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January 31, 2025

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January 7, 2025

November 25, 2024

November 15, 2024

Events

October 11, 2024

August 6, 2024

April 22, 2024

April 12, 2024

August 3, 2021

November 1, 2020

Publications

2024

Integrative ensemble modelling of cetuximab sensitivity in colorectal cancer patient-derived xenografts

Perron U, Grassi E, Chatzipli A, Viviani M, Karakoc E, Trastulla L, Brochier LM, Isella C, Zanella ER, Klett H, Molineris I, Schueler J, Esteller M, Medico E, Conte N, McDermott U, Trusolino L, Bertotti A, Iorio F
Nat Commun (2024), 15(1), 9139
New LsrK Ligands as AI-2 Quorum Sensing Interfering Compounds against Biofilm Formation

Milli G, Pellegrini A, Listro R, Fasolini M, Pagano K, Ragona L, Pietrocola G, Linciano P, Collina S
Med Chem (2024), 67(20), 18139-18156
Present Scenario and Future Landscape of Payloads for ADCs: Focus on DNA- Interacting Agents.

Valsasina B., Orsini P., Terenghi C., Ocana A.
Pharmaceuticals 2024, 17, 1338.
Visible Light Promoted Site-Specific Functionalization of α-Acyloxy Carboxamides: Unlocking a Forbidden Chemical Space in the Passerini Reaction

Brunelli F, Quartieri F, Miletto I, Pulici M, Papeo G, Tron GC
Chemistry (2024), Aug 21. Online ahead of print.
Discovery and optimization of 4-pyrazolyl-2-aminopyrimidine derivatives as potent spleen tyrosine kinase (SYK) inhibitors

Cervi G, D’Alessio R, Bindi S, Buffa L, Burocchi A, Canevari G, Modugno M, Motto I, Saturno G, Orsini P
Eur J Med Chem (2024), 270, 116375
Photocatalytic radical coupling of organoborates with α-Halogenated electron-poor olefins

Caldarelli M, Rezzi SJ, Colombo N, Pirali T, Papeo G
J Org Chem (2024), 5, 89(1), 633-643

Posters

A novel platform of diversified cytotoxins and targeted payloads to drive ADC innovation

P. Orsini, M. Salsa, S. Rizzi, U. Cucchi, D. Faiardi, A. Burocchi, A. Ciavolella, R. Lupi, F. Gasparri, B. Valsasina.
AACR Annual Meeting 2024; April 5-10, 2024; San Diego
Abstract 5805
Cancer Res (2024) 84 (6_Supplement)
The MPS1/TTK inhibitor, NMS-01940153, synergizes with tisotumab vedotin in colorectal cancer

G. Texido, F. Gasparri, A. Ciavolella, L. Gianellini, A. Burocchi, I. Fraietta, A.E. Pedersen, A. Ocaña, R. Colombo, D. Roberti, L. Mahnke, C. Perrera
AACR Annual Meeting 2024; April 5-10, 2024; San Diego
Abstract 509
Cancer Res (2024) 84 (6_Supplement)
Development of 14-amino-anthracyclines as novel payloads for ADC production showing potent anti-tumor activity and improved safety profile

P. Orsini, M. Salsa, A. Burocchi, A. Ciavolella, U. Cucchi, D. Faiardi, S. Rizzi, F. Gasparri, B. Valsasina
38th National Medicinal Chemistry Symposium; June 23-26, 2024; Seattle, WA.
A payload-linker generating machine to quickly move from small molecules to characterized tool ADCs and PDCs

R. Lupi, P. Orsini, M. Salsa, S. Rizzi, U. Cucchi, D. Faiardi, A. Burocchi, A. Ciavolella, F. Gasparri, B. Valsasina
14th World ADC London 2024; March 12-15, 2024; London, UK
Discovery of NMS-0963, a potent, selective and orally available Syk inhibitor with outstanding preclinical activity in diffuse large B-cell lymphoma

