AZD2014, an Inhibitor of mTORC1 and mTORC2, Is Highly Effective in ER+ Breast Cancer When Administered Using Intermittent or Continuous Schedules

No abstract is available for this paper.

• Publication year

  2015

• Venue

  Molecular Cancer Therapeutics

• Publication date

  2015-09-10

• Fields of study

  Biology, Medicine

• Identifiers
  DOI 10.1158/1535-7163.MCT-15-0365PMID 26358751
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Abstract CT233: A phase I study evaluating continuous and intermittent AZD2014 in combination with fulvestrant in patients with ER+ advanced metastatic breast cancer

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• O3.1Targeting the estrogen receptor: old receptor, new drug(s)

  2015cited by this paper
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  2014cited by this paper
• Aromatase inhibitors in the breast cancer clinic: focus on exemestane.

  2014cited by this paper
• Growing knowledge of the mTOR signaling network.

  2014cited by this paper
• mTOR signaling in tumorigenesis.

  2014cited by this paper
• Impact of dual mTORC1/2 mTOR kinase inhibitor AZD8055 on acquired endocrine resistance in breast cancer in vitro

  2014cited by this paper
• PI3K/AKT signaling pathway and cancer: an updated review

  2014cited by this paper
• Rapid induction of apoptosis by PI3K inhibitors is dependent upon their transient inhibition of RAS-ERK signaling.

  2014cited by this paper
• Resistance to everolimus driven by epigenetic regulation of MYC in ER+ breast cancers

  2014cited by this paper
• mTOR inhibitors: changing landscape of endocrine-resistant breast cancer.

  2014cited by this paper
• Where is mTOR and what is it doing there?

  2013cited by this paper
• Clinical instability of breast cancer markers is reflected in long-term in vitro estrogen deprivation studies

  2013cited by this paper
• Optimization of potent and selective dual mTORC1 and mTORC2 inhibitors: the discovery of AZD8055 and AZD2014.

  2013cited by this paper
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  2013cited by this paper
• Connecting mTORC1 signaling to SREBP-1 activation

  2012cited by this paper
• Everolimus in postmenopausal hormone-receptor-positive advanced breast cancer.

  2012cited by this paper
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  2012cited by this paper
• Regulation and function of ribosomal protein S6 kinase (S6K) within mTOR signalling networks.

  2012cited by this paper
• Mammalian TOR signaling to the AGC kinases

  2011cited by this paper
• mTOR kinase inhibition causes feedback-dependent biphasic regulation of AKT signaling.

  2011cited by this paper
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  2010cited by this paper
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  2010cited by this paper
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  2010influential reference
• Allosteric and ATP-competitive kinase inhibitors of mTOR for cancer treatment.

  2010influential reference
• An ATP-competitive Mammalian Target of Rapamycin Inhibitor Reveals Rapamycin-resistant Functions of mTORC1*

  2009cited by this paper
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  2009cited by this paper
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  2005cited by this paper
• A potent specific pure antiestrogen with clinical potential.

  1991cited by this paper
• Tamoxifen: A Review of its Pharmacological Properties and Therapeutic Use in the Treatment of Breast Cancer

  1978cited by this paper

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  2020cites this paper
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  2020cites this paper
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  2019cites this paper
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  2019cites this paper
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  2018cites this paper
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  2018cites this paper
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  2018cites this paper
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  2017cites this paper
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  2017cites this paper
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  2017cites this paper
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  2017cites this paper
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