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2. Round robin results of 3D electron diffraction data on inorganic and organic compounds

Author

Gemmi, M., primary, Palatinus, L., additional, Klar, P., additional, Faye, M., additional, Agbemeh, V., additional, Hajizadeh, A., additional, Chintakindi, H., additional, Suresh, A., additional, Jeriga, B., additional, Gemmrich Hernández, L., additional, Santucci, M., additional, Wang, L., additional, Vypritskaia, A., additional, Passuti, S., additional, Cordero Oyonarte, E., additional, Matinyan, S., additional, and Ben Meriem, A., additional

Published
2023
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9. Virtual screening identifies broad-spectrum β-lactamase inhibitors with activity on clinically relevant serine- and metallo-carbapenemases

Author

Spyrakis, F., Santucci, M., Maso, L., Cross, S., Gianquinto, E., Sannio, F., Verdirosa, F., De Luca, F., Docquier, J. D., Cendron, L., Tondi, D., Venturelli, A., Cruciani, G., and Costi, M. P.

Subjects
Virtual screening, Protein Conformation, Tetrazoles, lcsh:Medicine, Microbial Sensitivity Tests, Crystallography, X-Ray, Ligands, Article, beta-Lactamases, Databases, Bacterial Proteins, Anti-Bacterial Agents, Databases, Protein, Drug Design, Drug Discovery, Escherichia coli, Hydrolysis, Molecular Docking Simulation, Protein Binding, Recombinant Proteins, Semicarbazides, Serine, Sulfhydryl Compounds, Sulfonamides, beta-Lactamase Inhibitors, polycyclic compounds, lcsh:Science, Crystallography, Drug discovery, Protein, lcsh:R, biochemical phenomena, metabolism, and nutrition, bacterial infections and mycoses, X-Ray, lcsh:Q
Abstract

Bacteria are known to evade β-lactam antibiotic action by producing β-lactamases (BLs), including carbapenemases, which are able to hydrolyze nearly all available β-lactams. The production of BLs represents one of the best known and most targeted mechanisms of resistance in bacteria. We have performed the parallel screening of commercially available compounds against a panel of clinically relevant BLs: class A CTX-M-15 and KPC-2, subclass B1 NDM-1 and VIM-2 MBLs, and the class C P. aeruginosa AmpC. The results show that all BLs prefer scaffolds having electron pair donors: KPC-2 is preferentially inhibited by sulfonamide and tetrazole-based derivatives, NDM-1 by compounds bearing a thiol, a thiosemicarbazide or thiosemicarbazone moiety, while VIM-2 by triazole-containing molecules. Few broad-spectrum BLs inhibitors were identified; among these, compound 40 potentiates imipenem activity against an NDM-1-producing E. coli clinical strain. The binary complexes of the two most promising compounds binding NDM-1 and VIM-2 were obtained at high resolution, providing strong insights to improve molecular docking simulations, especially regarding the interaction of MBLs with inhibitors.

Published
2020

10. Clinical, histopathological and prognostic features of primary cutaneous acral CD8+ T-cell lymphoma and other dermal CD8+ cutaneous lymphoproliferations: results of an EORTC Cutaneous Lymphoma Group workshop*

Author

Kempf, W., Petrella, T., Willemze, R., Jansen, P., Berti, E., Santucci, M., Geissinger, E., Cerroni, L., Maubec, E., Battistella, M., Goodlad, J., Guenova, E., Lappalainen, K., Ranki, A., Craig, P., Calonje, E., Martin, B., Whittaker, S., Oschlies, I., Wehkamp, U., Nicolay, J. P., Wobser, M., Scarisbruck, J., Pimpinelli, N., Stadler, R., Kerl French, K., Quaglino, P., Lin, J., Chen, L., Beer, M., Emanuel, P., Dalle, S., and Robson, A.

Subjects
Cutaneous, Skin Neoplasms, Lymphoma, CD8-Positive T-Lymphocytes, Humans, Prognosis, Retrospective Studies, Lymphoma, T-Cell, Cutaneous, T-Cell
Published
2022

11. Repurposing the Trypanosomatidic GSK Kinetobox for the Inhibition of Parasitic Pteridine and Dihydrofolate Reductases

Author

Santucci, M., Luciani, R., Gianquinto, E., Pozzi, C., Di Pisa, F., Dello Iacono, L., Landi, G., Tagliazucchi, L., Mangani, S., Spyrakis, F., and Costi, M. P.