L. Buffa, G. Cervi, R. D'Alessio, S. Bindi, A. Burocchi, G. Canevari, M. Modugno, I. Motto, G. Saturno, P. Orsini
58th International Conference on Medicinal Chemistry (RICT 2024); July 3-5, 2024; Bordeaux, France
Photocatalytic Giese reaction of boron-containing compounds with α-Halogenated electron-poor olefins

M. Caldarelli, S.J. Rezzi, N. Colombo, T.Pirali, G. Papeo
EFMC-ISMC 2024; XXVIII EFMC International Symposium on Medicinal Chemistry; September 1-5, 2024; Rome, Italy
Abstract P411

2023

Novel Thienoduocarmycin-Trastuzumab ADC Demonstrates Strong Antitumor Efficacy with Favorable Safety Profile in Preclinical Studies

Valsasina B, Orsini P, Caruso M, Albanese C, Ciavolella A, Cucchi U, Fraietta I, Melillo N, Fiorentini F, Rizzi S, Salsa M, Isacchi A, Gasparri F
Mol Cancer Ther (2023), 22(12), 1465-1478

Posters

NMS-0963 is a novel potent, selective and orally available Syk inhibitor with promising preclinical activity in diffuse large B-cell lymphoma

G. Saturno, M. Modugno, P. Orsini, G. Cervi, L. Buffa, I. Motto, N. Avanzi, M. Montemartini, F. Gasparri, G. Texido, A. Galvani, A. Isacchi
AACR Annual Meeting 2023; 2023 April 14-19; Orlando, FL.
Abstract 4036
Cancer Res (2023) 83 (7_Supplement)
NMS-812, a novel potent PERK inhibitor that also inhibits GCN2, exhibits strong anti tumor activity as single agent and in combination in preclinical models.

C. Perrera, M. Pulici, P. Banfi, N. Avanzi, D. Carenzi, D. Casero, A. Ciavolella, L. Gianellini, F. Gasparri, G. Saturno, B. Valsasina, E. Ardini, A. Montagnoli, A. Galvani, A. Isacchi.
AACR Annual Meeting 2023; 2023 April 14-19; Orlando, FL.
Abstract 1615
Cancer Res (2023) 83 (7_Supplement)
Phase II study on safety and efficacy of NMS-01940153E, an MPS1 inhibitor with first-in class potential, in adult patients with unresectable hepatocellular carcinoma (HCC) previously treated with systemic therapy.

L. Rimassa, M. Reig, S. Damian, D. Roberti, S. Maruzzelli, F. Gasparri, P. Ghioni, M.T. De Pietro, T. Pressiani, M. Sanduzzi Zamparelli, M. Duca, A. Montagnoli, A. Galvani, E. Ardini, A. Isacchi, C. Davite, P. Crivori, L. Mahnke
2023 ASCO Annual Meeting; June 2-6, 2023; at Chicago, IL.
Slide deck
Abstract TPS4185
Journal of Clinical Oncology Volume 41, Number 16_suppl
Initial Results from 2 Phase I Studies of NMS-03305293, a Selective PARP1 Inhibitor

M. Geurts; D. Gramatzki; S. Merler; M. Duca; F. Girardi; U. T. Sener; D. Roberti; G. Saturno; P.
Crivori; A. Montagnoli; L. Mahnke; S. Fu; P. Gaviani; K. A. Jaeckle; J. Zhang; Y. Shi; V.
Guarneri; M. Weller; S. H. Kizilbash; M. J. van den Bent; M. Milella; S. Damian
AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics;
October 11-15 2023; Boston, MA.
Abstract LB_A12
Mol Cancer Ther (2023) 22 (12_Supplement): LB_A12

2022

PROTAC (PROteolysis TArgeting Chimera)

Mirizzi D
Chimica e Farmaceutica (2022), 6, 39-43
Molecular glues: un diverso approccio in drug discovery

