Catalytic mammalian target of rapamycin inhibitors as antineoplastic agents.

Abstract:

:The mammalian target of rapamycin (mTOR) pathway is a major therapeutic target in the treatment of hematological malignancies, as it controls cellular events of high importance for regulation of mRNA translation and protein production. Rapalogs, or first-generation mTOR inhibitors, have produced only modest clinical benefits so far. Limitations to rapalogs likely result from the partial inhibition of mTORC1 substrates and lack of effects on mTORC2. Efforts toward the development of agents with more potent and complete inhibitory effects on the mTOR pathway have resulted in the development of catalytic mTOR inhibitors. Key preclinical and early clinical investigations of several catalytic mTOR inhibitors and potential resistance mechanisms to their activities are summarized here.

journal_name

Leuk Lymphoma

journal_title

Leukemia & lymphoma

authors

Mohindra NA,Platanias LC

doi

10.3109/10428194.2015.1026816

subject

Has Abstract

pub_date

2015-01-01 00:00:00

pages

2518-23

issue

9

eissn

1042-8194

issn

1029-2403

journal_volume

56

pub_type

杂志文章
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