Subjects
trypanosomiasis, Drug discovery, DHFR-TS, GSK Kinetobox, Leishmaniasis, Medium throughput screening, Molecular modelling, PTR1, Trypanosomiasis, Article, molecular modelling, drug discovery, RS1-441, Pharmacy and materia medica, parasitic diseases, Medicine, medium throughput screening
Abstract

Three open-source anti-kinetoplastid chemical boxes derived from a whole-cell phenotypic screening by GlaxoSmithKline (Tres Cantos Anti-Kinetoplastid Screening, TCAKS) were exploited for the discovery of a novel core structure inspiring new treatments of parasitic diseases targeting the trypansosmatidic pteridine reductase 1 (PTR1) and dihydrofolate reductase (DHFR) enzymes. In total, 592 compounds were tested through medium-throughput screening assays. A subset of 14 compounds successfully inhibited the enzyme activity in the low micromolar range of at least one of the enzymes from both Trypanosoma brucei and Lesihmania major parasites (pan-inhibitors), or from both PTR1 and DHFR-TS of the same parasite (dual inhibitors). Molecular docking studies of the protein–ligand interaction focused on new scaffolds not reproducing the well-known antifolate core clearly explaining the experimental data. TCMDC-143249, classified as a benzenesulfonamide derivative by the QikProp descriptor tool, showed selective inhibition of PTR1 and growth inhibition of the kinetoplastid parasites in the 5 μM range. In our work, we enlarged the biological profile of the GSK Kinetobox and identified new core structures inhibiting selectively PTR1, effective against the kinetoplastid infectious protozoans. In perspective, we foresee the development of selective PTR1 and DHFR inhibitors for studies of drug combinations.

Published
2021

12. Cannabidiol in Pharmacoresistant Epilepsy: Clinical Pharmacokinetic Data From an Expanded Access Program

Author

Contin M., Mohamed S., Santucci M., Lodi M. A. M., Russo E., Mecarelli O., Bisulli F., Boni A., Cantalupo G., Cesaroni E., Coppola A., Di Bonaventura C., Fetta A., La Neve A., Matricardi S., Michelucci R., Papa A., Pilolli N., Pulitano P., Ragona F., Russo P., Striano P., Volpi L., Zucca C., Contin, M., Mohamed, S., Santucci, M., Lodi, M. A. M., Russo, E., Mecarelli, O., Bisulli, F., Boni, A., Cantalupo, G., Cesaroni, E., Coppola, A., Di Bonaventura, C., Fetta, A., La Neve, A., Matricardi, S., Michelucci, R., Papa, A., Pilolli, N., Pulitano, P., Ragona, F., Russo, P., Striano, P., Volpi, L., and Zucca, C.

Subjects
0301 basic medicine, medicine.medical_specialty, Evening, Gastroenterology, 03 medical and health sciences, cannabidiol, 0302 clinical medicine, Dravet syndrome, Pharmacokinetics, Internal medicine, medicine, Pharmacology (medical), antiseizure medication, Pharmacology, business.industry, epilepsy, Lennox–Gastaut syndrome, pharmacokinetics, lcsh:RM1-950, Venous blood, Brief Research Report, medicine.disease, digestive system diseases, 030104 developmental biology, lcsh:Therapeutics. Pharmacology, Concomitant, Expanded access, business, Cannabidiol, 030217 neurology & neurosurgery, medicine.drug
Abstract