Picconi P
Chimica e Farmaceutica (2022), 6, 34-38
Prossimità chimicamente indotta

Mirizzi D
Chimica e Farmaceutica (2022), 5, 48-52
Use of acridinium-based photocatalyst in the Giese-type coupling of arylboronic acids with electron poor olefins

Caldarelli M, Loriz L, Piazza L, Caputo G, DeAmici M, Papeo G
Tetrahedron Letters (2022) 103, 153978
Stereoselective synthesis of 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-one derivatives as PIM kinase inhibitors inspired from marine alkaloids

Casuscelli F, Ardini E, Avanzi N, Badari A, Casale E, Disingrini T, Donati D, Ermoli A, Felder E, Galvani A, Isacchi A, Menichincheri M, Montemartini M, Orrenius C, Piutti C, Salom B, Papeo G
Chirality (2022), 34(11), 1437-1452
BL-01, an Fc-bearing, tetravalent CD20 × CD5 bispecific antibody, redirects multiple immune cells to kill tumors in vitro and in vivo

Interdonato A, Choblet S, Sana M, Valgardsdottir R, Cribioli S, Alzani R, Roth M, Duonor-Cerutti M, Golay J
Cytotherapy (2022), 24(2), 161-171
First-in-man, first-in-class phase I study with the monopolar spindle 1 kinase inhibitor S81694 administered intravenously in adult patients with advanced, metastatic solid tumours

Schöffski P, Awada A, de la Bigne A, Felloussi Z, Burbridge M, Cantero F, Colombo R, Maruzzelli S, Ammattatelli K, de Jonge M, Aftimos P, Dumez H, Sleijfer S
Eur J Cancer (2022), 169 (135-145)
A single-cell analysis of breast cancer cell lines to study tumour heterogeneity and drug response

Gambardella G, Viscido G, Tumaini B, Isacchi A, Bosotti R, di Bernardo D
Nat Commun (2022), 13(1), 1714
A randomized phase III study of fractionated docetaxel, oxaliplatin, capecitabine (low-tox) vs epirubicin, oxaliplatin and capecitabine (eox) in patients with locally advanced unresectable or metastatic gastric cancer: the lega trial

Rosati G, Cella CA, Cavanna L, Codecà C, Prisciandaro M, Mosconi S, Luchena G, Silvestris N, Bernardini I, Casaretti R, Zoratto F, Amoroso D, Ciarlo A, Barni S, Cascinu S, Davite C, Di Sanzo A, Casolaro A, Bilancia D, Labianca R
Gastric Cancer (2022), 25, 783–793

Posters

NMS-173, a potent, covalent second generation IDH1/IDH2 inhibitor

Magnaghi P., Casuscelli F., Ardini E., Parazzoli A., Troiani S., Valsasina B., Texido G., Casale
E., Avanzi N., Orsini P., Nuvoloni S., Salom B., Lombardi Borgia A., Salsi E., Saturno G., Re
Depaolini S., Stellato C., Montagnoli A., Galvani A. and Isacchi A.
34th EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics;
October 26 - 28 2022; Barcelona, Spain
Abstract
European Journal of Cancer, Volume 174, S17

2021

Development of an Effective Tumor-Targeted Contrast Agent for Magnetic Resonance Imaging Based on Mn/H-Ferritin Nanocomplexes

Tullio C, Salvioni L, Bellini M, Degrassi A, Fiandra L, D’Arienzo M, Garbujo S, Rotem R, Testa F, Prosperi D, Colombo M
ACS Appl Bio Mater (2021), 15, 4(11), 7800-7810
A phase II trial of bendamustine in combination with ofatumumab in patients with relapsed or refractory marginal zone B-cell lymphomas

Vannata B, Vanazzi A, Negri M, Liptrott SJ, Bartosek A , Miani M , Di Sanzo A, Cavalli F, Zucca E, Stathis A
Hematol Oncol (2021), 39(1), 60-65.
Development of an Effective Tumor-Targeted Contrast Agent for Magnetic Resonance Imaging Based on Mn/H-Ferritin Nanocomplexes

