Search Results - "Moccia, Marialuisa"

Targeted activity of the small molecule kinase inhibitor Pz-1 towards RET and TRK kinases by Moccia, Marialuisa, Yang, Donglin, Lakkaniga, Naga Rajiv, Frett, Brendan, McConnell, Nicholas, Zhang, Lingtian, Brescia, Annalisa, Federico, Giorgia, Zhang, Lingzhi, Salerno, Paolo, Santoro, Massimo, Li, Hong-yu, Carlomagno, Francesca

“…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 (IC 50 …”
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Bioisosteric Discovery of NPA101.3, a Second-Generation RET/VEGFR2 Inhibitor Optimized for Single-Agent Polypharmacology by Moccia, Marialuisa, Frett, Brendan, Zhang, Lingtian, Lakkaniga, Naga Rajiv, Briggs, David C, Chauhan, Rakhee, Brescia, Annalisa, Federico, Giorgia, Yan, Wei, Santoro, Massimo, McDonald, Neil Q, Li, Hong-yu, Carlomagno, Francesca

“…RET receptor tyrosine kinase is a driver oncogene in human cancer. We recently identified the clinical drug candidate Pz-1, which targets RET and VEGFR2. A key…”
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Identification of Novel Small Molecule Inhibitors of Oncogenic RET Kinase by Moccia, Marialuisa, Liu, Qingsong, Guida, Teresa, Federico, Giorgia, Brescia, Annalisa, Zhao, Zheng, Choi, Hwan Geun, Deng, Xianming, Tan, Li, Wang, Jinhua, Billaud, Marc, Gray, Nathanael S, Carlomagno, Francesca, Santoro, Massimo

“…Oncogenic mutation of the RET receptor tyrosine kinase is observed in several human malignancies. Here, we describe three novel type II RET tyrosine kinase…”
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RET Gene Fusions in Malignancies of the Thyroid and Other Tissues by Santoro, Massimo, Moccia, Marialuisa, Federico, Giorgia, Carlomagno, Francesca

“…Following the identification of the BCR-ABL1 (Breakpoint Cluster Region-ABelson murine Leukemia) fusion in chronic myelogenous leukemia, gene fusions…”
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Discovery of pyrazolo-thieno[3,2-d]pyrimidinylamino-phenyl acetamides as type-II pan-tropomyosin receptor kinase (TRK) inhibitors: Design, synthesis, and biological evaluation by Yan, Wei, Zhang, Lingtian, Lv, Fengping, Moccia, Marialuisa, Carlomagno, Francesca, Landry, Christophe, Santoro, Massimo, Gosselet, Fabien, Frett, Brendan, Li, Hong-yu

“…Tropomyosin receptor kinase (TRK) represents an attractive oncology target for cancer therapy related to its critical role in cancer formation and progression…”
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Discovery of N‑Trisubstituted Pyrimidine Derivatives as Type I RET and RET Gatekeeper Mutant Inhibitors with a Novel Kinase Binding Pose by Zhang, Lingtian, Moccia, Marialuisa, Briggs, David C, Bharate, Jaideep B, Lakkaniga, Naga Rajiv, Knowles, Phillip, Yan, Wei, Tran, Phuc, Kharbanda, Anupreet, Wang, Xiuqi, Leung, Yuet-Kin, Frett, Brendan, Santoro, Massimo, McDonald, Neil Q, Carlomagno, Francesca, Li, Hong-yu

“…Mutations of the rearranged during transfection (RET) kinase are frequently reported in cancer, which make it as an attractive therapeutic target. Herein, we…”
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Identification of two novel RET kinase inhibitors through MCR-based drug discovery: Design, synthesis and evaluation by Frett, Brendan, Moccia, Marialuisa, Carlomagno, Francesca, Santoro, Massimo, Li, Hong-yu

“…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…”
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Identification of Novel Small Molecule Inhibitors of Oncogenic RET Kinase: e0128364 by Moccia, Marialuisa, Liu, Qingsong, Guida, Teresa, Federico, Giorgia, Brescia, Annalisa, Zhao, Zheng, Choi, Hwan Geun, Deng, Xianming, Tan, Li, Wang, Jinhua

“…Oncogenic mutation of the RET receptor tyrosine kinase is observed in several human malignancies. Here, we describe three novel type II RET tyrosine kinase…”
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