation identified in a patient who developed FSGS in adulthood. By generating adult podocytes using patient-specific induced pluripotent stem cells (iPSC), we developed an in vitro model to dissect the role of this mutation in the onset of FSGS. Despite the PAX2 mutation, patient iPSC properly differentiated into podocytes that exhibited a normal structure and function when compared to control podocytes. However, when exposed to an environmental trigger, patient podocytes were less viable and more susceptible to cell injury. Fixing the mutation improved their phenotype and functionality. Using a branching morphogenesis assay, we documented developmental defects in patient-derived ureteric bud-like tubules that were totally rescued by fixing the mutation. These data strongly support the hypothesis that the PAX2 mutation has a dual effect, first in renal organogenesis, which could account for a suboptimal nephron number at birth, and second in adult podocytes, which are more susceptible to cell death caused by environmental triggers. These abnormalities might translate into the development of proteinuria in vivo, with a progressive decline in renal function, leading to FSGS.
Language	English
Publishing date	2021-12-01
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2720867-9
ISSN	2227-9059
ISSN	2227-9059
DOI	10.3390/biomedicines9121808
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Article ; Online: 6,7-Dimethoxy-2-phenethyl-1,2,3,4-tetrahydroisoquinoline amides and corresponding ester isosteres as multidrug resistance reversers.

Braconi, Laura / Bartolucci, Gianluca / Contino, Marialessandra / Chiaramonte, Niccolò / Giampietro, Roberta / Manetti, Dina / Perrone, Maria Grazia / Romanelli, Maria Novella / Colabufo, Nicola Antonio / Riganti, Chiara / Dei, Silvia / Teodori, Elisabetta

Journal of enzyme inhibition and medicinal chemistry

2020 Volume 35, Issue 1, Page(s) 974–992

Abstract: Aiming to deepen the structure-activity relationships of the two P-glycoprotein (P-gp) modulators elacridar and tariquidar, a new series of amide and ester derivatives carrying a 6,7-dimethoxy-2-phenethyl-1,2,3,4-tetrahydroisoquinoline scaffold linked to ...

Abstract	Aiming to deepen the structure-activity relationships of the two P-glycoprotein (P-gp) modulators elacridar and tariquidar, a new series of amide and ester derivatives carrying a 6,7-dimethoxy-2-phenethyl-1,2,3,4-tetrahydroisoquinoline scaffold linked to different methoxy-substituted aryl moieties were synthesised. The obtained compounds were evaluated for their P-gp interaction profile and selectivity towards the two other ABC transporters, multidrug-resistance-associated protein-1 and breast cancer resistance protein, showing to be very active and selective versus P-gp. Two amide derivatives, displaying the best P-gp activity, were tested in co-administration with the antineoplastic drug doxorubicin in different cancer cell lines, showing a significant sensitising activity towards doxorubicin. The investigation on the chemical stability of the derivatives towards spontaneous or enzymatic hydrolysis, showed that amides are stable in both models while some ester compounds were hydrolysed in human plasma. This study allowed us to identify two chemosensitizers that behave as non-transported substrates and are characterised by different selectivity profiles.
MeSH term(s)	ATP Binding Cassette Transporter, Subfamily B, Member 1/antagonists & inhibitors ; ATP Binding Cassette Transporter, Subfamily B, Member 1/metabolism ; Amides/chemical synthesis ; Amides/chemistry ; Amides/pharmacology ; Animals ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacology ; Cells, Cultured ; Dogs ; Dose-Response Relationship, Drug ; Doxorubicin/pharmacology ; Drug Resistance, Multiple/drug effects ; Drug Resistance, Neoplasm/drug effects ; Drug Screening Assays, Antitumor ; Esters/chemical synthesis ; Esters/chemistry ; Esters/pharmacology ; Humans ; Molecular Structure ; Neoplasms/drug therapy ; Neoplasms/metabolism ; Structure-Activity Relationship ; Tetrahydroisoquinolines/chemical synthesis ; Tetrahydroisoquinolines/chemistry ; Tetrahydroisoquinolines/pharmacology
Chemical Substances	ATP Binding Cassette Transporter, Subfamily B, Member 1 ; Amides ; Antineoplastic Agents ; Esters ; Tetrahydroisoquinolines ; 1,2,3,4-tetrahydroisoquinoline (56W89FBX3E) ; Doxorubicin (80168379AG)
Language	English
Publishing date	2020-04-04
Publishing country	England
Document type	Journal Article
ZDB-ID	2082578-X
ISSN	1475-6374 ; 1475-6366
ISSN (online)	1475-6374
ISSN	1475-6366
DOI	10.1080/14756366.2020.1747449
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Article ; Online: Design, Biological Evaluation, and Molecular Modeling of Tetrahydroisoquinoline Derivatives: Discovery of A Potent P-Glycoprotein Ligand Overcoming Multidrug Resistance in Cancer Stem Cells.