Tullio C, Salvioni L, Bellini M, Degrassi A, Fiandra L, D’Arienzo M, Garbujo S, Rotem R, Testa F, Prosperi D, Colombo M
ACS Appl Bio Mater (2021), 15, 4(11), 7800-7810
The Coup-TFII orphan nuclear receptor is an activator of the γ-globin gene

Fugazza C, Barbarani G, Elangovan S, Marini MG, Giolitto S, Font-Monclus I, Marongiu MF, Manunza L, Strouboulis J, Cantù C, Gasparri F, Barabino SML, Nakamura Y, Ottolenghi S, Moi P, Ronchi AE.
Haematologica (2021), 106(2), 474-482
RNAdetector: a free user-friendly stand-alone and cloud-based system for RNA-Seq data analysis

La Ferlita A, Alaimo S, Di Bella S, Martorana E, Laliotis G, Bertoni F, Cascione L, Tsichlis P, Ferro A, Bosotti R, Pulvirenti A
BMC Bioinformatics (2021), volume 22, Article number: 298
EV20/NMS-P945, a Novel Thienoindole Based Antibody-Drug Conjugate Targeting HER-3 for Solid Tumors

Capone E, Lattanzio R, Gasparri F, Orsini P, Rossi C, Iacobelli V, De Laurenzi V, Natali PG, Valsasina B, Iacobelli S, Sala GL
Pharmaceutics (2021), 13(4), 483
Identification of unprecedented ATP-competitive choline kinase inhibitors

Quartieri F, Nesi M, Avanzi N, Borghi D, Casale E, Corti E, Cucchi U, Donati D, Fasolini M, Felder E, Galvani A, Giorgini ML, Lomolino A, Menichincheri M, Orrenius C, Perrera C, Re Depaolini S, Riccardi-Sirtori F, Salsi E, Isacchi A, Gnocchi P
Bioorg Med Chem Lett (2021), 51, 128310

2020

A benchmarking of pipelines for detecting ncRNAs from RNA-Seq data

Di Bella S, La Ferlita A, Carapezza G, Alaimo S, Isacchi A, Ferro A, Pulvirenti A, Bosotti R.
Brief Bioinform. 2020 Dec 1;21(6):1987-1998. doi: 10.1093/bib/bbz110. PMID: 31740918
Mining potentially actionable kinase gene fusions in cancer cell lines with the KuNG FU database

Somaschini A, Di Bella S, Cusi C, Raddrizzani L, Leone A, Carapezza G, Mazza T, Isacchi A, Bosotti R.
Sci Data. 2020 Nov 30;7(1):420. doi: 10.1038/s41597-020-00761-2. PMID: 33257674; PMCID: PMC7705673.
A phase II trial of bendamustine in combination with ofatumumab in patients with relapsed or refractory marginal zone B-cell lymphomas

Vannata B, Vanazzi A, Negri M, Liptrott SJ, Bartosek AA, Miani M, Di Sanzo A, Cavalli F, Zucca E, Stathis A.
Hematol Oncol. 2020 Oct 26. doi: 10.1002/hon.2822. Epub ahead of print. PMID: 33103778.
Entrectinib approval by EMA reinforces options for ROS1 and tumour agnostic NTRK targeted cancer therapies

Ardini E, Siena S.
ESMO Open. 2020 Sep;5(5):e000867. doi: 10.1136/esmoopen-2020-000867. PMID: 32907817; PMCID:PMC7481078.
Increased tumor burden in patients with chronic myeloid leukemia after 36 months of imatinib discontinuation

Diral E, Mori S, Antolini L, Abruzzese E, Le Coutre P, Martino B, Pungolino E, Elena C, Bergamaschi M, Assouline S, Di Bona E, Gozzini A, Andrade-Campos M, Stagno F, Iurlo A, Pirola A, Fontana D, Petiti J, Bonanomi ML, Crivori P, Piazza R, Fava C, Gambacorti-Passerini C.
Blood. 2020 Nov 5;136(19):2237-2240. doi: 10.1182/blood.2019004371. PMID: 32518953.

