Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Marialuisa Moccia"'
Autor:
Marialuisa Moccia, Donglin Yang, Naga Rajiv Lakkaniga, Brendan Frett, Nicholas McConnell, Lingtian Zhang, Annalisa Brescia, Giorgia Federico, Lingzhi Zhang, Paolo Salerno, Massimo Santoro, Hong-yu Li, Francesca Carlomagno
Publikováno v:
Scientific Reports, Vol 11, Iss 1, Pp 1-13 (2021)
Abstract We have recently described Pz-1, a benzimidazole-based type-2 RET and VEGFR2 inhibitor. Based on a kinome scan, here we show that Pz-1 is also a potent (IC50
Externí odkaz:
https://doaj.org/article/eab71864d5a542ee8748ff9464f7f61c
Autor:
Marialuisa Moccia, Qingsong Liu, Teresa Guida, Giorgia Federico, Annalisa Brescia, Zheng Zhao, Hwan Geun Choi, Xianming Deng, Li Tan, Jinhua Wang, Marc Billaud, Nathanael S Gray, Francesca Carlomagno, Massimo Santoro
Publikováno v:
PLoS ONE, Vol 10, Iss 6, p e0128364 (2015)
Oncogenic mutation of the RET receptor tyrosine kinase is observed in several human malignancies. Here, we describe three novel type II RET tyrosine kinase inhibitors (TKI), ALW-II-41-27, XMD15-44 and HG-6-63-01, that inhibit the cellular activity of
Externí odkaz:
https://doaj.org/article/d9d2d4a9cf564887b6516be9d95a7465
Autor:
Lingtian Zhang, Marialuisa Moccia, David C. Briggs, Jaideep B. Bharate, Naga Rajiv Lakkaniga, Phillip Knowles, Wei Yan, Phuc Tran, Anupreet Kharbanda, Xiuqi Wang, Yuet-Kin Leung, Brendan Frett, Massimo Santoro, Neil Q. McDonald, Francesca Carlomagno, Hong-yu Li
Publikováno v:
Journal of Medicinal Chemistry. 65:1536-1551
Mutations of the rearranged during transfection (RET) kinase are frequently reported in cancer, which make it as an attractive therapeutic target. Herein, we discovered a series of N-trisubstituted pyrimidine derivatives as potent inhibitors for both
Autor:
Hong-yu Li, Donglin Yang, Annalisa Brescia, Naga Rajiv Lakkaniga, Lingzhi Zhang, Massimo Santoro, Lingtian Zhang, Marialuisa Moccia, Nicholas J. McConnell, Brendan Frett, Paolo Salerno, Francesca Carlomagno, Giorgia Federico
Publikováno v:
Scientific Reports
Scientific Reports, Vol 11, Iss 1, Pp 1-13 (2021)
Scientific Reports, Vol 11, Iss 1, Pp 1-13 (2021)
We have recently described Pz-1, a benzimidazole-based type-2 RET and VEGFR2 inhibitor. Based on a kinome scan, here we show that Pz-1 is also a potent (IC50 50 ~ 1 nM), with a negligible effect against RET- and TRKA-negative cells. By testing mutati
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e8354ad427394efa97209f48734a6fe8
http://hdl.handle.net/11588/870897
http://hdl.handle.net/11588/870897
Autor:
Massimo Santoro, Christophe Landry, Francesca Carlomagno, Lingtian Zhang, Fengping Lv, Hong-yu Li, Brendan Frett, Fabien Gosselet, Marialuisa Moccia, Wei Yan
Publikováno v:
European Journal of Medicinal Chemistry
European Journal of Medicinal Chemistry, Elsevier, 2021, 216, pp.113265. ⟨10.1016/j.ejmech.2021.113265⟩
European Journal of Medicinal Chemistry, Elsevier, 2021, 216, pp.113265. ⟨10.1016/j.ejmech.2021.113265⟩
International audience; Tropomyosin receptor kinase (TRK) represents an attractive oncology target for cancer therapy related to its critical role in cancer formation and progression. NTRK fusions are found to occur in 3.3% of lung cancers, 2.2% of c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0d8ee8758e6c2fcd1873974978441761
http://hdl.handle.net/11588/870898
http://hdl.handle.net/11588/870898
Publikováno v:
Genes (Basel) 11 (2020). doi:10.3390/genes11040424
info:cnr-pdr/source/autori:Santoro M.; Moccia M.; Federico G.; Carlomagno F./titolo:Ret gene fusions in malignancies of the thyroid and other tissues/doi:10.3390%2Fgenes11040424/rivista:Genes (Basel)/anno:2020/pagina_da:/pagina_a:/intervallo_pagine:/volume:11