Riganti, Chiara / Contino, Marialessandra / Guglielmo, Stefano / Perrone, Maria G / Salaroglio, Iris C / Milosevic, Vladan / Giampietro, Roberta / Leonetti, Francesco / Rolando, Barbara / Lazzarato, Loretta / Colabufo, Nicola A / Fruttero, Roberta

Journal of medicinal chemistry

2019 Volume 62, Issue 2, Page(s) 974–986

Abstract: P-Glycoprotein is a well-known membrane transporter responsible for the efflux of an ample spectrum of anticancer drugs. Its relevance in the management of cancer chemotherapy is increased in view of its high expression in cancer stem cells, a population ...

Abstract	P-Glycoprotein is a well-known membrane transporter responsible for the efflux of an ample spectrum of anticancer drugs. Its relevance in the management of cancer chemotherapy is increased in view of its high expression in cancer stem cells, a population of cancer cells with strong tumor-promoting ability. In the present study, a series of compounds were synthesized through structure modulation of [4'-(6,7-dimethoxy-3,4-dihydro-1 H-isoquinolin-2-ylmethyl)biphenyl-4-ol] (MC70), modifying the phenolic group of the lead compound. Among them, compound 5b emerged for its activity against the transporter (EC
MeSH term(s)	ATP Binding Cassette Transporter, Subfamily B, Member 1/chemistry ; ATP Binding Cassette Transporter, Subfamily B, Member 1/genetics ; ATP Binding Cassette Transporter, Subfamily B, Member 1/metabolism ; Animals ; Antineoplastic Agents/chemistry ; Antineoplastic Agents/metabolism ; Antineoplastic Agents/pharmacology ; Binding Sites ; Cell Line, Tumor ; Cell Survival/drug effects ; Dogs ; Doxorubicin/pharmacology ; Drug Design ; Drug Resistance, Neoplasm/drug effects ; Gene Editing ; Humans ; Ligands ; Madin Darby Canine Kidney Cells ; Molecular Dynamics Simulation ; Neoplastic Stem Cells/cytology ; Neoplastic Stem Cells/drug effects ; Neoplastic Stem Cells/metabolism ; Permeability/drug effects ; Structure-Activity Relationship ; Tetrahydroisoquinolines/chemistry ; Tetrahydroisoquinolines/metabolism ; Tetrahydroisoquinolines/pharmacology
Chemical Substances	ATP Binding Cassette Transporter, Subfamily B, Member 1 ; Antineoplastic Agents ; Ligands ; Tetrahydroisoquinolines ; Doxorubicin (80168379AG)
Language	English
Publishing date	2019-01-09
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	218133-2
ISSN	1520-4804 ; 0022-2623
ISSN (online)	1520-4804
ISSN	0022-2623
DOI	10.1021/acs.jmedchem.8b01655
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Article ; Online: Design and synthesis of fluorescent ligands for the detection of cannabinoid type 2 receptor (CB2R).

Spinelli, Francesco / Giampietro, Roberta / Stefanachi, Angela / Riganti, Chiara / Kopecka, Joanna / Abatematteo, Francesca Serena / Leonetti, Francesco / Colabufo, Nicola Antonio / Mangiatordi, Giuseppe Felice / Nicolotti, Orazio / Perrone, Maria Grazia / Brea, José / Loza, María Isabel / Infantino, Vittoria / Abate, Carmen / Contino, Marialessandra

European journal of medicinal chemistry

2020 Volume 188, Page(s) 112037

Abstract: The Cannabinoid 2 receptor, CB2R, belonging to the endocannabinoid system, ECS, is involved in the first steps of neurodegeneration and cancer evolution and progression and thus its modulation may be exploited in the therapeutic and diagnostic fields. ... ...

Abstract	The Cannabinoid 2 receptor, CB2R, belonging to the endocannabinoid system, ECS, is involved in the first steps of neurodegeneration and cancer evolution and progression and thus its modulation may be exploited in the therapeutic and diagnostic fields. However, CB2Rs distribution and signaling pathways in physiological and pathological conditions are still controversial mainly because of the lack of reliable diagnostic tools. With the aim to produce green and safe systems to detect CB2R, we designed a series of fluorescent ligands with three different green fluorescent moieties (4-dimethylaminophthalimide, 4-DMAP, 7-nitro-4-yl-aminobenzoxadiazole, NBD, and Fluorescein-thiourea, FTU) linked to the N1-position of the CB2R pharmacophore N-adamantyl-4-oxo-1,4-dihydroquinoline-3-carboxamide through polymethylene chains. Compound 28 emerged for its compromise between good pharmacodynamic properties (CB2R K
MeSH term(s)	Cells, Cultured ; Drug Design ; Fluorescent Dyes/chemical synthesis ; Fluorescent Dyes/chemistry ; HEK293 Cells ; Humans ; Ligands ; Molecular Structure ; Receptor, Cannabinoid, CB2/analysis ; Receptor, Cannabinoid, CB2/genetics
Chemical Substances	Fluorescent Dyes ; Ligands ; Receptor, Cannabinoid, CB2
Language	English
Publishing date	2020-01-07
Publishing country	France
Document type	Journal Article
ZDB-ID	188597-2
ISSN	1768-3254 ; 0009-4374 ; 0223-5234
ISSN (online)	1768-3254
ISSN	0009-4374 ; 0223-5234
DOI	10.1016/j.ejmech.2020.112037
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