Background and Aim: Data on the clinical pharmacokinetics of cannabidiol (CBD) are scanty. We explored the effect of demographic and clinical variables on plasma concentrations of purified CBD in patients with Dravet (DS) and Lennox–Gastaut syndrome (LGS).Methods: The study design was an open, prospective, multicenter expanded access program (EAP). Venous blood samples were drawn from patients between 8 and 9 am, before the CBD morning dose, 12 h apart from the last evening dose, and then 2.5 h after their usual morning dose.Results: We collected 127 plasma samples (67-morning pre-dosing and 60 post-dosing) from 43 patients (24 females, 19 males), 27 with LGS and 16 with DS. Mean ± standard deviation age was 26 ± 15 years. Duration of CBD treatment averaged 4.2 ± 2.9 months at 13.2 ± 4.6 mg/kg/day. CBD median trough plasma concentration was 91 ng/ml; it doubled to 190 ng/ml 2.5 h post-dosing (p < 0.001). Cannabidiol trough plasma concentrations were linearly related to daily doses (r = 0.564, p < 0.001). Median trough CBD plasma concentration-to-weight-adjusted dose ratio (C/D) was 32% higher (p < 0.02) in plasma samples from subjects aged 18 and over than in those under 18. Sex and concomitant antiseizure medications (ASMs) were not associated with significant variations in CBD C/D, but caution is required due to the potential influence of confounders.Conclusion: These are the first data on CBD pharmacokinetics in children and adults with LGS or DS in a real-world setting. The most relevant finding was the higher CBD C/D in adults. In practice, reduced weight-normalized doses might be required with aging to achieve the same CBD plasma levels.

Published
2021

14. Molecular profiling of blastic plasmacytoid dendritic cell neoplasm reveals a unique pattern and suggests selective sensitivity to NF-kB pathway inhibition

Author

Sapienza, M R, Fuligni, F, Agostinelli, C, Tripodo, C, Righi, S, Laginestra, M A, Pileri, Jr, A, Mancini, M, Rossi, M, Ricci, F, Gazzola, A, Melle, F, Mannu, C, Ulbar, F, Arpinati, M, Paulli, M, Maeda, T, Gibellini, D, Pagano, L, Pimpinelli, N, Santucci, M, Cerroni, L, Croce, C M, Facchetti, F, Piccaluga, P P, and Pileri, S A

Published
2014
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17. Histopathological and immunophenotypical criteria for the diagnosis of Sézary syndrome in differentiation from other erythrodermic skin diseases: a European Organisation for Research and Treatment of Cancer (EORTC) Cutaneous Lymphoma Task Force Study of 97 cases

Author

Klemke, C. D., Booken, N., Weiss, C., Nicolay, J. P., Goerdt, S., Felcht, M., Géraud, C., Kempf, W., Assaf, C., Ortonne, N., Battistella, M., Bagot, M., Knobler, R., Quaglino, P., Arheiliger, B., Santucci, M., Jansen, P., Vermeer, M. H., and Willemze, R.

Published
2015
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21. ATP1A2- and ATP1A3-associated early profound epileptic encephalopathy and polymicrogyria

Author

Vetro, A, Nielsen, HN, Holm, R, Hevner, RF, Parrini, E, Powis, Z, Moller, RS, Bellan, C, Simonati, A, Lesca, G, Helbig, KL, Palmer, EE, Mei, D, Ballardini, E, Van Haeringen, A, Syrbe, S, Leuzzi, V, Cioni, G, Curry, CJ, Costain, G, Santucci, M, Chong, K, Mancini, GMS, Clayton-Smith, J, Bigoni, S, Scheffer, IE, Dobyns, WB, Vilsen, B, Guerrini, R, Vetro, A, Nielsen, HN, Holm, R, Hevner, RF, Parrini, E, Powis, Z, Moller, RS, Bellan, C, Simonati, A, Lesca, G, Helbig, KL, Palmer, EE, Mei, D, Ballardini, E, Van Haeringen, A, Syrbe, S, Leuzzi, V, Cioni, G, Curry, CJ, Costain, G, Santucci, M, Chong, K, Mancini, GMS, Clayton-Smith, J, Bigoni, S, Scheffer, IE, Dobyns, WB, Vilsen, B, and Guerrini, R

