Targeting the mTOR kinase domain: the second generation of mTOR inhibitors

YJ Zhang, Y Duan, XFS Zheng - Drug discovery today, 2011 - Elsevier
The mTOR signaling pathway is dysregulated in∼ 50% of all human malignancies and is a
major cancer drug target. Although rapamycin analogs (rapalogs) have shown clinical …

Drug discovery targeting the mTOR pathway

AM Martelli, F Buontempo, JA McCubrey - Clinical Science, 2018 - portlandpress.com
Mechanistic target of rapamycin (mTOR) is the kinase subunit of two structurally and
functionally distinct large multiprotein complexes, referred to as mTOR complex 1 (mTORC1) …

[HTML][HTML] Current development of the second generation of mTOR inhibitors as anticancer agents

HY Zhou, SL Huang - Chinese journal of cancer, 2012 - ncbi.nlm.nih.gov
The mammalian target of rapamycin (mTOR), a serine/threonine protein kinase, acts as a
“master switch” for cellular anabolic and catabolic processes, regulating the rate of cell …

mTOR inhibitors in cancer therapy

YY Zaytseva, JD Valentino, P Gulhati, BM Evers - Cancer letters, 2012 - Elsevier
The mammalian target of rapamycin (mTOR) plays a key role in regulation of cellular
metabolism, growth, and proliferation. The frequent hyperactivation of mTOR signaling …

Dissecting the role of mTOR: lessons from mTOR inhibitors

RJO Dowling, I Topisirovic, BD Fonseca… - … et Biophysica Acta (BBA …, 2010 - Elsevier
Recent years have observed significant advances in our understanding of how the
serine/threonine kinase target of rapamycin (TOR) controls key cellular processes such as …

[HTML][HTML] mTOR inhibitors in cancer therapy

J Xie, X Wang, CG Proud - F1000Research, 2016 - ncbi.nlm.nih.gov
The mammalian target of rapamycin, mTOR, plays key roles in cell growth and proliferation,
acting at the catalytic subunit of two protein kinase complexes: mTOR complexes 1 and 2 …

mTOR mediated anti-cancer drug discovery

Q Liu, C Thoreen, J Wang, D Sabatini… - Drug Discovery Today …, 2009 - Elsevier
The mammalian target of rapamycin (mTOR) is an evolutionarily conserved serine/threonine
kinase and the founding member of a signaling pathway that regulates many fundamental …

The pharmacology of mTOR inhibition

DA Guertin, DM Sabatini - Science signaling, 2009 - science.org
A flurry of reports indicates that we are entering a new phase in the development of
mammalian target of rapamycin (mTOR)–based therapies for oncology. Here, we summarize …

[HTML][HTML] mTOR inhibitors at a glance

Y Zheng, Y Jiang - Molecular and cellular pharmacology, 2015 - ncbi.nlm.nih.gov
Mechanistic target of rapamycin (mTOR) is a conserved threonine and serine protein kinase
that was identified more than two decades ago as the target of immunosuppressive drug …

Rapamycin passes the torch: a new generation of mTOR inhibitors

D Benjamin, M Colombi, C Moroni… - Nature reviews Drug …, 2011 - nature.com
Mammalian target of rapamycin (mTOR) is an atypical protein kinase that controls growth
and metabolism in response to nutrients, growth factors and cellular energy levels, and it is …