2019

Comprehensive kinome NGS targeted expression profiling by KING-REX

Carapezza G, Cusi C, Rizzo E, Raddrizzani L, Di Bella S, Somaschini A, Leone A, Lupi R, Mutarelli M, Nigro V, di Bernardo D, Magni P, Isacchi A, Bosotti R
BMC Genomics (2019), 20(1), 307
Discovery of Stereospecific PARP-1 Inhibitor Isoindolinone NMS-P515

G. Papeo, P. Orsini, N. Avanzi, D. Borghi, E. Casale, M. Ciomei, A. Cirla, V. Desperati, D. Donati, E. R. Felder, A. Galvani, M. Guanci, A. Isacchi, H. Posteri, S. Rainoldi, Federico Riccardi-Sirtori,§ Alessandra Scolaro,∥and Alessia Montagnoli
ACS Medicinal Chemistry Letters 2019
An antibody-drug conjugate directed to the ALK receptor demonstrates efficacy in preclinical models of neuroblastoma

Sano R, Krytska K, Larmour CE, Raman P, Martinez D, Ligon GF, Lillquist JS, Cucchi U, Orsini P, Rizzi S, Pawel BR, Alvarado D, Mossé YP
Sci Transl Med (2019), 11(483)
Neutrophil Elastase Promotes Linker Cleavage and Paclitaxel Release from an Integrin Targeted Conjugate

Raposo Moreira Dias A, Pina A, Dean A, Lerchen HG, Caruso M, Gasparri F, Fraietta I, Troiani S, Arosio D, Belvisi L, Pignataro L, Dal Corso A, Gennari C
Chemistry (2019), 25(7), 1696-1700
A benchmarking of pipelines for detecting ncRNAs from RNA-Seq data

Di Bella S, La Ferlita A, Carapezza G, Alaimo S, Isacchi A, Ferro A, Pulvirenti A, Bosotti R.
Brief Bioinform (2019), Nov 18 [Epub ahead of print]
Investigating miRNA-IncRNA interactions: Computational tools and resources

Veneziano D, Marceca GP, Di Bella S, Nigita G, Distefano R, Croce CM
Methods Mol Biol (2019), 1970 (Chapt 14), 251-277
Drug-Initiated synthesis of Heterotelechelic Polymer Prodrug Nanoparticles for in vivo imaging and cancer cell targeting

Vinciguerra D, Degrassi A, Mancini L, Mura S, Mougin J, Couvreur P, Nicolas J
Biomacromolecules (2019), 20(7), 2464-2476
Mechanism of action of the tumor vessel targeting agent NGR-hTNF: Role of both NGR peptide and hTNF in cell binding and signaling

Valentinis B, Porcellini S, Asperti C, Cota M, Zhou D, Di Matteo P, Garau G, Zucchelli C, Avanzi NR, Rizzardi GP, Degano M, Musco G, Traversari C
Int J Mol Sci (2019), 20(18), 4511-4533

News

Events

Publications

Posters

Discovery of NMS-0963, a potent, selective and orally available Syk inhibitor with outstanding preclinical activity in diffuse large B-cell lymphoma

Photocatalytic Giese reaction of boron-containing compounds with α-Halogenated electron-poor olefins

Posters

NMS-0963 is a novel potent, selective and orally available Syk inhibitor with promising preclinical activity in diffuse large B-cell lymphoma

NMS-812, a novel potent PERK inhibitor that also inhibits GCN2, exhibits strong anti tumor activity as single agent and in combination in preclinical models.

Posters

NMS-173, a potent, covalent second generation IDH1/IDH2 inhibitor

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