Abstract

Constitutional heterozygous mutations of ATP1A2 and ATP1A3, encoding for two distinct isoforms of the Na+/K+-ATPase (NKA) alpha-subunit, have been associated with familial hemiplegic migraine (ATP1A2), alternating hemiplegia of childhood (ATP1A2/A3), rapid-onset dystonia-parkinsonism, cerebellar ataxia-areflexia-progressive optic atrophy, and relapsing encephalopathy with cerebellar ataxia (all ATP1A3). A few reports have described single individuals with heterozygous mutations of ATP1A2/A3 associated with severe childhood epilepsies. Early lethal hydrops fetalis, arthrogryposis, microcephaly, and polymicrogyria have been associated with homozygous truncating mutations in ATP1A2. We investigated the genetic causes of developmental and epileptic encephalopathies variably associated with malformations of cortical development in a large cohort and identified 22 patients with de novo or inherited heterozygous ATP1A2/A3 mutations. We characterized clinical, neuroimaging and neuropathological findings, performed in silico and in vitro assays of the mutations' effects on the NKA-pump function, and studied genotype-phenotype correlations. Twenty-two patients harboured 19 distinct heterozygous mutations of ATP1A2 (six patients, five mutations) and ATP1A3 (16 patients, 14 mutations, including a mosaic individual). Polymicrogyria occurred in 10 (45%) patients, showing a mainly bilateral perisylvian pattern. Most patients manifested early, often neonatal, onset seizures with a multifocal or migrating pattern. A distinctive, 'profound' phenotype, featuring polymicrogyria or progressive brain atrophy and epilepsy, resulted in early lethality in seven patients (32%). In silico evaluation predicted all mutations to be detrimental. We tested 14 mutations in transfected COS-1 cells and demonstrated impaired NKA-pump activity, consistent with severe loss of function. Genotype-phenotype analysis suggested a link between the most severe phenotypes and lack of COS-1 cell survival, and al

Published
2021

22. Results From an Italian Expanded Access Program on Cannabidiol Treatment in Highly Refractory Dravet Syndrome and Lennox–Gastaut Syndrome

Author

Iannone, L. F., Arena, G., Battaglia, Domenica Immacolata, Bisulli, F., Bonanni, P., Boni, A., Canevini, M. P., Cantalupo, G., Cesaroni, E., Contin, M., Coppola, A., Cordelli, D. M., Cricchiuti, G., De Giorgis, V., De Leva, M. F., De Rinaldis, M., D'Orsi, Giovanni Maria, Elia, M., Galimberti, C. A., Morano, A., Granata, T., Guerrini, R., Lodi, M. A. M., La Neve, A., Marchese, F., Masnada, S., Michelucci, R., Nosadini, M., Pilolli, N., Pruna, D., Ragona, F., Rosati, A., Santucci, M., Spalice, A., Pietrafusa, N., Striano, P., Tartara, E., Tassi, L., Papa, A., Zucca, C., Russo, Elisa, Mecarelli, O., Battaglia D. (ORCID:0000-0003-0491-4021), d'Orsi G., Russo E., Iannone, L. F., Arena, G., Battaglia, Domenica Immacolata, Bisulli, F., Bonanni, P., Boni, A., Canevini, M. P., Cantalupo, G., Cesaroni, E., Contin, M., Coppola, A., Cordelli, D. M., Cricchiuti, G., De Giorgis, V., De Leva, M. F., De Rinaldis, M., D'Orsi, Giovanni Maria, Elia, M., Galimberti, C. A., Morano, A., Granata, T., Guerrini, R., Lodi, M. A. M., La Neve, A., Marchese, F., Masnada, S., Michelucci, R., Nosadini, M., Pilolli, N., Pruna, D., Ragona, F., Rosati, A., Santucci, M., Spalice, A., Pietrafusa, N., Striano, P., Tartara, E., Tassi, L., Papa, A., Zucca, C., Russo, Elisa, Mecarelli, O., Battaglia D. (ORCID:0000-0003-0491-4021), d'Orsi G., and Russo E.