Genes, Vol 11, Iss 424, p 424 (2020)
Genes
info:cnr-pdr/source/autori:Santoro M.; Moccia M.; Federico G.; Carlomagno F./titolo:Ret gene fusions in malignancies of the thyroid and other tissues/doi:10.3390%2Fgenes11040424/rivista:Genes (Basel)/anno:2020/pagina_da:/pagina_a:/intervallo_pagine:/volume:11
Genes, Vol 11, Iss 424, p 424 (2020)
Genes
Following the identification of the BCR-ABL1 (Breakpoint Cluster Region-ABelson murine Leukemia) fusion in chronic myelogenous leukemia, gene fusions generating chimeric oncoproteins have been recognized as common genomic structural variations in hum
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fff8ea0b7f29aa21b8544a996c721370
http://hdl.handle.net/11588/816056
http://hdl.handle.net/11588/816056
Autor:
Massimo Santoro, Jinhua Wang, Marc Billaud, Xianming Deng, Giorgia Federico, Hwan Geun Choi, Marialuisa Moccia, Francesca Carlomagno, Nathanael S. Gray, Qingsong Liu, Li Tan, Annalisa Brescia, Zheng Zhao, Teresa Guida
Publikováno v:
PLoS ONE, Vol 10, Iss 6, p e0128364 (2015)
PloS one 10 (2015). doi:10.1371/journal.pone.0128364
info:cnr-pdr/source/autori:Moccia M.; Liu Q.; Guida T.; Federico G.; Brescia A.; Zhao Z.; Choi H.G.; Deng X.; Tan L.; Wang J.; Billaud M.; Gray N.S.; Carlomagno F.; Santoro M./titolo:Identification of novel small molecule inhibitors of oncogenic RET kinase/doi:10.1371%2Fjournal.pone.0128364/rivista:PloS one/anno:2015/pagina_da:/pagina_a:/intervallo_pagine:/volume:10
PLoS ONE
PloS one 10 (2015). doi:10.1371/journal.pone.0128364
info:cnr-pdr/source/autori:Moccia M.; Liu Q.; Guida T.; Federico G.; Brescia A.; Zhao Z.; Choi H.G.; Deng X.; Tan L.; Wang J.; Billaud M.; Gray N.S.; Carlomagno F.; Santoro M./titolo:Identification of novel small molecule inhibitors of oncogenic RET kinase/doi:10.1371%2Fjournal.pone.0128364/rivista:PloS one/anno:2015/pagina_da:/pagina_a:/intervallo_pagine:/volume:10
PLoS ONE
Oncogenic mutation of the RET receptor tyrosine kinase is observed in several human malignancies. Here, we describe three novel type II RET tyrosine kinase inhibitors (TKI), ALW-II-41-27, XMD15-44 and HG-6-63-01, that inhibit the cellular activity of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2f8d5be160e758da1aeeb9a85a93bb3c
http://hdl.handle.net/11588/614470
http://hdl.handle.net/11588/614470
Publikováno v:
European journal of medicinal chemistry (Online) 86 (2014): 714–723. doi:10.1016/j.ejmech.2014.09.023
info:cnr-pdr/source/autori:Frett B.; Moccia M.; Carlomagno F.; Santoro M.; Li H.-Y./titolo:Identification of two novel RET kinase inhibitors through MCR-based drug discovery: Design, synthesis and evaluation/doi:10.1016%2Fj.ejmech.2014.09.023/rivista:European journal of medicinal chemistry (Online)/anno:2014/pagina_da:714/pagina_a:723/intervallo_pagine:714–723/volume:86
info:cnr-pdr/source/autori:Frett B.; Moccia M.; Carlomagno F.; Santoro M.; Li H.-Y./titolo:Identification of two novel RET kinase inhibitors through MCR-based drug discovery: Design, synthesis and evaluation/doi:10.1016%2Fj.ejmech.2014.09.023/rivista:European journal of medicinal chemistry (Online)/anno:2014/pagina_da:714/pagina_a:723/intervallo_pagine:714–723/volume:86
From an MCR fragment library, two novel chemical series have been developed as inhibitors of RET, which is a kinase involved in the pathology of medullary thyroid cancer (MTC). Structure activity relationship studies (SAR) identified two sub-micromol
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::989345c87d6ee767a3ab75444f801a16
https://publications.cnr.it/doc/350845
https://publications.cnr.it/doc/350845