PMID- 21299441
OWN - NLM
STAT- MEDLINE
DCOM- 20110614
LR  - 20211203
IS  - 1744-7658 (Electronic)
IS  - 1354-3784 (Linking)
VI  - 20
IP  - 3
DP  - 2011 Mar
TI  - Current and future directions in mammalian target of rapamycin inhibitors 
      development.
PG  - 381-94
LID - 10.1517/13543784.2011.541154 [doi]
AB  - INTRODUCTION: The mammalian target of the rapamycin (mTOR) signalling pathway has 
      a central role in the regulation of cell growth, survival and angiogenesis and 
      the frequent dysregulation of this pathway in tumor cells makes it a crucial 
      target in the treatment of cancer. Temsirolimus and everolimus are approved for 
      use in metastatic renal cell carcinoma and temsirolimus is also approved for 
      mantle cell lymphoma. All three rapalogs, temsirolimus, everolimus and 
      deforolimus, are currently being evaluated in Phase III studies in several 
      tumors. AREAS COVERED: This paper provides a review of the published literature 
      on the mTOR pathway and related pathway signaling, analogs and novel mTOR 
      inhibitors. The most recent and important data on the mTOR pathway, the role of 
      mTOR inhibitors in cancer treatment and the current status of development of 
      second-generation highly potent and selective mTOR inhibitors are overviewed. 
      EXPERT OPINION: The published data on new mTOR inhibitors are still limited, but 
      the available preclinical results indicate that they have a potent 
      antiproliferative activity against a broad panel of tumor cell lines, have a 
      favorable safety profile, can obtain disease stabilization or even tumor 
      regression and, in some cases, enhance the efficacy of other targeted or 
      standard-of-care anticancer drugs when used in vivo in preclinical studies.
FAU - Fasolo, Angelica
AU  - Fasolo A
AD  - Istituto Nazionale dei Tumori, via Venezian 1, Milan, Italy.
FAU - Sessa, Cristiana
AU  - Sessa C
LA  - eng
PT  - Journal Article
PT  - Review
DEP - 20110208
PL  - England
TA  - Expert Opin Investig Drugs
JT  - Expert opinion on investigational drugs
JID - 9434197
RN  - 0 (Antineoplastic Agents)
RN  - 0 (Protein Kinase Inhibitors)
RN  - EC 2.7.11.1 (TOR Serine-Threonine Kinases)
RN  - W36ZG6FT64 (Sirolimus)
SB  - IM
MH  - Animals
MH  - Antineoplastic Agents/*pharmacology/therapeutic use
MH  - Clinical Trials, Phase III as Topic
MH  - Humans
MH  - Neoplasms/*drug therapy/enzymology
MH  - Protein Kinase Inhibitors/*pharmacology/therapeutic use
MH  - Signal Transduction/drug effects
MH  - Sirolimus/*analogs & derivatives/pharmacology/therapeutic use
MH  - TOR Serine-Threonine Kinases/*antagonists & inhibitors/metabolism
EDAT- 2011/02/09 06:00
MHDA- 2011/06/15 06:00
CRDT- 2011/02/09 06:00
PHST- 2011/02/09 06:00 [entrez]
PHST- 2011/02/09 06:00 [pubmed]
PHST- 2011/06/15 06:00 [medline]
AID - 10.1517/13543784.2011.541154 [doi]
PST - ppublish
SO  - Expert Opin Investig Drugs. 2011 Mar;20(3):381-94. doi: 
      10.1517/13543784.2011.541154. Epub 2011 Feb 8.