Abstract

Background: Purified cannabidiol (CBD) was administered to highly refractory patients with Dravet (DS) or Lennox–Gastaut (LGS) syndromes in an ongoing expanded access program (EAP). Herein, we report interim results on CBD safety and seizure outcomes in patients treated for a 12-month period. Material and Methods: Thirty centers were enrolled from December 2018 to December 2019 within the open-label prospective EAP up to a maximum of 25 mg/kg per day. Adverse effects and liver function tests were assessed after 2 weeks; 1, 3, and 6 months of treatment; and periodically thereafter. Seizure endpoints were the percentage of patients with ≥50 and 100% reduction in seizures compared to baseline. Results: A total of 93 patients were enrolled and included in the safety analysis. Eighty-two patients [27 (32.9%) DS, 55 (67.1%) LGS] with at least 3 months of treatment have been included in the effectiveness analysis; median previously failed antiseizure medications was eight. Pediatric and adult patients were uniformly represented in the cohort. At 3-month follow-up, compared to the 28-day baseline period, the percentage of patients with at least a 50% reduction in seizure frequency was 40.2% (plus 1.2% seizure-free). Retention rate was similar according to diagnosis, while we found an increased number of patients remaining under treatment in the adult group. CBD was mostly coadministered with valproic acid (62.2%) and clobazam (41.5%). In the safety dataset, 29 (31.2%) dropped out: reasons were lack of efficacy [16 (17.2%)] and adverse events (AEs) [12 (12.9%)], and one met withdrawal criteria (1.1%). Most reported AEs were somnolence (22.6%) and diarrhea (11.9%), followed by transaminase elevation and loss of appetite. Conclusions: CBD is associated with improved seizure control also in a considerable proportion of highly refractory patients with DS and LGS independently from clobazam use. Overall, CBD safety and effectiveness are not dose-related in this cohort.

Published
2021

26. Primary cutaneous peripheral T‐cell lymphoma, not otherwise specified: results of a multicentre European Organization for Research and Treatment of Cancer (EORTC) cutaneous lymphoma taskforce study on the clinico‐pathological and prognostic features

Author

Kempf, W., primary, Mitteldorf, C., additional, Battistella, M., additional, Willemze, R., additional, Cerroni, L., additional, Santucci, M., additional, Geissinger, E., additional, Jansen, P., additional, Vermeer, M.H., additional, Marschalko, M., additional, Papadavid, E., additional, Piris, M.A., additional, Ortiz‐Romero, P.L., additional, Novelli, M., additional, Paulli, M., additional, Quaglino, P., additional, Ranki, A., additional, Rodríguez Peralto, J.L., additional, Wobser, M., additional, Auschra, B., additional, and Robson, A., additional

Published
2020
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27. ANTI-A AND SARS-COV-2: AN INTRIGUING ASSOCIATION

Author

Dutra, V.F., primary, Bub, C.B., additional, Yokoyama, A.P.H., additional, Durigon, E.L., additional, Fachini, R.M., additional, Candelaria, G., additional, Santucci, M., additional, Neto, S.W., additional, and Kutner, J.M., additional

Published
2020
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31. DISTRIBUTION OF PROGRESSIVE MYOCLONUS EPILEPSIES IN ITALY; POSITIVELY DIAGNOSED AND UNCLASSIFIED PATIENTS: p827

Author

Canafoglia, L., Franceschetti, S., Michelucci, R., Magaudda, A., Rubboli, G., Tinuper, P., Striano, P., Striano, S., Gambardella, A., Neve, La A., Francavilla, T., Ferlazzo, E., Italiano, D., Gobbi, G., Villani, F., Nardocci, N., Granata, T., Veggiotti, P., Pareyson, D., Coppola, G., Uziel, G., Belcastro, V., Bisulli, F., Spreafico, R., Guerrini, R., Viri, M., Zucca, C., Capovilla, G., Giovagnoli, A. R., Canevini, M. P., Binelli, S., Casazza, M., Cantisani, A. T., Filla, A., Pezzella, M., Santucci, M., Parmeggiani, A., Posar, A., De Maria, G., Marini, C., Bianchi, A., Ragona, F., Freri, E., Mariotti, C., and Costa, P.

Published
2012

36. A bivariate measurement error model for nitrogen and potassium intakes to evaluate the performance of regression calibration in the European Prospective Investigation into Cancer and Nutrition study

Author

Ferrari, P, Roddam, A, Fahey, M T, Jenab, M, Bamia, C, Ocké, M, Amiano, P, Hjartåker, A, Biessy, C, Rinaldi, S, Huybrechts, I, Tjønneland, A, Dethlefsen, C, Niravong, M, Clavel-Chapelon, F, Linseisen, J, Boeing, H, Oikonomou, E, Orfanos, P, Palli, D, de Magistris, Santucci M, Bueno-de-Mesquita, H B, Peeters, PHM, Parr, C L, Braaten, T, Dorronsoro, M, Berenguer, T, Gullberg, B, Johansson, I, Welch, A A, Riboli, E, Bingham, S, and Slimani, N

Published
2009

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