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TPX-0131, a Potent CNS-penetrant, Next-generation Inhibitor of Wild-type ALK and ALK-resistant Mutations

Autor: Xin Zhang, Dayong Zhai, Maria Barrera, Ung Jane, Vivian Nguyen, Dong J. Lee, Herve Aloysius, Wei Deng, Evan Rogers, Jessica Cowell, Ana Parra, Han Zhang, Brion W. Murray

Publikováno v: Molecular cancer therapeutics. 20(9)

Since 2011, with the approval of crizotinib and subsequent approval of four additional targeted therapies, anaplastic lymphoma kinase (ALK) inhibitors have become important treatments for a subset of patients with lung cancer. Each generation of ALK

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5467a422b080aefa64bc71e0aaeb28da
https://pubmed.ncbi.nlm.nih.gov/34158340

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Abstract 1469: TPX-0131, a potent inhibitor of wild type ALK and a broad spectrum of both single and compound ALK resistance mutations

Autor: Han Zhang, Dayong Zhai, Herve Aloysius, Evan Rogers, Xin Zhang, Ana Parra, Vivian Nguyen, Ung Jane, Dong Lee, Wei Deng, Maria Barrera, Jessica Cowell, Brion W. Murray

Publikováno v: Cancer Research. 81:1469-1469

Three generations of ALK inhibitors are approved for the treatment of ALK+ NSCLC but their efficacy is often limited by ALK resistance mutations. The solvent front mutation G1202R and gatekeeper mutation L1196M are major resistance mechanisms to the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::91e92a6cbe4f3f3dde1b53046b035905
https://doi.org/10.1158/1538-7445.am2021-1469

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Abstract 5226: TPX-0131: A next generation macrocyclic ALK inhibitor that overcomes ALK resistant mutations refractory to current approved ALK inhibitors

Autor: Vivian Nguyen, Maria Barrera, Wei Deng, Evan Rogers, Xin Zhang, J. Jean Cui, Han Zhang, Dong Lee, Ana Parra, Brion W. Murray, Dayong Zhai, Ung Jane

Publikováno v: Cancer Research. 80:5226-5226

Anaplastic lymphoma kinase (ALK) gene rearrangements occur in up to 7% of patients with non-small cell lung cancer (NSCLC) with the majority as EML4-ALK fusions. Crizotinib (first generation ALK inhibitor) was the first approved ALK inhibitor for the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::fbf193d812c87980254d376d4677dfb0
https://doi.org/10.1158/1538-7445.am2020-5226

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The next-generation RET inhibitor TPX-0046 is active in drug-resistant and naïve RET-driven cancer models

Autor: Xin Zhang, Vivek Subbiah, Evan Rogers, Dayong Zhai, Laura Rodon, Brion W. Murray, Wei Deng, Dong Lee, Armin Graber, Ung Jane, Alexander Drilon, Zachary Franklin Zimmerman

Publikováno v: Journal of Clinical Oncology. 38:3616-3616

3616 Background: RET fusions/mutations drive oncogenesis in lung and thyroid cancers, and several other malignancies. Selective RET inhibitors (selpercatinib/pralsetinib) are active in patients with these cancers; unfortunately, resistance often occu

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::98d9493b027197431e567002c73b66c8
https://doi.org/10.1200/jco.2020.38.15_suppl.3616

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TPX-0046 is a novel and potent RET/SRC inhibitor for RET-driven cancers

Autor: T. Hu, H. Zhuang, Zachary Franklin Zimmerman, Dong Lee, Vivek Subbiah, Armin Graber, Jeffrey P. Whitten, J. Jean Cui, Ung Jane, Y. Lu, Dayong Zhai, Wei Deng, J. Liu, R. Xin, Zhongdong Huang, Han Zhang, Evan Rogers, Xin Zhang, A. Drilon

Publikováno v: Annals of Oncology. 30:v190-v191

Background Oncogenic activation of the receptor tyrosine kinase (RTK) RET via point mutation or genomic rearrangement has been identified in multiple cancers, including medullary and papillary thyroid cancers, and non-small cell lung cancer (NSCLC).

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::78349b3aff4f6a1f3c474eb428279d4d
https://doi.org/10.1093/annonc/mdz244.068

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Akademický článek

Discovery and development of a novel class of phenoxyacetyl amides as highly potent TRPM8 agonists for use as cooling agents

Autor: Noncovich, Alain, Priest, Chad, Ung, Jane, Patron, Andrew P., Servant, Guy, Brust, Paul, Servant, Nicole, Faber, Nathan, Liu, Hanghui, Gonsalves, Nicole S., Ditschun, Tanya L.

Publikováno v: In Bioorganic & Medicinal Chemistry Letters 15 August 2017 27(16):3931-3938

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Abstract 1325: TPX-0022, a polypharmacology inhibitor of MET/CSF1R/SRC inhibits tumor growth by promoting anti-tumor immune responses

Autor: Yuelie Lu, Jeffrey P. Whitten, Wei Deng, Dayong Zhai, Jing Liu, Zach Zimmerman, Han Zhang, J. Jean Cui, John Huang, Evan Rogers, Armin Graber, Ung Jane, John Lim, Xin Zhang, Dong Lee

Publikováno v: Cancer Research. 79:1325-1325

In the tumor microenvironment, tumor associated macrophages (TAMs) support tumor growth by suppressing antitumor immune responses and promoting angiogenesis, which is associated with disease progression and poor clinical outcomes. In contrast to the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::1267c76f646b15c8963076acb06c4d24
https://doi.org/10.1158/1538-7445.am2019-1325

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Akademický článek

Total synthesis of the novel benzophenone NP-011694

Autor: Noncovich, Alain, Ung, Jane, Patron, Andrew

Publikováno v: In Tetrahedron Letters 12 August 2015 56(33):4836-4839

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